IP Library › Granted Patent US 8,435,996
Granted Patent B2
US 8,435,996 · App. 12/452,979 · Granted May 7, 2013

Heterocycle-aryl compounds for inflammation and immune-related uses

Inventor: Shoujun Chen (Bedford, MA)
Assignee: Synta Pharmaceuticals Corp.
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Quick Facts
Patent No.
US 8,435,996
App. No.
12/452,979
Granted
May 7, 2013
Kind
B2
Abstract

The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Claims (33)

1. A compound selected from the group consisting of:

2,6-difluoro-N-(4-(5-(isoxazol-5-yl)-3-methylthiophen-2-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(3-methyl-5-(thiazol-2-yl)thiophen-2-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(3-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-2-yl)phenyl)benzamide;

2,6-difluoro-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;

2,6-difluoro-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-2-yl)benzamide;

2,6-difluoro-N-(4-(3-methyl-5-(pyridin-3-yl)thiophen-2-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(2-methyl-5-(pyridin-3-yl)thiophen-3-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(2-methyl-5-(1,3,4-oxadiazol-2-yl)thiophen-3-yl)phenyl)benzamide;

2,6-difluoro-N-(6-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-3-yl)benzamide;

N-(4-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;

2,6-difluoro-N-(4-(2-methyl-5-(4-methylpyridin-3-yl)thiophen-3-yl)phenyl)benzamide;

N-(4-(5-(5-chloro-2-methoxypyridin-3-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;

2,6-difluoro-N-(5-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)pyridin-2-yl)benzamide;

2,6-difluoro-N-(5-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;

N-(5-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)pyridin-2-yl)-2,6-difluorobenzamide;

2,6-difluoro-N-(5-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)pyridin-2-yl)benzamide;

3-methyl-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-2-yl)isonicotinamide;

N-(4-(5-(4-chloropyridin-3-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;

2,6-difluoro-N-(4-(5-(4-methoxypyridin-3-yl)-2-methylthiophen-3-yl)phenyl)benzamide;

2,6-difluoro-N-(5-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;

N-(5-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)pyrazin-2-yl)-2,6-difluorobenzamide;

2,6-difluoro-N-(4-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)phenyl)benzamide;

2,6-difluoro-N-(4-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)phenyl)benzamide hydrochloride; and

N-(4-(5-(1-ethyl-1H-imidazol-5-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide; or

a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition, comprising a compound of claim 1 , and:

(i) a pharmaceutically acceptable carrier; and/or

(ii) one or more additional therapeutic agents.

3. The pharmaceutical composition according to claim 2 , wherein the one or more additional therapeutic agents is selected from

the group consisting of immunosuppressive agents, anti-inflammatory agents and mixtures thereof; or is selected from

the group consisting of steroids, non-steroidal anti-inflammatory agents, antihistamines, analgesics, and suitable mixtures thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2010
From: CHEN, SHOUJUN
To: SYNTA PHARMACEUTICALS CORP.
Reel/Frame 024570/0373 →
Continuity (2)
Provisional Application 60962824 · Aug 1, 2007
Related Publication 20100286103A1 · Nov 11, 2010