Tetrahydro-fused pyridines as histone deacetylase inhibitors

The invention relates to novel tetrahydrofusedpyridine derivatives, which are used in the pharmaceutical industry for the production of pharmaceutical compositions.

The invention further relates to certain salts of these tetrahydrofusedpyridine derivatives, which are used in the pharmaceutical industry for the production of pharmaceutical compositions.

Transcriptional regulation in cells is a complex biological process, regulated by multiprotein complexes including transcription factors, coactivators and repressors, receptors as well as platform/DNA binding proteins. One basic principle in transcriptional regulation is based on the posttranslational modification of histone proteins, namely histone proteins H2A/B, H3 and H4 forming the octameric histone core complex. The complex N-terminal modifications at lysine residues by acetylation or methylation and at serine residues by phosphorylation constitute part of the so called “histone code” (Strahl & Ellis, Nature 403, 41-45, 2000). In a simple model, acetylation of positively charged lysine residues decreases affinity to negatively charged DNA, which now becomes accessible for the entry of transcription factors.

Histone acetylation and deacetylation is catalysed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). In many cases, HDACs are associated with transcriptional repressor complexes, switching chromatin to a transcriptionally inactive, silent structure (Marks et al. Nature Cancer Rev 1, 194-202, 2001). The opposite holds true for HATs, which are frequently associated with transcriptional activator complexes. Nevertheless, opposite functions for HATs and HDACs have been described in the literature. The cAMP response element binding protein (CBP) and p300 as HATs contain the transcriptional repressor domain CRD1 (cell cycle regulatory domain 1), allowing these proteins to act as transcriptional repressors (Snowden et al., Mol Cell Biol 20, 2676-2686, 2000). Transcriptional signatures of HDAC inhibitors show a similar proportion of induced and repressed genes. In one study, HDAC inhibition abrogates interferon-induced gene transcription presumably by antagonizing the co-activator function of HDAC1 for the interferon stimulated gene factor 3 (ISGF3; Nusinzon & Horvath, Science STKE August 2005). In melanoma cells, interaction of NfκB p65 with STAT1 is dependent on STAT1 acetylation. HDAC inhibitor or interferon α mediated STAT1 hyperacetylation causes the cytoplasmatic retention of NfκB, finally leading to repression of NFκB regulated genes (Krämer et al. Gen Develop 20, 473-485, 2006).

Three different classes of HDACs have been described so far, namely class I (HDAC 1-3, 8) with Mr=42-55 kDa primarily located in the nucleus and sensitive towards inhibition by Trichostatin A (TSA), class II (HDAC 4-7, 9, 10) with Mr=120-130 kDa and TSA sensitivity and class DI (Sir2 homologues) which are quite distinct by their NAD + dependency and TSA insensitivity (Ruijter et al. Biochem. J. 370, 737-749, 2003; Khochbin et al. Curr Opin Gen Dev 11, 162-166, 2001; Verdin et al. Trends Gen 19, 286-293, 2003). HDAC 11 with Mr=39 kDa displayed homology to class I and II family members (Gao et al. J Biol Chem 277,25748-25755, 2002) and is now defined as the sofar only class IV member (Gregoretti et al. J Mol Biol 338, 17-31, 2004). HATs and HDACs exist in large complexes together with transcription factor and platform proteins in cells (Fischle et al. Mol Cell 9, 45-47, 2002).

Substrates different to histone proteins exist. For HDACs these include transcription factors like p53 STAT proteins and TFII E, α-tubulin as a major protein of microtubles, or chaperones like heat shock protein 90 (Hsp90; Johnstone & Licht, Cancer Cell 4, 13-18, 2003). Therefore the correct name for HDACs would be lysine-specific protein deacetylases. As a consequence of these findings, inhibitors of HDACs affect not only chromatin structure and gene transcription but also protein function and stability by regulating protein acetylation in general. This function of HDACs in protein acetylation might also be important for understanding of immediate gene repression by treatment with HDIs (von Lint et al. Gene Expression 5, 245-253, 1996). In this regard, proteins involved in oncogenic transformation, apoptosis regulation and malignant cell growth are of particular importance.

Different publications highlight the pathophysiological importance of reversible histone acetylation for cancer drug development (reviewed by Kramer et al. Trends Endocrin Metabol 12, 294-300, 2001; Marks et al. Nature Cancer Rev 1, 194-202, 2001; Minucci & Pelicci, Nature Rev Cane 6, 38-51, 2006; Yoo, & Jones Nat. Rev. Drug Discov. 5, 37-50 2006):

(i) Mutations of CBP as a HAT are associated with Rubinstein-Taybi syndrome, a cancer predisposition (Murata et al. Hum Mol Genet 10, 1071-1076, 2001), (ii) Aberrant recruitment of HDAC1 activity by transcription factors in acute promyelocytic leukemia (APL) is mediated by the PML-retinoic acid receptor α fusion gene (He et al. Nat genet 18, 126-135, 1998) (iii) Aberrant recruitment of HDAC activity by the overexpressed BCL6 protein was shown in non-Hodgkins lymphoma (Dhordain et al. Nucleic Acid Res 26, 4645-4651, 1998) and finally (iv) Aberrant recruitment of HDAC activity by the AML-ETO fusion protein was shown for acute myelogenous leukemia (AML M2 subtype; Wang et al. Proc Natl Acad Sci USA 95, 10860-10865, 1998). In this AML subtype, the recruitment of HDAC1 activity causally leads to gene silencing, a differentiation block and oncogenic transformation. (v) HDAC1 gene knock-out in mice showed that HDAC1 has a profound function in embryonal stem cell proliferation by repressing cyclin-dependent kinase inhibitors p21 waf1 and p27 kip1 (Lagger et al. Embo J. 21, 2672-2681, 2002). Since p21 waf1 is induced by HDIs in many cancer cell lines, HDAC1 might be a crucial component in cancer cell proliferation as well. Initial siRNA based gene-knock down experiments in HeLa cells support this hypothesis (Glaser et al. 310, 529-536, 2003) (vi) HDAC2 is overexpressed in colon carcinoma upon constitutive activation of the wnt/β-catenin/TCF signalling pathay by loss of functional adenomatosis polyposis coli (APC) protein as reported by Zhu et al. (Cancer Cell 5, 455-463, 2004) (vii) A high expression of HDAC1, 2 and 3 in prostate adenocarcinomas was shown by immunohistochemistry, with HDAC2 as an independent prognostic factor for patient survival and HDAC1/2 correlating positively with tumor grade (Roeske et al, EORTC-NCI-AACR meeting Prague 2006, Abstract 350)

About 2%-3% of all genes are regulated by histone acetylation as estimated by differential display analysis and array based whole genome studies (von Lint et al. Gene Expression 5, 245-253, 1996, Sasakawa et al. Biochem Pharmacol 69, 603-16, 2005). Studies with the HDAC classI/II selective inhibitor suberoylanilide hydroxamic acid (SAHA) in multiple myeloma cells showed that these transcriptional changes can be grouped into distinct functional gene classes important for e.g. regulation of apoptosis or proliferation (Mitsiades et al. Proc Natl Acad Sci 101, pp 540, 2004). In a different study with the natural compound KF228 (Depsipeptide) and the cancer cell lines ACHN (renal cancer), PC3 (prostate cancer) and U937 (histiocytic leukemia), 105 up- and 100 down-regulated genes were identified (Sasakawa et al. Biochem Pharmacol 69, 603-16, 2005). Genes encoding proteins important for cell cycle/mitosis regulation (e.g. p21 waf1 , CyclinA2, SAK, MKLP1), chromatin structure (e.g. histone proteins like histone H1, apoptosis/survival (e.g. caspase 9, TNF/TNFR family members), protein turnover (e.g. ubiquitin ligase E2H) or mitogenic/stress signaling (e.g. MKK3, MAPKAPK3, Ki67) were induced or repressed by treatment with FK228. Two of these genes (caspase 9 and mitogen activated protein kinase phosphatase 1/MKP1 were used as biomarkers to predict the response of human tumors xenografted onto nude mice to therapy with FK228 (Sasakawa et al. Biochem Pharmacol 69, 603-16, 2005). In a different study, the transcriptional changes in the acute human T-lymphoblastic leukemia cell line CCRF-CEM by SAHA and FK228 were studied (Peart et al. Proc Natl Acad Sci 102, 3697-3702, 2005). According to the experimental and statistical condition applied, the expression of 22.1% (SAHA) and 24.8% (FK228) of analyzed genes (about 10.000 unique accession numbers) were changed. Only a small subset of genes was identified that discriminated between both HDAC inhibitors. Finally, HDI regulated genes were functionally clustered showing alterations genes encoding protein involved, for example, in apoptosis regulation (e.g. caspases 3 and 5, APAF1, BCL XL, IKB, TNF) and proliferation (e.g. cyclins G1, G2, E1, B2, E2 and CKD2, CDC25c).

HDAC inhibitors arrest cells at G1 and G2/M within the cell cycle and deplete S-phase cells, as shown for Depsipeptide as an example (Sandor et al., British J Cancer 83, 817-825, 2000). The interaction of HDAC3 with the mitotic kinase Aurora B was shown recently (Li et al. Genes Dev. 20:2566-79, 2006). In this study, phosphorylation of histone H3 at S 10 by Aurora B was dependent on HDAC3 mediated N-terminal histone H3 deacetylation, giving a hint to the partial M-phase arrest seen by many HDIs.

HDAC inhibitory compounds induce p53 and caspase3/8 independent apoptosis and have broad anti-tumor activity. Anti-angiogenic activity was described also, which might be related to down-regulation of VEGF and HIF1α. In summary, HDAC inhibition affects tumor cells at different molecular levels and multiple cellular proteins are targeted.

Interestingly, HDAC inhibitors were found to induce cellular differentiation and this pharmacological activity might contribute to their anti-cancer activity as well. For example it was shown recently that suberoylanilide hydroxamic acid (SAHA) induces differentiation of breast cancer cell lines, exemplified by resynthesis of milk fat membrane globule protein (MFMG), milk fat globule protein and lipid (Munster et al. Cancer Res. 61, 8492, 2001). Also, induction of fetal hemoglobin synthesis in hematopoietic cells of the erythrocyte lineage has been studied in a clinical trial with the butyrate analog AN-9 (Patnaik et al. Clin Cancer Res. 8(7): 2142-8, 2002).

There is growing rational for synergism of HDAC inhibitors with chemotherapeutic as well as target specific cancer drugs. For example, synergism was shown for (i) SAHA with the kinase/cdk inhibitor flavopiridol (Alemenara et al. Leukemia 16, 1331-1343, 2002) or with the death receptor DR4/5 ligand TRAIL (Butler et al. Int J Cancer 119, 944-54, 2006; Sonnemann et al. Invest New drugs 23, 90-109, 2005), (ii) for LAQ-824 with the bcr-abl kinase inhibitor Glivec in CML cells (Nimmanapalli et al. Cancer Res. 63, 5126-5135, 2003) or the KDR/VEGFR2 kinase inhibitor PTK787/ZK222584 in angiogenesis (Qian et al. Cancer Res. 64, 6626-34, 2004), (iii) for SAHA and Trichostatin A (TSA) with etoposide (VP16), cisplatin and doxorubicin (Kim et al. Cancer Res. 63, 7291-7300, 2003), for TSA in combination with retinoid acid in acute myeloid leukemia/AML (Ferrara et al. Canc Res 61, 2-7, 2001) (iv) for LBH589 with the Hsp90 inhibitor 17-allyl-amino-demethoxy-geldanamycin (17-AAG; George et al. Blood online, Oct. 28, 2004) or the proteasome inhibitor bortezomib/Velcade (Maiso et al. Canc Res 66, 5781-5789, 2006, (iiv) PXD101 with 5-FU in colon cancer models (Tumber et al. Canc Chem Pharmacol nov. 2006) and Taxol or Carboplatin in ovarian carcinoma models (Qian et al. Mol Canc ther 5, 2086-95) Also it was shown that HDAC inhibition causes reexpression of estrogen or androgen receptors in breast and prostate cancer cells with the potential to resensitize these tumors to anti-hormone therapy (Yang et al. Cancer Res. 60, 6890-6894, 2000; Nakayama et al. Lab Invest 80, 1789-1796, 2000). Finally, histone deacetylase inhibitors sensitize towards cellular radiation responses as reviewed recently (Karagiannis & El-Osta, Oncogene 25, 3885-93, 2006).

HDAC inhibitors from various chemical classes were described in the literature with four most important classes, namely (i) hydroxamic acid analogs, (ii) benzamide analogs, (iii) cyclic peptides/peptolides and (iv) fatty acid analogs. A comprehensive summary of known HDAC inhibitors was published by various authors (Miller et al. J Med Chem 46, 5097-5116, 2003; Dokmanovic & Marks, J Cell Biochem 96, 293-304, 2005; Drummond et al. Ann Rev Pharmacol Toxicol 45, 495-528, 2005; Bolden J E, et al. Nat Rev Drug Discov 5:769-784, 2006; Sorbera, Drugs of the Future 31, 335-344, 2006). There is only limited data published regarding specificity of these histone deacetylase inhibitors. In general most hydroxamate based HDI are not specific regarding class I and II HDAC enzymes. For example TSA inhibits HDACs 1, 3, 4, 6 and 10 with IC 50 values around 20 nM, whereas HDAC8 was inhibited with IC 50 =0.49 (Tatamiya et al, AACR Annual Meeting 2004, Abstract #2451). But there are exceptions like the experimental HDI Tubacin, selective for the class II enzyme HDAC 6 (Haggarty et al. Proc. Natl. Acad. Sci. USA 100, 4389-4394, 2003). In addition, data on class I selectivity of benzamide HDIs are emerging. MS-275 inhibited class I HDAC1 and 3 with IC 50 =0.51 μM and 1.7 μM, respectively. In contrast class II HDACs 4, 6, 8 and 10 were inhibited with IC 50 values of >100 μM, >100 μM, 82.5 mM and 94.7 μM, respectively (Tatamiya et al, AACR Annual Meeting 2004, Abstract #2451). Comparable data were published by Hu et al. with inhibition of IC 50 =0.3 μM, 8 μM and >100 μM for HDAC1, 3 and 8, respectively (Hu et al. J Pharmacol Exp Therap 307, 720-28, 2003). Finally, the benzamide analog MGCD0103 inhibited HDAC1, 2, 3 and 11 with IC 50 from 0.1-2 μM and HDACs 4 to 8 with IC 50 values >20 μM (Kalita et al. AACR-NCI-EORTC Conference Philadelphia 2005; Abstract C216).

Clinical studies in cancer with HDAC inhibitors are on-going, namely with SAHA (Zolinza™ by Merck Inc.; Kelly et al. J Clin Oncol 23, 3923-31, 2005), CRA-024781 (Pharmacyclics Inc.; Buggy et al, Mol Canc Therap 5, 1309-17, 2006), ITF-2357 (Italfarmaco; J Hepatology 42, 210-17, 2005), Valproic acid (Topotarget; Göttlicher et al. EMBO J. 20, 6969-78, 2001), FK228/Depsipeptide (Gloucester Pharmaceuticals/NC; Nakajima et al. Exp Cell Res 241, 126-33, 19981), MS275 (Berlex-Schering; Ryan et al. J Clin Oncol 23, 3912-22, 2005), NVP LBH-589 (Novartis; Remiszewski et al. J Med Chem 46, 4609-24, 2003), PXD-101 (Topotarget/Curagen; Plumb et al. Mol Canc Therap 2, 721-28, 2003), and MGCD0103 (Methylgene Inc.; Kalita et al. AACR-EORTC-NCI meeting 2005, Abstract C216). These studies showed evidence of clinical efficacy, highlighted recently by partial and complete responses with FK228/Depsipeptide in patients with peripheral T-cell lymphoma (Plekarz et al. Blood, 98, 2865-2868, 2001) and approval in this indication of SAHA (Zolinza™) by Merck & Co., Inc. (Nature Biotechn 25, 17-18, 2007).

Recent publications also showed possible medical use of HDAC inhibitors in diseases different to cancer. These diseases include systemic lupus erythematosus (Mishra et al. J Clin Invest 111, 539-552, 2003; Reilly et al. J. Immunol. 173, 4171-4178, 2004), rheumatoid arthritis (Chung et al. Mol Therapy 8, 707-717, 2003; Nishida et al. Arthritis & Rheumatology 50, 3365-3376, 2004), inflammatory diseases (Leoni et al. Proc Natl Acad Sci USA 99, 2995-3000, 2002), neurodegenerative diseases like Huntington's disease (Steffan et al. Nature 413, 739-743, 2001, Hockly et al. Proc Natl Acad Sci USA 100(4): 2041-6, 2003), cardiac hyperthrophy (Kong et al., Circulation 113, 2579-88, 2006), muscle dystrophy (Minetti et al. Nat Med 12, 1147-50, 2006), adipositas (Lagace & Nachtigal, J Biol. Chem. 279, 18851-860, 2004) and diabetes (Gray & DeMeyts, Diabetes Metab Res Rev 21, 416-33, 2005).

It is known that the loss of histone acetyltransferase (HAT) activity or increased histone deacetylase (HDAC) function leads to neuronal dysfunction and degeneration. Consistent with this fact, HDAC inhibition can restore the HAT-HDAC balance in the CNS in favour of HAT activity, which may facilitate survival, reduce inflammation, and neuronal damage. HDAC inhibitors such as SAHA, TSA, and sodium butyrate have been shown to promote neuronal survival. Thus, HDAC inhibitors have potential applications for the treatment or as adjuncts in neurodegenerative disorders such as stroke, Huntington's disease, Alzheimer's disease, and other such CNS disorders (Langley, B.; Gensert, J. M.; Beal, M. F.; Ratan, R. R. Current Drug Targets—CNS & Neurological Disorders 2005, 4, 41-50).

In fungi such as Candida albicans , HDAC enzymes HDA1 and RPD3 are known to contribute to its virulent character. Some HDAC inhibitors such as SAHA have been shown to inhibit the fluconazole induced resistance induction in Candida cultures (Mai, A.; Rotili, D.; Massa, S.; Brosch, G.; Simonetti, G.; Passariello, C.; Palamara, A. T. Bioorg. Med. Chem. Lett. 2007, 17, 1221-1225). The biological activity of HDAC inhibitors also comprises antiprotozoal, antifungal, and antiviral effects. The HDAC inhibitor TSA initially was discovered as an antifungal antibiotic. Apicidin, a different natural compound type of a HDAC inhibitor, and its derivatives have been tested and shown to be effective antimalarial agents and according to one study, an increase in their HDAC inhibitory activity correlated with their improved antimalarial activity (Meinke, P. T.; Liberator, P. Current Medicinal Chemistry 2001, 8, 211-235).

Cancer chemotherapy was established based on the concept that cancer cells with uncontrolled proliferation and a high proportion of cells in mitosis are killed preferentially. Standard cancer chemotherapeutic drugs finally kill cancer cells upon induction of programmed cell death (“apoptosis”) by targeting basic cellular processes and molecules, namely RNA/DNA (alkylating and carbamoylating agents, platin analogs and topoisomerase inhibitors), metabolism (drugs of this class are named anti-metabolites) as well as the mitotic spindle apparatus (stabilizing and destabilizing tubulin inhibitors). Inhibitors of histone deacetylases (HDIs) constitute a new class of anti cancer drugs with differentiation and apoptosis inducing activity. By targeting histone deacetylases, HDIs effect histone (protein) acetylation and chromatin structure, inducing a complex transcriptional reprogramming, examplified by reactivation of tumor suppressor genes and repression of oncogenes. Beside affecting acetylation of N-terminal lysine residues in core histone proteins, also non-histone targets important for cancer cell biology are modified by acetylation at lysine residues. These non-histone substrates are, for example, heat-shock-protein 90 (Hsp90; Bali et al. J Biol Chem 280, 26729-734, 2005), α-tubulin (Hubbert et al. Nature 417, 455-58, 2002), STAT1 or STAT3 (Yuan et al. Science 307, 269-273, 2005; Krämer et al. Gen & Develop 20, 473-485, 2006) or the p53 tumor suppressor protein (Mol Cell 24, 807-808, 2006). The medical use of HDIs might not be restricted to cancer therapy, since efficacy in animal models for eg, rheumatoid arthritis, neurodegeneration, cardiac hyperthrophy and muscle dystrophy was shown.

Hydroxamic acid substituted fused heterocycles as metalloproteinase inhibitors are described in WO9906410, where as JP2004-203791 describes aromatic compounds that are potent FXa inhibitors.

Various compounds as HDAC inhibitors are reported in WO2005030705, WO03024448 and WO0138322.

There still remains a need in the art for new, well-tolerated and more efficacious inhibitors of HDAC.

It has now been found that the tetrahydrofusedpyridine derivatives, which are described in greater details below, differ profoundly from prior art compounds and are effective inhibitors of histone deacetylases and have surprising and particularly advantageous properties.

In addition and based on the foregoing, it has also been found, that certain salts of these tetrahydrofusedpyridine derivatives have surprising and particularly advantageous properties.

The invention thus relates to compounds of formula I:

wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy (C 1 -C 2 ) alkyl, (C 1 -C 4 ) alkylthio (C 1 -C 2 ) alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, (C 3 -C 7 )cycloalkyl optionally substituted by R1 and/or R2, (C 3 -C 7 )cycloalkyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, pyrrolidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidinyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9; quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, thiazolyl optionally substituted by R1 and/or R2 or indazolyl optionally substituted by R1 and/or R2;

R1 is halogen, hydroxyl, cyano, nitro, amino, carboxyl, (C 1 -C 4 ) alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino;

R2 is halogen, hydroxyl, amino, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or

R1 and R2 when ortho to each other form a methylenedioxy or ethylenedioxy group;

R3 is 3-pyridyl, or 4-pyridyl;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or (C 1 -C 4 )alkylphenylsulfonylamino;

R5 is (C 1 -C 4 )alkylphenylsulfonylamino or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, pyrrolidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl- or thiomorpholinyl-ring;

R8 is pyridyl or (C 1 -C 4 )alkylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—, —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-, —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, —N(R10)CH 2 C(═O) or —N═C(NR11)-;

R10 is hydrogen, (C 1 -C 4 )alkyl or (C 1 -C 4 ) alkoxy(C 1 -C 2 )alkyl;

R11 is hydrogen, hydroxyl, cyano, nitro, or (C 1 -C 4 )alkyl;

B is hydrogen, halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkylcarbonyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, pyrrolidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl- or thiomorpholinyl-ring;

R14 is hydrogen or (C 1 -C 4 )alkyl;

n is an integer selected from 0 to 2;

and the salts of these compounds.

Halogen means fluorine, chlorine, bromine or iodine. The preferred halogen is fluorine and chlorine.

(C 1 -C 4 )alkyl represents a straight chain or branched alkyl radical having 1 to 4 carbon atoms. Examples which may be mentioned are methyl, ethyl, propyl, isopropyl, butyl, isobutyl, secbutyl, ter-butyl.

(C 1 -C 4 )alkoxy represents straight chain or branched alkyl radicals having 1 to 4 carbon atoms and having a terminal oxygen atom. Examples, which may be mentioned, are methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, and tert-butoxy.

(C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl represents (C 1 -C 2 )alkyl radicals having 1 to 2 carbon atoms, which are substituted by one of the abovementioned (C 1 -C 4 )alkoxy radicals. Examples, which may be mentioned, are the methoxymethyl, ethoxymethyl, methoxyethyl, ethoxyethyl, isopropoxymethyl and the isopropoxyethyl radicals, particularly the 2-methoxyethyl, 2-ethoxyethyl and the 2-isopropoxyethyl radicals.

(C 1 -C 4 )alkylthio represents radicals which contain one of the abovementioned (C 1 -C 4 )alkyl radicals and have a terminal sulfur atom. Examples, which may be mentioned, are the butylthio, isobutylthio, sec-butylthio, tert-butylthio, isopropylthio, propylthio and preferably the ethylthio and methylthio radicals.

(C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl represents (C 1 -C 2 )alkyl radicals having 1 to 2 carbon atoms, which are substituted by one of the abovementioned (C 1 -C 4 )alkylthio radicals. Examples, which may be mentioned, are the methylthiomethyl, ethylthiomethyl, methylthioethyl, ethylthioethyl, isopropylthiomethyl, isopropylthioethyl and the butylthioethyl and butylthiomethyl radicals, particularly the 2-methylthioethyl, 2-ethylthioethyl and the 2-isopropylthioethyl radicals.

In addition to the nitrogen atom, mono- or di-(C 1 -C 4 )alkylamino radicals contain one or two of the above-mentioned (C 1 -C 4 )alkyl radicals independently. Examples which may be mentioned are methylamino, ethylamino, propylamino, isopropylamino, and butylamino. Di-(C 1 -C 4 )alkylamino is preferred and here, in particular, dimethyl-, ethylmethyl-, diethyl- or diisopropylamino.

Mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl represents (C 1 -C 2 )alkyl radicals having 1 to 2 carbon atoms, which are substituted by one of the above mentioned mono- or di-(C 1 -C 4 )alkylamino radicals. Examples which may be mentioned are dimethyl-, diethyl- or diisopropylaminomethyl, dimethyl-, diethyl- or diisopropylaminoethyl.

(C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, represents straight chain or branched alkyl radicals having 1 to 4 carbon atoms wherein one or more hydrogen atoms are replaced by a fluorine atom. Examples which may be mentioned are the 2,2,3,3,3-pentafluoropropyl, the perfluoroethyl, the 1,2,2-trifluoroethyl, the 1,1,2,2-tetrafluoroethyl, the 2,2,2-trifluoroethyl, the trifluoromethyl, the difluoromethyl and, in particular, the 2,2-difluoroethyl radicals.

(C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine represents straight chain or branched alkyl radicals having 1 to 4 carbon atoms and a terminal oxygen atom. Examples which may be mentioned are the 2,2,3,3,3-pentafluoropropoxy, the perfluoroethoxy, the 1,2,2-trifluoroethoxy, the 1,1,2,2-tetrafluoroethoxy, the 2,2,2-trifluoroethoxy, the trifluoromethoxy and the difluoromethoxy radical, of which the difluoromethoxy and trifluoromethoxy radical is preferred. “Predominantly” in this connection means that more than half of the hydrogen atoms of the C 1 -C 4 -alkoxy group are replaced by fluorine atoms.

(C 1 -C 4 )alkoxycarbonyl represents a radical which, in addition to the carbonyl group, contains one of the above mentioned alkoxy radicals. Examples which may be mentioned are methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl and butoxycarbonyl.

(C 1 -C 4 )alkylcarbonylamino represents a radical, which contains one of the above mentioned alkyl radicals linked to a carbonyl group, which is then linked to a terminal amino group. Examples, which may be mentioned are methylcarbonylamino, ethylcarbonylamino, propylcarbonylamino, isopropylcarbonylamino.

(C 3 -C 7 )cycloalkyl represents cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, of which cyclohexyl and cyclopropyl is preferred.

B is selected from hydrogen, halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, N(R12)R13 wherein R12 and R13 are as defined above. Examples which may be mentioned are fluorine, chlorine, methyl, ethyl, isopropyl, propyl, methoxy, 2-thienyl, 3-thienyl, pyrrolidin-1-yl, and dimethylamino.

B can be attached in the ortho, meta or para position with respect to the binding position in which the amino radical is bonded to the phenyl ring, whereby, preference is given to the attachment in the para or ortho position.

The heterocyclic groups mentioned herein refer, unless otherwise noted, in particular to all of the possible positional isomers thereof. Thus, for example, the term pyridyl or pyridinyl, alone or as part of another group, includes pyridin-2-yl, pyridin-3-yl and pyridin-4-yl with pyridin-4-yl being preferred. Thienyl includes thiophen-2-yl and thiophen-3-yl. The heterocyclic groups mentioned herein refer, unless otherwise noted, to all of the possible tautomers, e.g. the keto/enol tautomers, thereof, in pure form as well as any mixtures thereof. Thus, for example, pyridine compounds which are substituted by a hydroxyl or an oxo group in the 2- or 4-position of the pyridine ring can exist in different tautomeric forms, i.e. the enol and the keto form, which are both contemplated by the present invention in pure form as well as in any mixtures thereof.

Constituents, which are optionally substituted as stated herein, may be substituted, unless otherwise noted, at any possible position.

Compounds of the invention and salts thereof containing a double bond may exist as E isomers and Z isomers. Both said isomers as well as mixtures of said isomers are included in the invention. The Z isomer is the geometric isomer in which the carbon atoms connected by the double bond each have the two highest ranking groups on the same side of the double bond. The E isomer is the geometric isomer in which the carbon atoms connected by the double bond each have the two highest ranking groups on opposite sides of the double bond.

In a preferred embodiment the invention relates to compounds of formula I:

wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, (C 3 -C 7 )cycloalkyl optionally substituted by R1 and/or R2, (C 3 -C 7 )cycloalkyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, pyrrolidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidinyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9; quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 is halogen, hydroxyl, cyano, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino;

R2 is halogen, hydroxyl, amino, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or

R1 and R2 when ortho to each other form a methylenedioxy or ethylenedioxy group;

R3 is 3-pyridyl, or 4-pyridyl;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or (C 1 -C 4 )alkylphenylsulfonylamino;

R5 is (C 1 -C 4 )alkylphenylsulfonylamino or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, pyrrolidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl- or thiomorpholinyl-ring;

R8 is pyridyl or (C 1 -C 4 )alkylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—, —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-, —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, or —N═C(NR11)-;

R10 is hydrogen, (C 1 -C 4 )alkyl or (C 1 -C 4 ) alkoxy(C 1 -C 2 )alkyl;

R11 is hydrogen, hydroxyl, cyano, nitro, or (C 1 -C 4 )alkyl;

B is hydrogen, halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkylcarbonyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, pyrrolidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl- or thiomorpholinyl-ring;

R14 is hydrogen or (C 1 -C 4 )alkyl;

n is an integer selected from 0 to 2;

and the salts of these compounds.

In a preferred embodiment the invention relates to compounds of formula I as defined above, wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 ) alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio (C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidinyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9, quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2 or indazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, cyano, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino;

R2 is fluorine, hydroxyl, amino, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or

R1 and R2 when ortho to each other form a methylenedioxy or ethylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

R5 is methylphenylsulfonylamino, or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—, —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-, —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, —N(R10)CH 2 C(═O)— or —N═C(NR11)-;

R10 is hydrogen, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy (C 1 -C 2 )alkyl;

R11 is hydrogen, hydroxyl, cyano, nitro, methyl, or ethyl;

B is hydrogen, halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-, ring;

R14 is hydrogen or methyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

In a further preferred embodiment the invention relates to compounds of formula I as defined above,

wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9, quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2 or indazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino,

R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—, —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-, —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, —N(R10)CH 2 C(═O)— or —N═C(NR11)-;

R10 is hydrogen, methyl, ethyl, propyl, methoxyethyl, ethoxyethyl, methoxymethyl, or ethoxymethyl;

R11 is hydrogen, hydroxyl, cyano, nitro, methyl, or ethyl;

B is hydrogen, fluorine, chlorine, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, thienyl, N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, methyl, ethyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-ring;

R14 is hydrogen or methyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═O)C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino or (C 1 -C 4 )alkylcarbonylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring; R10 is hydrogen or (C 1 -C 4 )alkyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2 or indazolyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino or or (C 1 -C 4 )alkylcarbonylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R10 is hydrogen, (C 1 -C 4 )alkyl, methoxyethyl, ethoxyethyl, methoxymethyl, or ethoxymethyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-ring; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N(R10)CH 2 C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2 or indazolyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy (C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino or or (C 1 -C 4 )alkylcarbonylamino; R2 is hydroxyl, (C 1 -C 4 ) alkyl, or (C 1 -C 4 ) alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R10 is hydrogen, (C 1 -C 4 )alkyl, methoxyethyl, ethoxyethyl, methoxymethyl, or ethoxymethyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 ) alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 ) alkyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-ring; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —C(═O)—;

A is (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy (C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 ) alkyl or (C 1 -C 4 )alkoxy; R4 is phenyl or phenoxy; B is hydrogen, fluorine, chlorine, (C 1 -C 4 ) alkyl, or thienyl; R14 Is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═N(R11))-;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl or phenoxy; R10 is hydrogen, or (C 1 -C 4 )alkyl; R11 is hydrogen, cyano, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N═C(R11)-;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; R11 is hydrogen, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N(R10)C(═C(R11))-;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 ) alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; R10 is hydrogen, or (C 1 -C 4 )alkyl; R11 is hydrogen, nitro, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n S(O) 2 —;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, thiazolyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino; R2 is (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N(R10)C(═S)—;

A is (C 1 -C 4 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 ) alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl; R10 is hydrogen or (C 1 -C 4 )alkyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —OCH 2 C(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n OC(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C r C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —C═C—C(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is bond;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, or pyrimidinyl substituted by R8; R1 is fluorine, hydroxyl, nitro, amino, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl, phenoxy, benzylNHC(═O)NH—, or methylphenylsulfonylamino; R5 is methylphenylsulfonylamino, or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R8 is pyridyl or methylphenylsulfonylamino; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

A special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is bond and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n S(O) 2 — and A, B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═S)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n OC(═O)— and A, B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N(R10)CH 2 C(═O)— and A, B, R10, have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═NR11)- and A, B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═S)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C═C—C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(R11)- and A, B, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)C(═O)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —OCH 2 C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N(R10)C(═CR11)- and A, B, R10, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(NR11)- and A, B, R11 have the meanings as defined above and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is bond, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n S(O) 2 —, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═S)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n OC(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N(R10)CH 2 C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C r C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═NR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═S)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C═C—C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(R11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —OCH 2 C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and, B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

and L is —N(R10)C(═CR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

and L is —N═C(NR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is bond; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino,

R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is bond; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino,

R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n S(O) 2 —; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 Is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

and B, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n S(O) 2 —; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino; and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n OC(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n OC(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N(R10)CH 2 C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

and B, R10, have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N(R10)CH 2 C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═NR11)- or —N═C(NR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl; nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy; and B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═NR11)- or —N═C(NR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═S)—; A cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl; and B, R10, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═S)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C═C—C(═O)—; A is phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C═C—C(═O)—; A phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N═C(R11)-; A phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4 or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N═C(R11)-; A phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4 or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; R11 has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and

L is —(CH 2 ) n N(R10)C(═O)C(═O)—, A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino; R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

and B, R10, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —OCH 2 C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —OCH 2 C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

L is —N(R10)C(═CR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B, R10, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

L is —N(R10)C(═CR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, R11 have the meanings as defined above, and the salts of those compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n S(O) 2 — or —O(CH 2 ) n C(═O)—;

R10 is hydrogen or (C 1 -C 4 )alkyl;

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n S(O) 2 — or —O(CH 2 ) n C(═O)—;

R10 is hydrogen or (C 1 -C 4 )alkyl;

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n S(O) 2 — or —O(CH 2 ) n C(═O)—;

R10 is hydrogen or (C 1 -C 4 )alkyl;

R14 is hydrogen or methyl:

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n S(O) 2 — or —O(CH 2 ) n C(═O)—;

R10 is hydrogen or (C 1 -C 4 )allyl;

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 ) alkyl, (C 1 -C 4 ) alkoxy, (C 1 -C 4 ) alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 ) alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n S(O) 2 — or —O(CH 2 ) n C(═O)—;

R10 is hydrogen or (C 1 -C 4 )alkyl;

R14 is hydrogen or methyl:

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

In another preferred embodiment the invention relates to compounds of formula I as defined above,

wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidinyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9, quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, cyano, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino;

R2 is fluorine, hydroxyl, amino, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or

R1 and R2 when ortho to each other form a methylenedioxy or ethylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

R5 is methylphenylsulfonylamino, or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—; —(CH 2 ) n N(R10)C(═O)—; —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-; —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, or —N═C(NR11)-;

R10 is hydrogen, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl;

R11 is hydrogen, hydroxyl, cyano, nitro, methyl, or ethyl;

B is hydrogen, halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-, ring;

R14 is hydrogen or methyl;

n is an integer selected from 0 and 1; and the salts of these compounds.

In a further preferred embodiment the invention relates to compounds of formula I as defined above,

wherein

ring D and ring E together form a fused ring system selected from

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, triazinyl optionally substituted by R1 and/or R2, triazinyl substituted by R9, quinolinyl optionally substituted by R1 and/or R2, isoquinolinyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino,

R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

R9 is piperidinyl;

L is bond, —(CH 2 ) n S(O) 2 —, —C(═O)—, —C(═S)—, —(CH 2 ) n OC(═O)—, —(CH 2 ) n N(R10)C(═O)—, —(CH 2 ) n N(R10)C(═NR11)-, —(CH 2 ) n N(R10)C(═S)—, —C═C—C(═O)—, —N═C(R11)-, —(CH 2 ) n N(R10)C(═O)C(═O)—, —OCH 2 C(═O)—, —N(R10)C(═CR11)-, or —N═C(NR11)-;

R10 is hydrogen, methyl, ethyl, propyl, methoxyethyl, ethoxyethyl, methoxymethyl, or ethoxymethyl;

R11 is hydrogen, hydroxyl, cyano, nitro, methyl, or ethyl;

B is hydrogen, fluorine, chlorine, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, thienyl, N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, methyl, ethyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-ring;

R14 is hydrogen or methyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═O)C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C r C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino or (C 1 -C 4 )alkylcarbonylamino;

R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or

R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

R10 is hydrogen or (C 1 -C 4 )alkyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl; n is an integer selected from 0 and 1; and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I wherein ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino or or (C 1 -C 4 )alkylcarbonylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R10 is hydrogen, (C 1 -C 4 )alkyl, methoxyethyl, ethoxyethyl, methoxymethyl, or ethoxymethyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, thienyl, or N(R12)R13 wherein R12 and R13 independently of one another are hydrogen, (C 1 -C 4 )alkyl, or R12 and R13 together and with inclusion of the nitrogen atom to which they are bonded form a pyrrolidinyl-ring; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —C(═O)—;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy; R4 is phenyl or phenoxy; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, or thienyl; R14 Is hydrogen or methyl; and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n N(R10)C(═N(R11))-;

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl, mono- or -di(C 1 -C 4 )alkylamino(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl or phenoxy; R10 is hydrogen, or (C 1 -C 4 )alkyl; R11 is hydrogen, cyano, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N═C(R11)-;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; R11 is hydrogen, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N(R10)C(═C(R11))-;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; R10 is hydrogen, or (C 1 -C 4 )alkyl; R11 is hydrogen, nitro, or methyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen, or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n S(O) 2 —;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, thiazolyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, mono- or -di(C 1 -C 4 )alkylamino, or (C 1 -C 4 )alkylcarbonylamino; R2 is (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —N(R10)C(═S)—;

A is (C 1 -C 4 )alkyl, cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or

R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R3 is 3-pyridyl or 4-pyridyl; R4 is phenyl; R10 is hydrogen or (C 1 -C 4 )alkyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —OCH 2 C(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy, or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —(CH 2 ) n OC(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5; R1 is fluorine, hydroxyl, nitro, amino, carboxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl, phenoxy, or 4-methylpiperazinyl; R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl; n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is —C═C—C(═O)—;

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2; R1 is fluorine, hydroxyl, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl; and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form a fused ring system selected from

wherein L is bond;

A is (C 1 -C 4 )allyl, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, or pyrimidinyl substituted by R8; R1 is fluorine, hydroxyl, nitro, amino, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino; R2 is hydroxyl, (C 1 -C 4 )alkyl, or (C 1 -C 4 )alkoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl, phenoxy, benzylNHC(═O)NH—, or methylphenylsulfonylamino; R5 is methylphenylsulfonylamino, or N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R8 is pyridyl or methylphenylsulfonylamino; B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl; R14 is hydrogen or methyl;

and the salts of these compounds.

A special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is bond and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n S(O) 2 — and A, B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═S)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n OC(═O)— and A, B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═NR11)- and A, B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═S)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C═C—C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(R11)- and A, B, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)C(═O)— and A, B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —OCH 2 C(═O)— and A, B have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N(R10)C(═CR11)- and A, B, R10, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(NR11)- and A, B, R11 have the meanings as defined above and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is bond, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n S(O) 2 —, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C(═S)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n OC(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═NR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═S)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —C═C—C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —N═C(R11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —(CH 2 ) n N(R10)C(═O)C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

and L is —OCH 2 C(═O)—, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and, B has the meaning as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

and L is —N(R10)C(═CR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R10, R11 have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

and L is —N═C(NR11)-, A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, or (C 1 -C 4 )alkylthio(C 1 -C 2 )alkyl and B, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is bond; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino; R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or R1 and R2 when ortho to each other form a methylenedioxy group; R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino, R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring; R8 is pyridyl or methylphenylsulfonylamino; and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is bond; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, pyrimidinyl optionally substituted by R1 and/or R2, pyrimidyl substituted by R8, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino,

R5 is methylphenylsulfonylamino, N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

R8 is pyridyl or methylphenylsulfonylamino;

and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n S(O) 2 —; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 Is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

and B, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n S(O) 2 —; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, thienyl optionally substituted by R1 and/or R2, or thiazolyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino; and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl, phenoxy, 4-methylpiperazinyl, benzylNHC(═O)NH—, or methylphenylsulfonylamino;

and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

and B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n OC(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

and B, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n OC(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, or diethylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl, and n has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

and B, R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, azetidinyl optionally substituted by R1 and/or R2, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, or morpholinyl-ring;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═NR11)- or —N═C(NR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

and B, R10, R11, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═NR11)- or —N═C(NR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl or phenoxy;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, R11, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═S)—; A cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl; and B, R10, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═S)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, piperidinyl optionally substituted by R1 and/or R2, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl;

and R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C═C—C(═O)—; A is phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —C═C—C(═O)—; A phenyl optionally substituted by R1 and/or R2, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N═C(R11)-; A phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4 or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —N═C(R11)-; A phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4 or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; R11 has the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)C(═O)—, A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring; and B, R10, n have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —(CH 2 ) n N(R10)C(═O)C(═O)—; A is cyclohexyl optionally substituted by R1 and/or R2, cyclohexyl substituted by R3, phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, naphthyl optionally substituted by R1 and/or R2, pyridyl optionally substituted by R1 and/or R2, pyridyl substituted by R5, quinolinyl optionally substituted by R1 and/or R2, or isoquinolinyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R3 is 3-pyridyl or 4-pyridyl;

R4 is phenyl, phenoxy, or 4-methylpiperazinyl;

R5 is —N(R6)R7, wherein R6 and R7 together and with inclusion of the nitrogen atom to which they are bonded form an azetidinyl-, piperidinyl-, piperazinyl-, 4-methylpiperazinyl-, morpholinyl-ring;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; R10, n have the meanings as defined above, and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —OCH 2 C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B has the meaning as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form the fused ring system

L is —OCH 2 C(═O)—; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and the salts of those compounds.

Another special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

L is —N(R10)C(═CR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl; and B, R10, R11 have the meanings as defined above, and the salts of those compounds.

A further special embodiment of the compounds of the present invention include those compounds of formula I wherein

ring D and ring E together form a fused ring system selected from

L is —N(R10)C(═CR11)-; A is phenyl optionally substituted by R1 and/or R2, phenyl substituted by R4, or naphthyl optionally substituted by R1 and/or R2;

R1 is fluorine, hydroxyl, nitro, cyano, amino, carboxyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, isopropoxy, trifluoromethyl, difluoromethyl, difluoromethoxy, trifluoromethoxy, methoxyethyl, ethoxyethyl, methoxymethyl, ethoxymethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, methylamino, dimethylamino, ethylamino, diethylamino, methylcarbonylamino, or ethylcarbonylamino;

R2 is fluorine, hydroxyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, or isopropoxy or

R1 and R2 when ortho to each other form a methylenedioxy group;

R4 is phenyl;

B is fluorine, chlorine, methoxy, isopropyl or thienyl, in particular thienyl; and R10, R11 have the meanings as defined above, and the salts of those compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)— or —(CH 2 ) n S(O) 2 —;

R10 is hydrogen or (C 1 -C 4 )alkyl;

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I

wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )alkyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)— or —(CH 2 ) n S(O) 2 —;

R10 is hydrogen or (C 1 -C 4 )alkyl;

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another preferred embodiment of the present invention relates to compounds of formula I wherein

ring D and ring E together form the fused ring system

A is (C 1 -C 4 )alkyl, phenyl optionally substituted by R1 and/or R2, naphthyl optionally substituted by R1 and/or R2, or pyridyl optionally substituted by R1 and/or R2;

R1 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl which is partially or completely substituted by fluorine, (C 1 -C 4 )alkoxy which is predominantly or completely substituted by fluorine, (C 1 -C 4 )alkoxy(C 1 -C 2 )allyl, (C 1 -C 4 )alkoxycarbonyl, or mono- or -di(C 1 -C 4 )alkylamino;

R2 is (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or

R1 and R2 when ortho to each other form a methylenedioxy group;

L is —(CH 2 ) n N(R10)C(═O)— or —(CH 2 ) n S(O) 2 —;

R10 is hydrogen or (C 1 -C 4 )alkyl;

R14 is hydrogen or methyl:

B is hydrogen, fluorine, chlorine, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, or thienyl;

n is an integer selected from 0 and 1;

and the salts of these compounds.

Another embodiment of the compounds according to the present invention relates to compounds of formula I selected from:

N 2 -(2-aminophenyl)-N 5 -biphenyl-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -benzyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, Methyl 4-[({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)amino]benzoate, N 2 -(2-aminophenyl)-N 5 -(4-phenoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[2-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -quinolin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-methylphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(pyridin-3-ylmethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -ethyl-N 5 -isopropyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(dimethylamino)phenyl]-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -methyl-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -ethyl-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(4-methylpiperazin-1-yl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-morpholin-4-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-azetidin-1-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[6-(dimethylamino)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -butyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-pyridin-3-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -piperidin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-pyridin-4-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-pyrrolidin-1-ylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N-(2-aminophenyl)-5-[{[4-(dimethylamino)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-4-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]-thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[isoquinolin-5-ylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-3-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-methoxypyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(dimethylamino)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo{[4-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-morpholin-4-ylpyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(1,3-benzodioxol-5-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methylphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(5-methylpyridin-2-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[oxo(quinolin-3-ylamino)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(4-methylpiperazin-1-yl)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(pyridin-3-ylmethyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylcarbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methylbenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 4-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)benzoate, N-(2-aminophenyl)-5-[4-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, 5-Acetyl-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methoxybenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(quinolin-3-ylcarbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(6-methylpyridin-3-yl)carbonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-({[4-(dimethylamino)phenyl]amino}carbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(piperidin-4-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{([(4-pyridin-3-ylcyclohexyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(isoquinolin-5-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[benzylamino)(imino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[[(4-methoxyphenyl)amino](methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(cyanoimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(3,4-dimethoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(2-methylphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino){[4-(dimethylamino)phenyl]amino}methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino)(pentylamino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(cyanoimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(cyano amino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{(cyanoamino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{(cyanoamino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{N-[4-(dimethylamino)phenyl]ethanimidoyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-(butylamino)-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(3,4-dimethoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(1-methylethyl)phenyl]-5-{1-[(4-methoxyphenyl)amino]-2-nitroethenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-fluorophenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(benzylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 5-[(4-acetamidophenyl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-thienylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 3-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}sulfonyl)thiophene-2-carboxylate, 5-[(2-acetamido-4-methyl-1,3-thiazol-5-yl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-fluorophenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(isopropylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(phenoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(2-naphthyloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(biphenyl-4-yloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Biphenyl-4-yl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 4-Methylphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-Methoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-(Propoxycarbonyl)phenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 2-Naphthyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 3,4-Dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, Butyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Pyridin-3-ylmethyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, N-(2-aminophenyl)-5-[3-(1,3-benzodioxol-5-yl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(3,4-dihydroxyphenyl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-pyrimidin-2-yl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-pyridin-3-ylpyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-nitropyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[5-(trifluoromethyl)pyridin-2-yl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{4-[(benzylcarbamoyl)amino]phenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-{[(4-methylphenyl)sulfonyl]amino}phenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrofuro[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-1-methyl-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, 6,7-Dihydro-4H-thieno[3,2-c]pyridine-2,5-dicarboxylic acid 2-[(2-amino-phenyl)-amide]5-[(2-difluoromethoxy-phenyl)-amide], N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -butyl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-thiophen-2-ylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydrothieno[3,2-c]-pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydrothieno[3,2-c]pyridine-5(4H)carboxylate, N 2 -(2-aminophenyl)-1-methyl-N 5 -pyridin-3-yl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-2,5-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-2,5-dicarboxamide, 2-(difluoromethoxy)phenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate, N 2 -(2-aminophenyl)-N 6 -pyridin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(2-methoxyethyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -[2-(difluoromethoxy)phenyl]-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -pyridin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -[3-(difluoromethoxy)phenyl]-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -(4-fluorophenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -(3,4-dimethoxyphenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-4,7-dihydrothieno[2,3-c]pyridine-6(5H)carboxylate, 3,4-dimethoxyphenyl 2-[(2-amino-5-isopropylphenyl)carbamoyl]-4,7-dihydrothieno[2,3-c]pyridine-6(5H)-carboxylate, N-(2-aminophenyl)-6-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-6-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-1-methyl-N 6 -pyridin-3-yl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(2-methoxyethyl)-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -pyridin-3-yl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-6-carboxylate, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-6-carboxylate, N-(2-aminophenyl)-5-(N-1,3-benzodioxol-5-ylglycyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(3-methoxyphenyl)glycyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(6-methoxypyridin-3-yl)glycyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-morpholin-4-ylphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(methylthio)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(methylthio)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1H-indazol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 ,N 5 -diethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(methylsulfonyl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(methylsulfonyl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N 5 -1,3-benzodioxol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-cyanophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-cyanophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N-(2-aminophenyl)-5-[4-(trifluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[4-(difluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(trifluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-pyridin-3-ylprop-2-enoyl]-4,5,6,7 tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, 3-methoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 3,4-dimethoxyphenyl 2-{[2-amino-5-(3-thienyl)phenyl]carbamoyl}-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 3,4-dimethoxyphenyl 2-{[2-amino-5-(2-thienyl)phenyl]carbamoyl}-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, N-(2-aminophenyl)-5-[{[3-(difluoromethoxy)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo{[3-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo{[2-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[2-(difluoromethoxy)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo{[2-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(2-thienyl)phenyl]-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(3-thienyl)phenyl]-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-fluorophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide-4-methylaniline (1:2), N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide-4-methylaniline (1:2), N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide-4-methylaniline (1:1), benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate-4-methylaniline (1:1), N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide methanesulfonate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate methanesulfonate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate sulfate, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide sulphate, N 2 -(2-aminophenyl)-N-5-pyridin-3-yl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-2,5-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N6-pyridin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N6-(pyridin-3-ylmethyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N6-pyridin-4-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N6-quinolin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N6-(pyridin-3-ylmethyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N6-pyridin-4-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N6-quinolin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide or salts of these compounds.

Another embodiment of the compounds according to the present invention relates to compounds of formula I selected from:

N 2 -(2-aminophenyl)-N 5 -biphenyl-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -benzyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, Methyl 4-[({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)amino]benzoate, N 2 -(2-aminophenyl)-N 5 -(4-phenoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[2-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -quinolin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-methylphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(pyridin-3-ylmethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -ethyl-N 5 -isopropyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(dimethylamino)phenyl]-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -methyl-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -ethyl-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1,3-benzodioxol-5-yl-N 5 -methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(4-methylpiperazin-1-yl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-morpholin-4-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-azetidin-1-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[6-(dimethylamino)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -butyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-pyridin-3-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -piperidin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-pyridin-4-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N 5 -(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-pyrrolidin-1-ylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N-(2-aminophenyl)-5-[{[4-(dimethylamino)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-4-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]-thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(isoquinolin-5-ylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-3-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-methoxypyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(dimethylamino)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo {[4-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-morpholin-4-ylpyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(1,3-benzodioxol-5-ylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methylphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(5-methylpyridin-2-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[oxo(quinolin-3-ylamino)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(4-methylpiperazin-1-yl)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(pyridin-3-ylmethyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylcarbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methylbenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 4-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)benzoate, N-(2-aminophenyl)-5-[4-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, 5-Acetyl-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methoxybenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(quinolin-3-ylcarbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(6-methylpyridin-3-yl)carbonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-({[4-(dimethylamino)phenyl]amino}carbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(piperidin-4-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-pyridin-3-ylcyclohexyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(isoquinolin-5-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(imino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[[(4-methoxyphenyl)amino](methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(cyanoimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(3,4-dimethoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(2-methylphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino) {[4-(dimethylamino)phenyl]amino}methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino)(pentylamino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(cyanoimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(cyanoamino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{(cyanoamino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{(cyanoamino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{N-[4-(dimethylamino)phenyl]ethanimidoyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-(butylamino)-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(3,4-dimethoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(1-methylethyl)phenyl]-5-{1-[(4-methoxyphenyl)amino]-2-nitroethenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-fluorophenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(benzylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 5-[(4-acetamidophenyl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-thienylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 3-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}sulfonyl)thiophene-2-carboxylate, 5-[(2-acetamido-4-methyl-1,3-thiazol-5-yl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-fluorophenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(isopropylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7 N-(2-aminophenyl)-5-(phenoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(2-naphthyloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(biphenyl-4-yloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Biphenyl-4-yl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 4-Methylphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-Methoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-(Propoxycarbonyl)phenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 2-Naphthyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 3,4-Dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, Butyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Pyridin-3-ylmethyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, N-(2-aminophenyl)-5-[3-(1,3-benzodioxol-5-yl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(3,4-dihydroxyphenyl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-pyrimidin-2-yl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-pyridin-3-ylpyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-nitropyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[5-(trifluoromethyl)pyridin-2-yl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{4-[(benzylcarbamoyl)amino]phenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-{[(4-methylphenyl)sulfonyl]amino}phenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrofuro[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-1-methyl-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, 6,7-Dihydro-4H-thieno[3,2-c]pyridine-2,5-dicarboxylic acid 2-[(2-amino-phenyl)-amide]5-[(2-difluoromethoxy-phenyl)-amide], N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -butyl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-thiophen-2-ylphenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydrothieno[3,2-c]-pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(2-methoxyethyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydrothieno[3,2-c]pyridine-5(4H)carboxylate, N 2 -(2-aminophenyl)-1-methyl-N 5 -pyridin-3-yl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-2,5-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3,4-dimethoxyphenyl)-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-2,5-dicarboxamide, 2-(difluoromethoxy)phenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate, N 2 -(2-aminophenyl)-N 6 -pyridin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(2-methoxyethyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -[2-(difluoromethoxy)phenyl]-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -pyridin-3-yl-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -[3-(difluoromethoxy)phenyl]-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -(4-fluorophenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N 6 -(3,4-dimethoxyphenyl)-4,7-dihydrothieno[2,3-c]pyridine-2,6(5H)-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-4,7-dihydrothieno[2,3-c]pyridine-6(5H)carboxylate, 3,4-dimethoxyphenyl 2-[(2-amino-5-isopropylphenyl)carbamoyl]-4,7-dihydrothieno[2,3-c]pyridine-6(5H)-carboxylate, N-(2-aminophenyl)-6-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-6-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-1-methyl-N 6 -pyridin-3-yl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(2-methoxyethyl)-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -pyridin-3-yl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, N 2 -(2-aminophenyl)-N 6 -(3,4-dimethoxyphenyl)-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-2,6-dicarboxamide, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1-methyl-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-6-carboxylate, 3,4-dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-1,4,5,7-tetrahydro-6H-pyrrolo[2,3-c]pyridine-6-carboxylate, N-(2-aminophenyl)-5-(N-1,3-benzodioxol-5-ylglycyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(3-methoxyphenyl)glycyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(6-methoxypyridin-3-yl)glycyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-morpholin-4-ylphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(methylthio)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(methylthio)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -1H-indazol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)dicarboxamide, N 2 -(2-aminophenyl)-N 5 ,N 5 -diethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-chlorophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[4-(methylsulfonyl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -[3-(methylsulfonyl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N 5 -1,3-benzodioxol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-fluorophenyl)-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N 5 -[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(4-cyanophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N 5 -(3-cyanophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N-(2-aminophenyl)-5-[4-(trifluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[4-(difluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(trifluoromethoxy)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-pyridin-3-ylprop-2-enoyl]-4,5,6,7 tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, 3-methoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 3,4-dimethoxyphenyl 2-{[2-amino-5-(3-thienyl)phenyl]carbamoyl}-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 3,4-dimethoxyphenyl 2-{([2-amino-5-(2-thienyl)phenyl]carbamoyl}-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, N-(2-aminophenyl)-5-[{[3-(difluoromethoxy)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo {[3-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo {[2-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[2-(difluoromethoxy)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo{[2-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(2-thienyl)phenyl]-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(3-thienyl)phenyl]-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-fluorophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N 2 -(2-aminophenyl)-N 5 -(6-methoxypyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide-4-methylaniline (1:2), N 2 -(2-aminophenyl)-N 5 -pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide-4-methylaniline (1:2), N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide-4-methylaniline (1:1), benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate-4-methylaniline (1:1), N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide methanesulfonate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate methanesulfonate, benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate sulfate, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide sulphate or salts of these compounds.

Another embodiment of the compounds according to the present invention relates to compounds of formula I selected from:

N 2 -(2-aminophenyl)-N5-biphenyl-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-benzyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, Methyl 4-[({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)amino]benzoate, N 2 -(2-aminophenyl)-N5-(4-phenoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-1,3-benzodioxol-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[2-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[4-(trifluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[2-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[4-(difluoromethoxy)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-quinolin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(4-methylphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(pyridin-3-ylmethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-pyridin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(2-methoxyethyl)-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-ethyl-N5-isopropyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[4-(dimethylamino)phenyl]-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[3-(dimethylamino)phenyl]-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(3,4-dimethoxyphenyl)-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(3,4-dimethoxyphenyl)-N5-ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(3,4-dimethoxyphenyl)-N5-(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-methyl-N5-pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-ethyl-N5-pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-1,3-benzodioxol-5-yl-N5-ethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-1,3-benzodioxol-5-yl-N5-(2-methoxyethyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-1,3-benzodioxol-5-yl-N5-methyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[3-(4-methylpiperazin-1-yl)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(2-methoxyethyl)-N5-pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(6-morpholin-4-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(6-azetidin-1-ylpyridin-3-yl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[6-(dimethylamino)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-butyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(4-pyridin-3-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-piperidin-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(4-pyridin-4-ylcyclohexyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N5-isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-methoxyphenyl)-N5-(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-pyrrolidin-1-ylphenyl)-N5-(4-methoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(3-thienyl)phenyl]-N5-[4-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-isopropylphenyl)-N5-pyridin-3-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(dimethylamino)phenyl]-N5-(3,4-dimethoxyphenyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-isoquinolin-5-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-[3-(dimethylamino)phenyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide dihydrochloride, N-(2-aminophenyl)-5-[{[4-(dimethylamino)phenyl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-4-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]-thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(isoquinolin-5-ylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(4-pyridin-3-ylcyclohexyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-methoxypyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(dimethylamino)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(oxo {[4-(trifluoromethoxy)phenyl]amino}acetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(6-morpholin-4-ylpyridin-3-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(1,3-benzodioxol-5-ylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-methylphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(5-methylpyridin-2-yl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[oxo(quinolin-3-ylamino)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(3,4-dimethoxyphenyl)amino](oxo)acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(butylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[{[6-(4-methylpiperazin-1-yl)pyridin-3-yl]amino}(oxo)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{oxo[(pyridin-3-ylmethyl)amino]acetyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylcarbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methylbenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 4-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)yl}carbonyl)benzoate, N-(2-aminophenyl)-5-[4-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, 5-Acetyl-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-methoxybenzoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(quinolin-3-yl carbonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthoyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(6-methylpyridin-3-yl)carbonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(dimethylamino)benzoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-({[4-(dimethylamino)phenyl]amino}carbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(piperidin-4-ylamino)carbonothioyl]tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[(4-pyridin-3-ylcyclohexyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(isoquinolin-5-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(butylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(pyridin-3-ylamino)carbonothioyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-(anilinocarbonothioyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{[(4-methoxyphenyl)amino]carbonothioyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{imino[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(imino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[[(4-methoxyphenyl)amino](methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[anilino(cyanoimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(4-methoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(3,4-dimethoxyphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{(cyanoimino)[(2-methylphenyl)amino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino){[4-(dimethylamino)phenyl]amino}methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(cyanoimino)(pentylamino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(benzylamino)(cyano imino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(cyano amino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{(cyano amino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{(cyano amino)[(4-methoxyphenyl)imino]methyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7 tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(4-methoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-(3,4-dimethoxyphenyl)ethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{N-[4-(dimethylamino)phenyl]ethanimidoyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyri dine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[N-phenylethanimidoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-(butylamino)-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{1-[(3,4-dimethoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-methoxyphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-anilino-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-[2-amino-5-(1-methylethyl)phenyl]-5-{1-[(4-methoxyphenyl)amino]-2-nitroethenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[1-{[4-(dimethylamino)phenyl]amino}-2-nitrovinyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-{1-[(4-isopropylphenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-{1-[(4-fluorophenyl)amino]-2-nitrovinyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(benzylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(biphenyl-4-ylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 5-[(4-acetamidophenyl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-naphthylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(2-thienylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 3-({2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)-yl}sulfonyl)thiophene-2-carboxylate, 5-[(2-acetamido-4-methyl-1,3-thiazol-5-yl)sulfonyl]-N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethyl)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-fluorophenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(isopropylsulfonyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(difluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[3-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{[4-(trifluoromethoxy)phenyl]sulfonyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-methoxyphenyl)-5-[(4-methoxyphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(phenoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(2-naphthyloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(biphenyl-4-yloxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(methoxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-amino-5-isopropylphenyl)-5-[(4-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(3-methoxyphenoxy)acetyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, Methyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Biphenyl-4-yl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 4-Methylphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-Methoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 4-(Propoxycarbonyl)phenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, 2-Naphthyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, 3,4-Dimethoxyphenyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, Butyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Benzyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)carboxylate, Pyridin-3-ylmethyl 2-[(2-aminophenyl)carbamoyl]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate, N-(2-aminophenyl)-5-[3-(1,3-benzodioxol-5-yl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[3-(3,4-dihydroxyphenyl)prop-2-enoyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-pyrimidin-2-yl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-pyridin-3-ylpyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-nitropyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[5-(trifluoromethyl)pyridin-2-yl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(5-{[(4-methylphenyl)sulfonyl]amino}pyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-{4-[(benzylcarbamoyl)amino]phenyl}-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-(4-{[(4-methylphenyl)sulfonyl]amino}phenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydrofuro[3,2-c]pyridine-2-carboxamide, N-(2-aminophenyl)-1-methyl-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide, N 2 -(2-aminophenyl)-N5-pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-aminophenyl)-N5-(3,4-dimethoxyphenyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N5-butyl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -[2-amino-5-(2-thienyl)phenyl]-N5-pyridin-3-yl-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, N 2 -(2-amino-5-thiophen-2-ylphenyl)-N5-(4-methoxyphenyl)-6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxamide, or salts of these compounds.

Suitable salts for compounds of formula I according to this invention are acid addition salts or salts with bases. Particular mention may be made of the pharmacologically tolerable inorganic and organic acids and bases customarily used in pharmacy. Those suitable are, on the one hand, water-insoluble and, particularly, water-soluble acid addition salts with acids such as, for example, hydrochloric acid, hydrobromic acid, phosphoric acid, nitric acid, sulphuric acid, acetic acid, citric acid, D-gluconic acid, benzoic acid, 2-(4-hydroxybenzoyl)benzoic acid, butyric acid, sulphosalicylic acid, maleic acid, lauric acid, malic acid, fumaric acid, succinic acid, oxalic acid, tartaric acid, embonic acid, stearic acid, toluenesulphonic acid, methanesulphonic acid or 3-hydroxy-2-naphthoic acid, the acids being employed in salt preparation—depending on whether a mono- or polybasic acid is concerned and depending on which salt is desired—in an equimolar quantitative ratio or one differing therefrom.

On the other hand, salts with bases are—depending on substitution—also suitable. As examples of salts with bases are mentioned the lithium, sodium, potassium, calcium, aluminium, magnesium, titanium, ammonium, meglumine or guanidinium salts, here, too, the bases being employed in salt preparation in an equimolar quantitative ratio or one differing therefrom.

Pharmacologically intolerable salts, which can be obtained, for example, as process products during the preparation of the compounds of formula I according to this invention on an industrial scale, are converted into pharmacologically tolerable salts by processes known to the person skilled in the art.

According to expert's knowledge the compounds of formula I according to this invention as well as their salts may contain, e.g. when isolated in crystalline form, varying amounts of solvents. Included within the scope of the invention are therefore all solvates and in particular all hydrates of the compounds of formula I according to this invention as well as all solvates and in particular all hydrates of the salts of the compounds of formula I according to this invention.

Some of the compounds and salts according to the invention may exist in different crystalline forms (polymorphs), which are within the scope of the invention.

It is to be understood, that the present invention also includes any or all possible combinations and subsets of the embodiments defined above.

Exemplary compounds according to the present invention may include, without being restricted thereto, any compounds of formula I selected from the group consisting of those compounds of formula I disclosed in the following examples as final compounds, as well as the salts thereof.

The compounds according to the invention can be prepared, for example, as described as follows and according to the following specified reaction steps, or, particularly, in a manner as described by way of example in the following examples.

As shown in reaction scheme Ia, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)—, R10 is H and all other symbols have the meanings as defined above can be obtained by reacting in a first step ethyl thioxamate of formula 4 with tert-butyl 3-bromo-4-oxopiperidine-1-carboxylate of formula 3 to yield 5-tert-butyl 2-ethyl 6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate of formula 5 which is then hydrolysed in the presence of lithium hydroxide to provide the corresponding lithium salt of formula 6. The lithium salt of formula 6 is reacted with an ortho phenylene diamine derivative of formula 7 (or alternatively a boc protected ortho phenylene diamine derivative of formula 7), wherein B has the meanings as defined above in the presence of dicyclohexyl carbodiimide and HOBt to provide the compound of formula 8 which is then deprotected to provide the corresponding compound of formula 2. The compound of formula 2 is finally reacted with an appropriate isocyanate of formula A—(CH 2 ) n N═C═O wherein A and n have the meanings as defined above to provide a compound of formula I wherein L is —(CH 2 ) n N(R10)C(═O)—, R10 is H and all other symbols are as defined above.

Alternatively, as shown in reaction scheme Ib, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting 1,1′-carbonyldiimidazole with a suitable amine of formula A—(CH 2 ) n —NH(R10) wherein A, R10 and n is as defined above to obtain the corresponding imidazolylcarbonyl amide of formula 9. The compound of formula 9 is reacted with a compound of formula 2 in the presence of a catalytic amount of 4-dimethylamino pyridine to provide the compound of formula I, wherein L is —(CH 2 ) n N(R10)C(═O)— and all other symbols have the meanings as defined above.

Alternatively, as shown in reaction scheme Ic, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)—, R10 is H and all other symbols have the meanings as defined above can be obtained by reacting a suitable amine of formula A—(CH 2 ) n —NH(R10) wherein A and n are as defined above and R10 is H, with triphosgene under basic conditions followed by reaction with compound of formula 2 to provide the compound of formula I.

Alternatively, as shown in reaction scheme Id, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a suitable amine of formula A—(CH 2 ) n —NH(R10) wherein A, n and R10 have the meanings as defined above with phenylchloroformate or p-nitrophenylchloroformate (R═H or NO 2 ) to provide the corresponding phenyl or p-nitrophenyl carbonate of the amine having formula 11. The compound of formula 11 is then reacted with a compound of formula 2 under microwave conditions or alternatively at 60-100° C. in the presence of a solvent (DMF/DME/DMSO or a mixture thereof in any proportion) to provide the compound of formula I.

Alternatively, as shown in reaction scheme Ie, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a suitable amine of formula A—(CH 2 ) n —NH(R10) wherein A, n and R10 have the meanings as defined above with phenyl chloroformate to provide the compound of formula 12 which is then reacted with ethyl 4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxylate hydrochloride (compound of formula 13) to provide the compound of formula 14. The ester function of the compound of formula 14 is hydrolysed to afford the acid of formula 15 which is reacted with a ortho phenylene diamine derivative of formula 7 (or alternatively a mono boc protected orthophenylene derivative of formula 7), wherein B has the meanings as defined above to yield the compound of formula I.

Alternatively, as shown in reaction scheme I f, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting compound of formula 12 as obtained in Scheme 1 e and compound of formula 2 in the presence of a base to yield the compound of formula I.

As shown in reaction scheme II, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting an amine of formula A—(CH 2 ) n —N(R10)H wherein n, R10 and A have the meanings as defined above with ethyl chlorooxalate to obtain the corresponding compound of formula 16 which on its part is reacted with a compound of formula 2 to obtain the compound of formula I.

As shown in reaction scheme III, compounds of formula I wherein L is —C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 wherein B has the meanings as defined above with an acid of formula A-C(═O)OH or an acid chloride of formula A-C(═O)Cl wherein A has the meanings as defined above to obtain a compound of formula I, wherein L is —C(═O)— and A and B have the meanings as defined above.

As shown in reaction scheme IV, compounds of formula I wherein L is —N(R10)C(═S)—, R10 is H and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a suitable isothiocyanate of formula A-N═C═S wherein A has the meanings as defined above to obtain the desired compound of formula I, wherein L is —N(R10)C(═S)—, R10 is H and A and B have the meanings as defined above.

As shown in scheme Va, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═NR11)-, R11 is hydrogen and all other symbols have the meanings as defined above can be obtained by reacting cyanobromide with an appropriate amine of formula A—(CH 2 ) n —N(R10)H wherein n, R10 and A have the meanings as defined above to afford the cyanamide of formula 17 which on its part is then reacted with a compound of formula 2 to afford the desired compound of formula I.

As shown in scheme Vb, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═NR11)-, R10 is H, R11 is cyano and all other symbols have the meanings as defined above can be obtained by deprotecting 5-tert-butyl 2-ethyl 6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate (compound of formula 5) to obtain the compound of formula 18 which is reacted with an appropriate isothiocyanate of formula A—(CH 2 ) n —N═C═S, wherein A and n have the meanings as defined above to afford the thioamide of formula 19 which is reacted with iodomethane to provide compound of formula 20. The compound of formula 20 is hydrolysed to yield the compound of formula 21. Compound of formula 21 is reacted with a mono boc protected ortho phenylene diamine of formula 7 to obtain compound of formula 22, which is reacted with cyanamide to yield the desired compound of formula I.

As shown in scheme Vc, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═NR11)-, R10 is H, R11 is (C 1 -C 4 )alkyl and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 21 with mono boc protected ortho phenylene diamine of formula 7 to afford compound of formula 23. Compound of formula 23 is reacted with an alkyl amine hydrochloride to provide compound of formula 24 which is then deprotected to obtain the desired compound of formula I.

As shown in scheme VIa, compounds of formula I wherein L is —(CH 2 ) n N═C(R11)-, R11 is (C 1 -C 4 )alkyl and all other symbols have the meanings as defined above can be obtained by boc deprotection of compound of formula 5 to obtain compound of formula 25 which is acylated using acetic anhydride to obtain the acetyl compound of formula 26. Compound of formula 26 is then reacted with a suitable amine of formula A—(CH 2 ) n —NH 2 , wherein A and n have the meanings as defined above to obtain the compound of formula 27, which is then hydrolysed to obtain the compound of formula 28. The compound of formula 28 is finally reacted with mono boc protected ortho phenylene diamine of formula 7 to yield the desired compound of formula I.

Alternatively, as shown in scheme VIb, compounds of formula I wherein L is (CH 2 ) n N(R10)C(═CR11), R11 is nitro and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with trichloro nitro ethane to obtain a compound of formula 29 which is reacted with a suitable amine of formula A—(CH 2 ) n —N(R10)H wherein A, n and R10 have the meanings as defined above to yield the desired compound of formula I.

As shown in reaction scheme VII, compounds of formula I wherein L is —(CH 2 ) n S(O) 2 — and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a suitable sulfonyl chloride of formula A—(CH 2 ) n —S(O) 2 Cl, wherein A and n have the meanings as defined above to obtain the desired compound of formula I.

As shown in reaction scheme VIII a, compounds of formula I wherein L is —OCH 2 C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a suitable oxy acetic acid of formula A-O—CH 2 —C(═O)OH wherein A has the meanings as defined above to obtain the desired compound of formula I.

As shown in reaction scheme VIII b, compounds of formula I wherein L is —OCH 2 C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a suitable oxy acetyl chloride of formula A-O—CH 2 —C(═O)Cl, wherein A has the meanings as defined above to obtain the desired compound of formula I.

As shown in reaction scheme IX a, compounds of formula I wherein L is —(CH 2 ) n OC(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a mixture of 1,1′-carbonyldiimidazole and a suitable alcohol of formula A-(CH 2 ) n —OH, wherein A and n have the meanings as defined above.

Alternatively, as shown in reaction scheme IX b, compounds of formula I wherein L is —(CH 2 ) n OC(═O)—, A is alkyl and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a suitable alkyl chloroformate of formula A—(CH 2 ) n —OC(═O)Cl, wherein A is alkyl and n has the meanings as defined above.

As shown in reaction scheme X, compounds of formula I wherein L is —C═C—C(═O)— and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with an acrylic acid of formula A-CH═CH—C(O)OH wherein A has the meanings as defined above to yield the desired compound of formula I.

As shown in reaction scheme XI, compounds of formula I wherein L is a bond and all other symbols have the meanings as defined above can be obtained by reacting a compound of formula 2 with a compound of formula A-X, wherein A has the meanings as defined above and X is a suitable leaving group, such as for example a halogen atom, preferably a chlorine atom to yield the desired compound of formula I.

As shown in reaction scheme XII, compounds of formula I wherein L is —(CH 2 ) n S(O) 2 — and all other symbols have the meanings as defined above can be obtained by reacting piperidon hydrochloride with an appropriate sulfonyl chloride of formula A—(CH 2 ) n —S(O) 2 Cl wherein A and n have the meanings as defined above to obtain a compound of formula 30 which is then converted to the aldehyde of formula 31 under Vilsmeier Hack conditions. The compound of formula 31 is then reacted with ethyl thioglycolate to afford the compound of formula 32, which is then hydrolysed to obtain the compound of formula 33. The compound of formula 33 is reacted with the mono boc protected ortho phenylene diamine of formula 7 to yield the desired compound of formula I.

As shown in reaction scheme XIII, compounds of formula I wherein L is —(CH 2 ) n S(O) 2 — and all other symbols have the meanings as defined above can be obtained by reacting the aldehyde of formula 31 with ethyl glycolate to afford the compound of formula 34 which is hydrolysed to obtain the compound of formula 35. The compound of formula 35 is reacted with mono boc protected ortho phenylene diamine of formula 7 to yield the desired compound of formula I.

As shown in reaction scheme XIV, compounds of formula I wherein L is —(CH 2 ) n S(O) 2 — and all other symbols have the meanings as defined above can be obtained by reacting the aldehyde of formula 31 with sarcosine hydrochloride to afford the compound of formula 36 which is hydrolysed to yield the compound of formula 37. The compound of formula 37 is reacted with mono boc protected ortho phenylene diamine of formula 7 to yield the desired compound of formula I.

As shown in reaction scheme XV, compounds of formula I wherein L is —(CH 2 ) n N(R10)C(═O)—, R10 is hydrogen and all other symbols have the meanings as defined above can be obtained by converting piperidon hydrochloride to its carbamate derivative of formula 38, which on its part is formylated under Vilsmeier Hack conditions to yield the chloro aldehyde of formula 39. The chloro aldehyde of formula 39 is reacted with ethyl thioglycolate to afford the compound of formula 40 which is hydrolysed to obtain compound of formula 41 which then is esterified to obtain the tetrahydro thieno pyridine of formula 42. The amino function of the compound of formula 42 is then boc protected to afford the compound of formula 43 and the ester function is hydrolysed to yield the compound of formula 44 The compound of formula 44 is then reacted with mono boc protected ortho phenylene diamine of formula 7 to obtain the diamine of formula 45. The compound of formula 45 is then finally reacted with a compound of formula A—(CH 2 ) n N(R10)C(═O)OPh or alternatively a compound of formula A—(CH 2 ) n —N═C═O to yield the desired compound of formula I.

As shown in reaction scheme XVI, compounds of formula I wherein L is —(CH 2 ) n NR10C(O)—, R10 is hydrogen and all other symbols are as defined above can be obtained by converting thiopene 3-carbaldehyde to its α-β unsaturated nitro derivative which is hydrogenated followed by cyclisation to yield the boc protected tetrahydro thienopyridine compound of formula 46. The cyclised compound of formula 47 is reacted with ethyl chloro formate and butyl lithium to afford the compound of formula 48 which is further hydrolysed to obtain compound of formula 49. The compound of formula 49 is then reacted with mono boc protected ortho phenylene diamine 7 to obtain the diamine of formula III. The compound of formula III is then reacted with A—(CH 2 ) n NR10C(═O)OPh to yield the desired compound of formula I.

As shown in reaction scheme XVII, compounds of formula I wherein L is —(CH 2 ) n NR10C(O)—, R10 is hydrogen and all other symbols are as defined above can be obtained by converting 4-methyl-3-nitro pyridine to its keto ester of formula 50 which on catalytic hydrogenation gave compound of formula 51. Compound of formula 51 is boc protected to obtain compound of formula 52 followed by reduction in the presence of benzyl bromide to yield the compound of formula 53. Compound of formula 53 is further debenzylate and again protected with boc anhydride to yield the compound of formula 55. Compound of formula 55 is treated with methyl iodide to get its N-methyl derivative 56, which on hydrolysis provided compound of formula 57. The compound of formula 57 is then reacted with mono boc protected ortho phenylene diamine 7 to obtain the diamine of formula IV. The compound of formula IV is then reacted with A—(CH 2 ) n NR10C(═O)OPh to yield the desired compound of formula I.

As shown in reaction scheme XVIII, compounds of formula I wherein L is —N(R10)CH 2 C(═O)—, R10 is H and all other symbols have the meanings as defined above can be obtained by reacting A-NH 2 , wherein A is as defined above with bromoacetyl bromide to afford a compound of formula 58 which is then hydrolysed to get respective acid of formula 59. Acid of formula 59 is then reacted with compound 2 to get the desired compound of formula I, wherein L is —N(R10)CH 2 C(═O)—, R10 is H and A and B have the meanings as defined above.

As shown in reaction scheme XIX, compounds of formula I wherein L is —(CH 2 ) n NR10C(O)—, R10 is hydrogen and all other symbols are as defined above can be obtained by reacting N-boc piperidone with bromo ethyl pyruvate in presence of base to affors compound of formula 60 which is then alkylated using methyl iodide to yield N-methylated compound of formula 61. Ester of formula 61 is hydrolysed to get corresponding acid 62, which is then reacted, with mono boc protected ortho phenylene diamine 7 to obtain the boc protected diamine of formula 63. Compound of formula 63 is deprotected to get free amine of formula 64. The compound of formula 64 is then reacted with A—(CH 2 ) n NR10C(═O)OPh to yield the desired compound of formula I.

As shown in reaction scheme XX, compounds of formula I wherein L is —O(CH 2 )—C(O)— and all other symbols are as defined above can be obtained by reacting compound of formula 64 as shown in scheme-XIX with A—O(CH 2 )—C(═O)OPh-NO2 to afford desired compound of formula I.

As shown in reaction scheme XXI, compounds of formula I wherein L is —O(CH 2 )—C(O)— and all other symbols are as defined above can be obtained by reacting compound of formula 45 as shown in scheme-XV with A—O(CH 2 ) n C(═O)OPh-NO2 to afford desired compound of formula I.

As shown in scheme XXII, compound of formula I wherein L is —O(CH 2 ) n C(O)— and all other symbols are as defined above can be obtained by reacting compound of formula IV obtained in scheme-XVII with A—O(CH 2 ) n C(═O)OPh-NO2 to afford desired compound of formula I.

As shown in scheme XXIII, compound of formula I wherein L is —O(CH 2 ) n C(O)— and all other symbols are as defined above can be obtained by reacting compound of formula III obtained in scheme-XVI with A—O(CH 2 ) n C(═O)OPh-NO2 to afford desired compound of formula I.

As shown in reaction scheme XXIV, compounds of formula I wherein L is —(CH 2 ) n NR10C(O)—, R10 is hydrogen and all other symbols are as defined above can be obtained by hydrolyzing compound of formula 60 obtained in reaction scheme XIX in presence of aqueous sodium hydroxide in ethanol to yield compound of formula 65. Compound of formula 65 which is then reacted, with mono boc protected ortho phenylene diamine 7 to obtain the boc protected diamine of formula 66. Compound of formula 66 is deprotected to get free amine of formula 67. The compound of formula 67 is then reacted with A-(CH 2 ) n NR10C(═O)OPh to yield the desired compound of formula I.

The methods mentioned above can be expediently carried out analogously to the methods known to the person skilled in the art or as described by way of example in the following examples.

Optionally, compounds of the formula I can be converted into their salts, or, optionally, salts of the compounds of the formula I can be converted into the free compounds. Corresponding processes are habitual per se to the skilled person.

It is moreover known to the person skilled in the art that if there are a number of reactive centers on a starting or intermediate compound it may be necessary to block one or more reactive centers temporarily by protective groups in order to allow a reaction to proceed specifically at the desired reaction center. A detailed description for the use of a large number of proven protective groups is found, for example, in “Protective Groups in Organic Synthesis” by T. Greene and P. Wuts (John Wiley & Sons, Inc. 1999, 3rd Ed.) or in “Protecting Groups (Thieme Foundations Organic Chemistry Series N Group” by P. Kocienski (Thieme Medical Publishers, 2000).

The compounds according to the invention are isolated and purified in a manner known per se, for example by distilling off the solvent under reduced pressure and recrystallizing the residue obtained from a suitable solvent or subjecting it to one of the customary purification methods, such as, for example, column chromatography on a suitable support material.

Salts can be obtained by dissolving the free compound in a suitable solvent (e.g. a ketone, such as acetone, methyl ethyl ketone or methyl isobutyl ketone, an ether, such as diethyl ether, tetrahydrofuran or dioxane, a chlorinated hydrocarbon, such as methylene chloride or chloroform, or a low-molecular-weight aliphatic alcohol, such as ethanol or isopropanol) which contains the desired acid or base, or to which the desired acid or base is then added. The salts can be obtained by filtering, reprecipitating, precipitating with a nonsolvent for the addition salt or by evaporating the solvent. Salts obtained can be converted into the free compounds, which can in turn be converted into salts, by alkalization or by acidification. In this manner, pharmacologically unacceptable salts can be converted into pharmacologically acceptable salts.

Suitably, the conversions mentioned in this invention can be carried out analogously or similarly to methods which are familiar per se to the person skilled in the art.

The person skilled in the art knows on the basis of his/her knowledge and on the basis of those synthesis routes, which are shown and described within the description of this invention, how to find other possible synthesis routes for compounds according to this invention. All these other possible synthesis routes are also part of this invention.

Having described the invention in detail, the scope of the present invention is not limited only to those described characteristics or embodiments. As will be apparent to persons skilled in the art, modifications, analogies, variations, derivations, homologisations and adaptations to the described invention can be made on the base of art-known knowledge and/or, particularly, on the base of the disclosure (e.g. the explicite, implicite or inherent disclosure) of the present invention without departing from the spirit and scope of this invention as defined by the scope of the appended claims.

The following examples serve to illustrate the invention further without restricting it. Likewise, further compounds according to this invention, whose preparation is not explicitly described, can be prepared in an analogous or similar manner or in a manner familiar per se to the person skilled in the art using customary process techniques.

Any or all of the compounds of formula I according to the present invention which are specified as final compounds in the following examples, as well as the salts thereof, are a particularly interesting subject of the present invention.

In the examples, mp/M.P. stands for melting point, h for hour(s), min for minutes, conc. for concentrated, calc. for calculated, fnd.for found, EDCI for N-(3-Dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, HOBT for 1-Hydroxybenzotriazole hydrate, DCC for N,N′-Dicyclohexylcarbodiimide, TEA for triethyl amine, DMF for N,N-Dimethylformamide, DMAP for 4-(Dimethylamino) pyridine, Boc anhydride/boc/(BOC) 2 O for di-tert-butyl dicarbonate, DCM for dichoromethane, tBuOK for potassium tert.butoxide, DMSO for dimethyl sulfoxide, NaOH for sodium hydroxide, THF for tetrahydrofuran, PTSA for 4-methyl benzene sulfonic acid, and all other abbreviations have their meanings customary per se to the skilled person.

Preparation 1

tert-Butyl 2-amino-4-methoxyphenylcarbamate

To a solution of NaH (2.2 eq) in tetrahydrofuran, HMDS (2.2 eq) was added at 0° C. and the reaction mixture was stirred for 15 Min. Then, 4-methoxy-2-nitroaniline (1.0 eq) in tetrahydrofuran was added at 0° C., continued the reaction at room temperature for Sirs. Then, (Boc) 2 O (1.0 eq.) was added, stirred the reaction at room temp overnight. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 4-methoxy-2-nitrophenylcarbamate. (Yield=63%)

tert-Butyl 4-methoxy-2-nitrophenylcarbamate as obtained in step I (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-methoxyphenylcarbamate. (Yield=83%)

1 H NMR (DMSO-D6) δ (ppm) 1.38 (s, 9H), 3.64 (s, 3H), 4.82 (s, 2H), 6.11 (dd, 1H, J=6.3 & 2.7 Hz), 6.97 (d, 1H, J=2.7 Hz) 8.11 (s, 1H).

Preparation 2

tert-Butyl 2-amino-4-isopropylphenylcarbamate

To a solution of 4-isopropylaniline (1.0 eq) in dichloromethane at 0° C., triethylamine (2.2 eq) was added and stirred for 15 min. Then, acetic anhydride (1.0 eq) in dichloromethane was added at 0° C., after addition the reaction was continued at room temperature for 5 hrs. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 , concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired N-(4-isopropylphenyl)acetamide. (Yield=95%)

N-(4-Isopropylphenyl)acetamide obtained in step I above was nitrated using nitric acid (1.2 eq)+H 2 SO 4 (1.0 eq) at 0 to 5° C. for 2 hrs. After the completion of the reaction, reaction mixture was added to ice and pH was adjusted to 8, extracted with dichloromethane, which was evaporated to dryness to obtain N-(4-isopropyl-2-nitrophenyl)acetamide.

To a solution of N-(4-isopropyl-2-nitrophenyl)acetamide obtained in step II above (1.0 eq) in MeOH and water was added KOH (1.5 eq) at room temperature and stirred for 5 hrs. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired 4-isopropyl-2-nitroaniline. (Yield=65%).

To a solution of NaH (2.2 eq) in tetrahydrofuran, HMDS (2.2 eq) was added at 0° C. and the reaction mixture was stirred for 15 min. Then, 4-isopropyl-2-nitroaniline (1.0 eq) in tetrahydrofuran was added at 0° C., continued the reaction at room temperature for 5 hrs. Then, (Boc) 2 O (1.0 eq.) was added, stirred the reaction at room temp overnight. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 4-isopropyl-2-nitrophenylcarbamate. (Yield=70%)

tert-Butyl 4-isopropyl-2-nitrophenylcarbamate as obtained in step IV (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-isopropylphenylcarbamate. (Yield=80%)

1 H NMR (DMSO-D6) δ (ppm) 1.15 (d, 6H, J=6.9 Hz), 1.45 (s, 9H), 2.71 (m, 1H), 4.82 (s, 2H), 6.42 (d, 1H, J=8.1 Hz), 6.65 (s, 1H), 7.05 (d, 1H, J=8.1 Hz), 8.21 (s, 1H).

Preparation 3

tert-Butyl 4-(dimethylamino)-2-nitrophenylcarbamate

To a solution of N,N-dimethylbenzene-1,4-diamine (1.0 eq) in dichloromethane, triethylamine (2.2 eq) was added at 0° C. and stirred for 15 min. To the above mixture was then added a solution of acetic anhydride (1.0 eq) in dichloromethane at 0° C., after addition the reaction was continued at room temperature for 5 hrs. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 , concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired N-[4-(dimethylamino)phenyl]acetamide. (Yield=69%)

N-[4-(dimethylamino)phenyl]acetamide obtained in step I above was nitrated using nitric acid (1.2 eq)+H 2 SO 4 (1.0 eq) at 0 to 5° C. for 2 hrs. After the completion of the reaction, reaction mixture was added to ice and pH was adjusted to 8, extracted with dichloromethane, which was evaporated to dryness to obtain N-[4-(dimethylamino)-2-nitrophenyl]acetamide.

To a solution of N-[4-(dimethylamino)-2-nitrophenyl]acetamide obtained in step 11 above (1.0 eq) in MeOH and water was added KOH (1.5 eq) at room temperature and stirred for 5 hrs. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired N-(4-amino-3-nitrophenyl)-N,N-dimethylamine. (Yield=65%).

To a solution of NaH (2.2 eq) in tetrahydrofuran, HMDS (2.2 eq) was added at 0° C. and the reaction mixture was stirred for 15 min. Then, N-(4-amino-3-nitrophenyl)-N,N-dimethylamine (1.0 eq) in tetrahydrofuran was added at 0° C., continued the reaction at room temperature for 5 hrs. Then, (Boc) 2 O (1.0 eq.) was added, stirred the reaction at room temp overnight. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 4-(dimethylamino)-2-nitrophenylcarbamate. (Yield=67%)

tert-Butyl 4-(dimethylamino)-2-nitrophenylcarbamate as obtained in step IV (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-(dimethylamino)phenylcarbamate. (Yield=90%)

1 H NMR (DMSO-D6) δ (ppm) 1.40 (s, 9H), 2.78 (s, 6H), 4.60 (s, 2H), 5.96 (dd, 1H, J=6.3 & 2.7 Hz), 6.0 (d, 1H, J=2.7 Hz), 6.86 (d, 1H, J=3.0 HZ), 8.01 (s, 1H).

Preparation 4

tert-Butyl 2-amino-4-thien-2-ylphenylcarbamate

To a solution of 4-bromoaniline (1.0 eq) in dichloromethane, triethylamine (2.2 eq) was added at 0° C. and stirred for 15 min. To this mixture was added acetic anhydride (1.0 eq) in dichloromethane at 0° C., after addition the reaction was continued at room temperature for 5 hrs. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 , concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired N-(4-bromophenyl)acetamide. (Yield=65%)

N-(4-Bromophenyl)acetamide obtained in step I above was nitrated using nitric acid (1.2 eq)+H 2 SO 4 (1.0 eq) at 0 to 5° C. for 2 hrs. After the completion of the reaction, reaction mixture was added to ice and pH was adjusted to 8, extracted with dichloromethane, which was evaporated to dryness to obtain N-(4-bromo-2-nitrophenyl)acetamide. (Yield=95%)

To a solution of N-(4-bromo-2-nitrophenyl)acetamide obtained in step H above (1.0 eq) in MeOH and water was added KOH (1.5 eq) at room temperature and stirred for 5 hrs. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired 4-bromo-2-nitroaniline. (Yield=95%)

To a solution of NaH (2.2 eq) in tetrahydrofuran, HMDS (2.2 eq) was added at 0° C. and the reaction mixture was stirred for 15 min. Then, 4-bromo-2-nitroaniline (1.0 eq) in tetrahydrofuran was added at 0° C., continued the reaction at room temperature for 5 hrs. Then, (Boc) 2 O (1.0 eq.) was added, stirred the reaction at room temp overnight. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 4-bromo-2-nitrophenylcarbamate. (Yield=72%)

1 H NMR (DMSO-d 6 ) δ (ppm) 1.42 (s, 9H), 7.57 (d, 1H, J=8.7 Hz), 7.85 (dd, 1H, J=8.7 & 2.4 Hz), 8.11 (d, 1H, J=2.4 Hz), 9.67 (s, 1H).

To a solution of tert-butyl 4-bromo-2-nitrophenylcarbamate obtained in step IV above (1.0 eq) in toluene, was added 10 mol % of tetrakis Pd, heated to 90° C. for 30 min, then aq K 2 CO 3 and ethanol were added, followed by addition of 2-thienyl boronic acid portionwise and then reaction was refluxed overnight. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 2-nitro-4-thien-2-ylphenylcarbamate. (Yield=88%)

1 H NMR (DMSO-d 6 ) δ (ppm); 1.44 (s, 9H), 7.16 (dd, 1H, J=3.6 & 1.5 Hz), 7.61 (m, 2H), 7.67 (d, 1H, J=8.7 Hz), 7.93 (dd, 1H, J=8.7 & 2.1 Hz), 8.13 (d, 1H, J=2.4 Hz), 9.64 (s, 1H).

To a solution of tert-butyl 2-nitro-4-thien-2-ylphenylcarbamate as obtained in step V above (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-thien-2-ylphenylcarbamate (Yield=95%).

1 H NMR (DMSO-d 6 ) δ (ppm); 1.45 (s, 9H), 5.00 (s, 2H), 6.83 (dd, 1H, J=8.1 & 1.8 Hz), 6.97 (d, 1H, J=2.1 Hz), 7.07 (dd, 1H, J=3.6 & 1.5 Hz), 7.27 (m, 2H), 7.42 (dd, 1H, J=4.2 & 0.9 Hz), 8.34 (s, 1H).

Preparation 5

tert-Butyl 2-amino-4-thien-3-ylphenylcarbamate

To a solution of tert-butyl 4-bromo-2-nitrophenylcarbamate obtained in step IV preparation 4 above (1.0 eq) in toluene, was added 10 mol % of tetrakis Pd, heated to 90° C. for 30 min, then aq K 2 CO 3 and ethanol were added, followed by addition of 3-thienyl boronic acid portionwise and then reaction was refluxed overnight. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 2-nitro-4-thien-3-ylphenylcarbamate. (Yield=88%)

1 H NMR (DMSO-d 6 ) δ (ppm); 1.44 (s, 9H), 7.64 (m, 3H), 8.02 (m, 2H), 8.23 (d, 1H, J=2.1 Hz), 9.61 (s, 1H).

To a solution of tert-butyl 2-nitro-4-thien-2-ylphenylcarbamate as obtained in step I above (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-thien-2-ylphenylcarbamate (Yield=95%).

1 H NMR (DMSO-d 6 ) δ (ppm); 1.44 (s, 9H), 4.89 (s, 2H), 6.86 (dd, 1H, J=8.1 & 2.1 Hz), 7.00 (d, 1H, J=2.1 Hz), 7.23 (d, 1H, J=8.1 Hz), 7.37 (dd, 1H, J=4.8 & 1.2 Hz), 7.57 (m, 2H), 8.30 (s, 1H).

Preparation 6

tert-Butyl 2-amino-4-pyrrolidin-1-ylphenylcarbamate

To a solution of 4-fluoronitrobenzene (1.0 eq.) in isopropyl alcohol, pyrrolidine (2.2 eq) and triethylamine (11.0 eq) were added and reaction mixture was refluxed overnight. Reaction mixture was cooled to room temperature, product obtained was collected by filtration and dried to get the desired 1-(4-nitrophenyl)pyrrolidine. (Yield=85%)

To a solution of 1-(4-nitrophenyl)pyrrolidine as obtained in step I above (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired 4-pyrrolidin-1-ylaniline. (Yield=78%)

To a solution of 4-pyrrolidin-1-ylaniline as obtained in step II above (1.0 eq) in dichloromethane, triethylamine (2.2 eq) was added at 0° C. and stirred for 15 min. To this mixture was added acetic anhydride (1.0 eq) in dichloromethane at 0° C., after addition the reaction was continued at room temperature for 5 hrs. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 , concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired N-(4-pyrrolidin-1-ylphenyl)acetamide. (Yield=90%)

N-(4-Pyrrolidin-1-ylphenyl)acetamide obtained in step III above was nitrated using nitric acid (1.2 eq)+H 2 SO 4 (1.0 eq) at 0 to 5° C. for 2 hrs. After the completion of the reaction, reaction mixture was added to ice and pH was adjusted to 8, extracted with dichloromethane, which was evaporated to dryness to obtain N-(2-nitro-4-pyrrolidin-1-ylphenyl)acetamide

To a solution of N-(2-nitro-4-pyrrolidin-1-ylphenyl)acetamide obtained in step IV above (1.0 eq) in MeOH and water was added NaOH (1.5 eq) at room temperature and stirred for 5 hrs. Water was added to the reaction mixture and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired 2-nitro-4-pyrrolidin-1-ylaniline. (Yield=85%)

To a solution of NaH (2.2 eq) in tetrahydrofuran, HMDS (2.2 eq) was added at 0° C. and the reaction mixture was stirred for 15 min. Then, 2-nitro-4-pyrrolidin-1-ylaniline (1.0 eq) in tetrahydrofuran was added at 0° C., continued the reaction at room temperature for 5 hrs. Then, (Boc) 2 O (1.0 eq.) was added, stirred the reaction at room temp overnight. Water was added and the organic layer was separated, dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the desired tert-butyl 2-nitro-4-pyrrolidin-1-ylphenylcarbamate. (Yield=65%)

To a solution of tert-butyl 2-nitro-4-pyrrolidin-1-ylphenylcarbamate obtained in step VI above (1.0 eq) in MeOH was hydrogenated using Pd/C under H 2 atmosphere. After completion of the reaction, reaction mixture was filtered through celite and evaporated to dryness to get desired tert-butyl 2-amino-4-pyrrolidin-1-ylphenylcarbamate. (Yield=90%)

1 H NMR (DMSO-D6) δ (ppm); 1.40 (s, 9H), 1.91 (m, 4H), 3.12 (m, 4H), 4.5 (s, 2H), 5.76 (s, 1H), 5.8 (m, 1H), 5.9 (d, 1H, J=2.7 Hz), 7.9 (s, 1H).

N 2 -(2-aminophenyl)-N5-biphenyl-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide

Preparation of Ethyloxamate

Solution of diethyl oxalate (1 mole, 136 ml) in absolute ethanol (100 ml) was cooled to 0° C. 68.1 ml of ammonium hydroxide was added and mixture was stirred for 4 h at 0° C. White precipitate formed was filtered, collected and recrystallised from ethanol. Yield 67.5 gm. M. P. 108-110° C.

NMR: 1 H NMR (CDCl 3 ) δ(ppm) 8.20 (br s, 1H, NH), 7.92 (br s, 1H, NH), 4.20 (q, 211, J=7.2 Hz), 1.23 (t, 2H, J=7.2 Hz).

Preparation of Ethyl Thioxamate

Ethyl oxamate (46.8 gm, 0.4 mole) obtained in step I was dissolved in 400 ml of toluene and heated to 100° C. Phosphorus pentasulphide (88.9 gm, 0.4 mole) was added under stirring and continued further stirring for 2 h. Reaction mixture was cooled to 50° C. and filtered by vacuum filtration. The precipitate was filtered and purified by column chromatography. Yield 20.0 gm. M. P. 58-61° C.

1 H NMR (CDCl 3 ) δ(ppm): −8.28 (br s, 1H, NH), 7.85 (br s, 1H, NH), 4.37 (q, 2H, J=7.2 Hz), 1.41 (t, 2H, J=7.2 Hz).

N-boc 4-piperidone

4-piperidone monohydrate hydrochloride (250 g, 1.62 mole) was dissolved in dioxane (1.5 L) and water (0.5 L). 217 g of NaHCO 3 was added at 0° C. followed by slow addition of (BOC) 2 O (459 g, 2.1 mole). Reaction mixture was stirred for overnight. Solution was concentrated; residue was taken in water and extracted with ethyl acetate, washed with water and dried over anhydrous Na 2 SO 4 . Solvent was evaporated and product obtained was washed with hexane to get N-boc 4-piperidone (280 g).

1 H NMR (CDCl 3 ) δ(ppm) 3.32 (t, 4H, J=6.3 Hz), 2.44 (t, 4H), J=6.3 Hz)

N-boc-3-bromo-4-piperidone

N-boc-4-piperidone (100 gm, 0.5 mole) obtained in step H1 was dissolved in 4.0 L of dichloromethane. Bromine (96.3 gm, 0.6 mole) in 100 ml of dichloromethane was added at room temperature under stirring and nitrogen bubbling. After completion of bromine addition, the reaction mixture was stirred further at room temperature for additional 30 minutes and then filtered. Filtrate was concentrated and crystallized by dichloromethane/petroleum ether to get the product N-boc-3-bromo-4-piperidone (45.0 gm).

NMR: 1 H NMR (CDCl 3 ) δ(ppm) 4.34 (br s, 1H), 3.98 (s, 3H), 3.70 (m, 2H), 3.03 (s, 1H), 1.50 (s, 9H).

5-tert-butyl 2-ethyl 6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate

N-boc-3-bromo-4-piperidone (110 gm, 0.395 mole) obtained in step IV was dissolved in 500 ml of dry toluene. Ethyl thioxamate (68.4 g, 0.514 mole) obtained in step II and PPTS (10 gm, 0.039 mole) were added to toluene solution. Mixture was refluxed azeotropically for 8 h, followed by concentration. The residue obtained was taken in water and extracted with dichloromethane. The organic layer was washed with water, brine and dried over anhydrous sodium sulphate and concentrated. Residue obtained was purified by column chromatography using 1% MeOH/CH 2 Cl 2 as eluent to get the 39.0 gm of N-boc-4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-ethylcarboxylate.

1 H NMR (CDCl 3 ) δ(ppm) 4.72 (s, 2H), 4.47 (q, 2H, 7.2 Hz), 3.74 (m, 2H), 2.97 (t, 2H, J=5.4 Hz), 2.40 (t, 2H, J=6.3 Hz), 1.50 (s, 9H), 1.43 (t, 3H, J=7.2 Hz).

Lithium salt of N-boc-4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-carboxylate

5-tert-butyl 2-ethyl 6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate (39 gm, 0.125 mole) obtained in step V was dissolved in mixture of solvents containing 170 ml THF and 30 ml water. To this solution was added 6.3 gm of LiOH.H 2 O (0.15 mole) and stirred for 4 h Reaction mixture was then concentrated to dryness. Solid mass was taken in ether and stirred for 1 h Ether layer was decanted and residue was dried under vacuum to get Lithium salt of N-boc-4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-carboxylate. 36.0 gm yield.

1 H NMR (DMSO-d 6 ) δ(ppm) 4.54 (s, 2H), 3.63 (t, 2H, J=6.0 Hz), 2.71 (t, 2H, J=5.4 Hz), 141 (s, 9H).

tert-butyl 2-({2-[(tert-butoxycarbonyl)amino]phenyl}carbamoyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate

53.36 gm of DCC (0.26 mole) and 28 gm of HOBt (0.21 mole) were added to the well stirred solution of Lithium salt of N-boc-4,5,6,7-tetrahydrothiazolo-[5,4-c]pyridine-2-carboxylate (50 gm, 0.172 mole) obtained in step VI in 1.5 L of dichloromethane. Mono boc protected o-phenylene diamine (43.0 gm, 0.21 mole) was then added and mixture was stirred for overnight. The reaction mixture was washed with water, cold-dil HCl(5%), brine, dried over anhydrous Na 2 SO 4 and then concentrated. Crude mass (100.0 gm) obtained was purified by column chromatography using 18% ethyl acetate/petroleum ether as eluent to yield 22.0 gm of tert-butyl 2-({2-[(tert-butoxycarbonyl)amino]phenyl}carbamoyl)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate. M.P.: 188° C.

1 H NMR (DMSO-d 6 ) δ(ppm) 10.07 (s, 1H), 9.16 (s, 1H), 7.80 (m, 1H), 7.33 (m, 1H), 7.27 (m, 2H), 4.71 (s, 2H), 3.70 (t, 2H, J=5.7 Hz), 2.83 (t, 2H, J=5.4 Hz), 1.49 (s, 9H), 1.43 (s, 9H).

N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide

TFA (70 ml) was added dropwise under stirring to N-boc-4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-(2′-boc-aminophenyl)carboxamide (22 g gm) obtained in step VII which was dissolved in 70 ml of dichloromethane, and stirred for 2 hr at room temperature. Reaction mixture was concentrated and dried under vacuum. Residue was taken in water and dichloromethane. Solid K 2 CO 3 was added slowly with continuous stirring till pH become basic (8-9). Reaction mixture was extracted with dichloromethane, washed with brine, dried over anhydrous Na 2 SO 4 and concentrated to yield 9.0 gm of 4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-(2′-aminophenyl)carboxamide.

1 H NMR (DMSO-d 6 ) δ(ppm) 9.90 (s, 1H), 7.27 (dd, 1H, J=1.2 Hz, 7.8), 6.96 (dt, 1H, J=1.5 Hz, 7.5 Hz), 6.78 (dd, 1H, J=1.2 Hz, 7.5 Hz), 6.60 (dt, 1H, J=1.5 Hz, 7.8 Hz), 4.90 (s, 2H), 3.97 (s, 2H), 3.00 (t, 2H, J=5.7 Hz), 2.76 (t, 2H, J=5.7 Hz).

N 2 -(2-aminophenyl)-N5-biphenyl-4-yl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxamide

Biphenylisocyanate was added to a solution of 4,5,6,7-tetrahydrothiazolo-[5,4-c]-pyridine-2-(2′-aminophenyl)carboxamide obtained in step VIII in DMF. The reaction mixture was stirred for 3 h at room temperature and then concentrated under vacuum. The residue was diluted with water and extracted with dichloromethane washed with brine, dried over anhydrous Na 2 SO 4 and concentrated to yield the title compound.

1 HNMR (DMSO-d 6 ) δ(ppm) 8.89 (s, 1H, NH), 7.57 (m, 4H), 7.44 (m, 5H), 7.38 (d, 1H, J=7.2 Hz), 7.11 (t, 1H, J=7.5 Hz), 6.86 (m, 2H), 6.54 (s, 1H), 4.87 (br s, 2H, NH2), 4.82 (s, 2H), 3.85 (t, 2H, J=5.4 Hz), 2.95 (m, 2H).

Examples 2-11 were Obtained by Following the Procedure of Example 1

6-Morpholin-4-yl-pyridin-3-yl-amine (1.0 mmol) was dissolved in 4 mL of dichloromethane and cooled to 0° C. 4-nitrophenylchloroformate (1.0 mmol) solution in 2 mL of dichloromethane was added followed by addition of pyridine (1.0 mmol). Mixture was stirred for 30 minutes at 0° C. brought to room temperature and stirred for additional 12 h. The precipitate formed was collected by filtration washed with dichloromethane and dried. The product 4-nitrophenyl carbonate of respective amine was used for next step without further purification.

The intermediate obtained in step I (1.0 mmol) and N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide. obtained in step VIII of Example 1 (1 mmol) were dissolved in dry DMF or dimethoxyethane/DMSO (7:3) solvent and exposed to microwave radiation at 100° C. for 20 minutes. The reaction mixture was concentrated, diluted with water, extracted with dichloromethane, washed with brine solution, and dried over anhydrous Na 2 SO 4 . Concentrated and purified by column chromatography to yield the title compound.

1 HNMR (DMSO-d 6 ) δ(ppm) 9.97 (s, 1H, NH), 8.64 (s, 1H, NH), 8.17 (d, 1H, J=2.7 Hz), 7.65 (dd, 1H, J=9.0 Hz, 2.7 Hz), 7.27 (dd, 1H, J=8.1 Hz, 1.2 Hz), 6.97 (dt, 1H, J=8.1 Hz, 1.5 Hz), 6.79 (d, 2H, J=9.3 Hz), 6.61 (dt, 1H, J=7.8 Hz, 1.2 Hz), 4.93 (br s, 2H, NH2), 4.83 (s, 2H), 3.86 (t, 2H, J=5.4 Hz), 3.67 (m, 4H), 3.34 (m, 4H), 2.96 (m, 2H)

Examples 35-39 were Obtained by Following the Procedure of Example 34

To a solution of a 5-aminoisoquinoline (1 eq) in dichloromethane, phenyl chloroformate was added at 0° C. and after addition the reaction was continued at room temperature for 1 h Water was added and the organic layer was separated, dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford crude product desired carbamate derivative of Isoqunoline.

NMR (CDCl3) d (ppm) 10.74 (s, 1H), 9.95 (s, 1H), 8.75 (d, 1H, J=6.6 Hz), 8.6 (q, 1H, J=6.6 & 6.9 Hz), 8.38 (q, 2H=5.4 Hz & 4.8 Hz), 8.05 (t, 2H, J=8.1 Hz), 7.72 (m, 1H), 7.44 (m, 2H), 7.30 (m, 3H).

5-tert-butyl 2-ethyl 6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate obtained in step V of example 1 was deprotected to get the hydrochloride salt of 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid ethyl ester. To a solution of a HCl salt of 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid ethyl ester (1.0 eq) in DMF was added Et3N (1.0 eq.) followed by carbamate derivative of Isoquinoline (1.0 eq) obtained in step I above. The reaction mixture was refluxed for 3 h at 90° C. Water was added and the organic layer was separated, dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford crude product, which, was hydrolysed by stirring in MeOH: water and K2CO3 (2.0 eq.) for 48 h Reaction mixture was concentrated under reduced pressure and neutralized to pH 7.0 to afford 5-(Quinolin-5-ylcarbamoyl)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid).

1 HNMR (DMSO-d 6 ) δ(ppm) 9.3 (s, 1H), 8.94 (s, 1H), 8.49 (d, 1H, J=6), 7.93 (d, 1H, J=7.8 Hz), 7.77 (d, 1H, J=7.8 Hz), 7.66 (m, 2H), 4.76 (s, 2H), 3.89 (t, 2H, J=5.6 Hz), 2.87 (t, 2H, J=5.6).

To a solution of the acid derivative (1.0 eq) obtained in step II above in DMF was added triethyl amine (2.2 eq.), EDCI (1.2 eq) and HOBt (1.2 eq) and reaction was stirred for 1 h and then added ortho phenylene diamine and was stirred overnight. Water was added and the organic layer was separated, dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford crude product, which, on purification by column chromatography afforded the title compound.

1 HNMR (DMSO-d 6 ) δ(ppm) 10.01 (s, 1H), 9.31 (s, 1H), 9.03 (s, 1H), 8.50 (d, 1H, J=6.0 Hz), 7.94 (d, 1H, J=7.8 Hz), 7.78 (d, 1H, J=6.0 Hz), 7.62-7.73 (m, 2H), 7.28 (d, 1H, J=7.8 Hz), 6.98 (t, 1H, J=8.7 Hz), 6.80 (d, 1H, J=6.9 Hz), 6.98 (t, 1H, J=7.5 Hz), 4.94 (s, 2H), 4.05 (s, 2H), 3.98 (t, 2H, J=5.4 Hz), 3.06 (b t, 2H)

Methyl 2-({2-[(tert-butoxycarbonyl)amino]phenyl}carbamoyl)-N-phenyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carbimidothioate

A suspension of 5-[(Z)-(methylthio)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxylic acid obtained in step III of example 116 (1 eq), mono Boc-protected o-phenylene diamine (1.2 eq), EDCI (1.2 eq), HOBt (1.2 eq) and triethylamine in DMF were stirred at room temperature for 15 h. Solvent was evaporated and the title intermediate which was purified by either column chromatography or preparative HPLC.

Step-II

tert-butyl {2-[({5-[(E)-(methylamino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl}carbonyl)amino]phenyl}carbamate

A solution of methyl 2-({2-[(tert-butoxycarbonyl)amino]phenyl}carbamoyl)-N-phenyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carbimidothioate obtained form step I (1 eq), and methylamine HCl (60 eq) in DMF was heated at 50° C. in a sealed tube for 72 h. Solvent was evaporated and the residue was purified by either column chromatography or preparative HPLC to afford the tert-butyl {2-[({5-[(E)-(methylamino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl}carbonyl)amino]phenyl}carbamate

1 H NMR (DMSO-d 6 ) δ (ppm): −10.08 (s, 1H), 9.20 (s, 1H), 8.27 (s, 1H), 7.80 (dd, 1H, J=7.2, 2.4 Hz), 7.19-7.33 (m, 5H), 6.86-6.95 (m, 3H), 4.61 (s, 2H), 3.64 (t, 2H, J=5.7 Hz), 2.86 (br t, 2H), 2.64 (s, 3H), 1.47 (s, 9H)

Step-III

N-(2-aminophenyl)-5-[anilino(methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide

tert-butyl {2-[({5-[(E)-(methylamino)(phenylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl}carbonyl)amino]phenyl}carbamate obtained in step II above was treated with ethereal HCl at room temperature for 5-15 h. Solvent was evaporated and the residue was purified by either column chromatography or preparative HPLC to give N-(2-aminophenyl)-5-[anilino(methylimino)methyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide, which was then converted into its dihydrochloride salt.

1 H NMR (DMSO-d 6 ) δ (ppm): −10.43 (s, 1H), 10.21 (s, 1H), 8.81 (m, 1H), 7.39-7.44 (m, 3H), 7.20 (m, 5H), 4.77 (s, 2H), 3.85 (t, 2H, J=5.4 Hz), 3.03 (br t, 2H), 2.83 (d, 3H, J=4.5 Hz)