The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk ofâ€”or susceptible toâ€”a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity. [structure]

Claims

10 · 1 independent · depth 2

10 granted claims

›1.independentA compound of the formula (I):+9

›2.↳ 1The compound according to claim 1, represented by the formula (Ia):d2

›3.↳ 1The compound according to claim 1, represented by the formula (Ib):d2

›4.↳ 1The compound according to claim 1 represented by the formula (Ic):d2

›5.↳ 1The compound according to claim 1, represented by the formula (Id):d2

›6.↳ 1The compound according to claim 1 wherein said compound is:n5-isoxazoyl-Cha-Ile-aminomethylphenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-methoxy)phenyl;5-…d2

The compound according to claim 1 wherein said compound is:n5-isoxazoyl-Cha-Ile-aminomethylphenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-methoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3-methoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(4-methoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-methyl)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-ethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-propoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-isopropoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-butoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-isobutoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-chloro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-nitro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-trifluoromethyl)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3-trifluoromethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-trifluoromethyl)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(4-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(1,3-dioxalane)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3,4-dichloro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,4-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,5-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3,4-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,3-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,3,4-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,6-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-methoxy-5-trifluoromethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2,4-dimethoxy)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3,5-bis(trifluoromethyl))phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(2-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(4-fluoro)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(1,3-dioxalane)phenyl;5-isoxazoyl-Cha-Ile-aminomethyl-(3,4-dichloro)phenyl;5-isoxazoyl-Cha-Ile-(4-phenyl) piperidine;5-isoxazoyl-Cha-Ile-4-(p-methoxy)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(p-chloro)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(o-trifluoromethyl)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(o-phenyl)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(m-phenyl)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(p-phenyl)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(p-phenoxy)phenyl piperidine;5-isoxazoyl-Cha-Ile-4-(2,5-dimethoxy)phenyl piperidine;5-isoxazoyl-Cha-Ile-(4-benzyl)piperidine;5-isoxazoyl-Cha-Ile-2S-(tert-butylamide)piperidine;5-isoxazoyl-Cha-Ile-4-(4-acetamide)phenyl piperidine;5-isoxazoyl-Cha-Ile-3-(o-fluoro)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-3-(m-fluoro)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-3-(p-fluoro)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-3-(o-trifluoromethyl)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-3-(m-trifluoromethyl)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-3-(p-trifluoromethyl)aminophenylpiperidine;5-isoxazoyl-Cha-Ile-spirochroman-2,4⬲-piperidine;5-isoxazoyl-Cha-Ile-[(S)-N-(tert-butyl)]piperidine;5-isoxazoyl-Cha-Ile-aminodimethyl-(2-methoxy)phenyl;5-isoxazoyl-Cha-Ile-(3-[aminomethyl]phenyl)-amino-4-aminobutane-1-carboxamide;5-isoxazoyl-Cha-Ile-(3-[aminomethyl]phenyl)-amino-3-aminopropane-1-carboxamide; or 5-isoxazoyl-Cha-Ile-4-(p-fluorophenyl)piperazine.

›7.↳ 1The compound according to claim 1 wherein said compound is:n5-isoxazoyl-Cha-Ile-aminomethyl-benzimidazole;5-isoxazoyl-Cha-Ile-aminomethyl-2-biphenyl;5…d2

›8.↳ 1A method of modulating the activity of PAR2 comprising exposing the receptor to a compound according claim 1.d2

›9.↳ 1A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier, excipient, diluent and/or adjuvant.d2

›10.↳ 1The compound according to claim 1, represented by the formula (Ia):d2

Classifications

20 codes

IPC · International Patent Classification

Section A — Human necessities

A61K38/07
A61K38/00
A61K38/06
A61K38/05

Section C — Chemistry; metallurgy

C07K17/00
C07K5/065
C07D471/00
C07K5/062
C07D401/00
C07K5/00
C07D455/00
C07D451/00
C07D453/00
C07K5/083
C07K7/00
C07K16/00

USPC · US Patent Classification

514/21.9530/331546/17514/21.91

Claim changes

Soon

Coming soonHow the claims changed between publication and grant

See which claims were amended, added or cancelled during examination, with every added and removed word marked.

AmendedAddedCancelledUnchanged

The published claims of this patent are not paired with the granted ones in what we hold.

File wrapper

Pendency

3.3 y

1,223 days filing → grant

Office actions

after a restriction

Responses

no RCE

Interviews

examiner interview summaries

Examiner

Zachary J Miknis

art unit —

Law firm

Law firm · Log in to unlock

Citations: 38 back · 0 forward

See the full prosecution history — every USPTO and applicant action on this file, in order.

Term & fees

See the term timeline — pendency span, in-force span, the maintenance fees paid and both computed expiry dates.

Priority chain

1 priority documents

›Priority documents — 1

Type	Document	Date
related publication	US 20130184226 A1	18 Jul 2013

Validity challenges

See the validity challenges on record — reexaminations, IPRs and PGRs, with their institution decisions and outcomes.

Citations

See every patent this one cites and every patent that cites it back — publication, assignee, and how each one was found.