The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (â€œmGluR2â€ ) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

Claims

18 · 1 independent · depth 3

18 granted claims

›1.independentA compound of formula+17

›2.↳ 1A compound as claimed in claim 1 wherein R1 is C4-6 alkyl.d2+1

›4.↳ 1A compound as claimed in claim 1 wherein R1 is C1-3 alkyl substituted with C3-7 cycloalkyl.d2+1

›6.↳ 1A compound as claimed in claim 1 wherein R2 is hydrogen or halo.d2

›7.↳ 1A compound as claimed in claim 1 wherein R2 is trifluoromethyl.d2

›8.↳ 1A compound as claimed in claim 1 wherein R3 is hydrogen.d2

›9.↳ 1A compound as claimed in claim 1 wherein R3 is C1-4 alkyl substituted with hydroxyl.d2+1

›11.↳ 1A compound as claimed in claim 1 wherein X is O or NH.d2

›12.↳ 1A compound as claimed in claim 1 wherein n is 1 or 2.d2

›13.↳ 1A compound as claimed in claim 1 wherein n is 1 and R2 is other than hydrogen and said R2 is placed in meta position compared to the pyridinone moiety…d2

›14.↳ 1A compound as claimed in claim 1 wherein R1 is 1-butyl, methyl-1-butyl, cyclopropylmethyl or 2-(cyclopropyl)-1-ethyl; R2 is hydrogen, fluoro, chloro o…d2

›15.↳ 1A compound as claimed in claim 1 wherein the compound is selected fromd2

›16.↳ 1A compound as claimed in claim 1 wherein the compound is selected fromd2

›17.↳ 1A pharmaceutical composition comprising a therapeutically effective amount of a compound as claimed in claim 1 and a pharmaceutically acceptable carri…d2

›18.↳ 1A process for preparing a compound as claimed in claim 1, comprisingna) reacting an intermediate of formula (II) wherein Y represents a halo or trifla…d2

Classifications

4 codes

IPC · International Patent Classification

Section A — Human necessities

A61K31/4433

Section C — Chemistry; metallurgy

C07D405/12

USPC · US Patent Classification

514/336546/282.1

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Pendency

6.4 y

2,342 days filing → grant

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5 RCE

Examiner

Zinna Northington Davis

art unit 1625 · TC 1600

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1 priority documents

›Priority documents — 1

Type	Document	Date
related publication	US 20100087487 A1	8 Apr 2010

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