IP Library › Granted Patent US 8,455,658
Granted Patent B2
US 8,455,658 · App. 11/698,772 · Granted Jun 4, 2013

Thiazole and thiadiazole compounds for inflammation and immune-related uses

Inventors: Nha Huu Vo (Southborough, MA); Shoujun Chen (Bedford, MA); Qinglin Che (Foxboro, MA); Yu Xie (Natick, MA)
Assignee: Synta Pharmaceuticals Corp.
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Quick Facts
Patent No.
US 8,455,658
App. No.
11/698,772
Granted
Jun 4, 2013
Kind
B2
Abstract

The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R′ 1 , X, X′, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Claims (35)

1. A compound represented by formula (XI):

or a pharmaceutically acceptable salt or prodrug thereof, wherein:

L 1 is —NR—C(O)— or —C(O)—NR—;

Y′ is aryl substituted with one or more halo and/or alkyl groups;

Z is selected from the group consisting of optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, an optionally substituted heteraralkyl, a haloalkyl, —C(O)NR 1 R 2 , —NR 4 C(O)R 5 , halo, —OR 4 , cyano, nitro, haloalkoxy, —C(O)R 4 , —NR 1 R 2 , —SR 4 , —C(O)OR 4 , —OC(O)R 4 , —NR 4 C(O)NR 1 R 2 , —OC(O)NR 1 R 2 , —NR 4 C(O)OR 5 , —S(O) p R 4 , and —S(O) p NR 1 R 2 ;

Z 10 is an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, an optionally substituted heteraralkyl, a haloalkyl, —C(O)NR 1 R 2 , —NR 4 C(O)R 5 , halo, cyano, nitro, haloalkoxy, —C(O)R 4 , —NR 1 R 2 , —SR 4 , —C(O)OR 4 , —OC(O)R 4 , —NR 4 C(O)NR 1 R 2 , —OC(O)NR 1 R 2 , —NR 4 C(O)OR 5 , —S(O) p R 4 , or —S(O) p NR 1 R 2 ;

Z 11 is —H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, an optionally substituted heteraralkyl, a haloalkyl, —C(O)NR 1 R 2 , —NR 4 C(O)R 5 , halo, —OR 4 , cyano, nitro, haloalkoxy, —C(O)R 4 , —NR 1 R 2 , —SR 4 , —C(O)OR 4 , —OC(O)R 4 , —NR 4 C(O)NR 1 R 2 , —OC(O)NR 1 R 2 , —NR 4 C(O)OR 5 , —S(O) p R 4 , or —S(O) p NR 1 R 2 ;

R, for each occurrence, is independently —H, alkyl, —C(O)—R 7 , or —C(O)OR 7 ;

R 1 and R 2 , for each occurrence are, independently, H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, or an optionally substituted heteraralkyl; or R 1 and R 2 taken together with the nitrogen to which they are attached is optionally substituted heterocyclyl or optionally substituted heteroaryl;

R 4 and R 5 , for each occurrence are, independently, H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, or an optionally substituted heteraralkyl;

R 6 , for each occurrence, is —H or alkyl;

R 7 , for each occurrence is, independently, H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted cycloalkyl, an optionally substituted cycloalkenyl, an optionally substituted heterocyclyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl, or an optionally substituted heteraralkyl; and

p is 0, 1, or 2.

2. The compound of claim 1 , wherein:

L 1 is —NR—C(O)—, or —C(O)—NR—;

Y′ is a substituted phenyl, wherein the substituents are each independently a lower alkyl or a halo;

Z is chloro, bromo, fluoro, cyano, trifluoromethyl, —OCH 3 , —C(O)CH 3 , 2-methyl-2H-tetrazolyl, methoxy, nitro, dimethylamino, thiazol-2-yl, oxazol-2-yl, or methyl;

Z 10 is halo or an optionally substituted lower alkyl;

Z 11 is —H, an optionally substituted lower alkyl, an optionally substituted lower alkenyl, an optionally substituted lower alkynyl, an optionally substituted cycloalkyl, —C(O)OR 4 , —C(O)R 4 , —C(O)NR 1 R 2 , —NR 1 R 2 , cyano, halo, an optionally substituted oxazolyl, an optionally substituted imidazolyl, an optionally substituted oxadiazolyl, an optionally substituted thiazolyl, an optionally substituted pyrazolyl, an optionally substituted pyridinyl, or an optionally substituted phenyl.

3. The compound of claim 2 , wherein

L 1 is —NH—C(O)— or —C(O)—NH—;

Y′ is 2,6-difluorophenyl;

Z 10 is halo or methyl; and

Z 11 is —H or methyl.

4. A compound selected from the group consisting of:

(2-(2-Chloro-5-trifluoromethyl-phenyl)-thiazole-5-carboxylic acid 2,6-difluoro-phenyl)-amide;

2-(2-Chloro-5-trifluoromethyl-phenyl)-4-methyl-thiazole-5-carboxylic acid (2,6-difluoro-phenyl)-amide;

N-(2,6-difluorophenyl)-2-(2-methyl-5-(oxazol-2-yl)phenyl)thiazole-5-carboxamide;

N-(2,6-difluorophenyl)-2-(2-methyl-5-(thiazol-2-yl)phenyl)thiazole-5-carboxamide;

N-(2,6-difluorophenyl)-2-(3-(trifluoromethyl)phenyl)thiazole-5-carboxamide;

N-(2,6-difluorophenyl)-2-(3-(oxazol-2-yl)phenyl)thiazole-5-carboxamide;

2-(2-chloro-5-(thiazol-2-yl)phenyl)-N-(2,6-difluorophenyl)thiazole-5-carboxamide; or

N-(2,6-difluorophenyl)-2-(2-methyl-5-(1,3,4-oxadiazol-2-yl)phenyl)thiazole-5-carboxamide;

or a pharmaceutically acceptable salt or prodrug thereof.

5. A pharmaceutical composition, comprising a pharmaceutically acceptable carrier and a compound of claim 4 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2009
From: VO, NHA H.; CHEN, SHOUJUN; CHE, QINGLIN; XIE, YU
To: SYNTA PHARMACEUTICALS CORP.
Reel/Frame 022431/0852 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2007
From: VO, NHA HUU; CHEN, SHOUJUN; CHE, QINGLIN; XIE, YU
To: SYNTA PHARMACEUTICALS CORP.
Reel/Frame 019565/0255 →
Continuity (3)
Provisional Application 60761974 · Jan 25, 2006
Provisional Application 60761933 · Jan 25, 2006
Related Publication 20070254925A1 · Nov 1, 2007