IP Library Granted Patent US 7,618,981
Granted Patent B2
US 7,618,981 · App. 11/121,709 · Granted Nov 17, 2009

Imidazopyridinyl-benzamide anti-cancer agents

Assignees: Cytokinetics, Inc.; SmithKline Beecham Corporation
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Quick Facts
Patent No.
US 7,618,981
App. No.
11/121,709
Granted
Nov 17, 2009
Kind
B2
Abstract

Provided are compounds of Formula V and pharmaceutically acceptable salts thereof which may be useful for the treatment of cancer or other proliferative disorders.

Claims (36)

1. A compound of Formula V

or a pharmaceutically acceptable salt thereof wherein

R 2 is hydrogen or lower alkyl;

R 3 is chosen from

lower alkyl substituted with a hydroxyl or a phosphate ester thereof and

lower alkyl substituted with an amino group wherein the amino group is further substituted with a group —COR b wherein R b is chosen from hydrogen, C 1 -C 6 alkyl, aryl, and heteroaryl;

R 11 is hydrogen, cyano, nitro, or halo;

R 12 is lower alkoxy or 2,2,2-trifluoro-1-methyl-ethoxy;

R 13 is hydrogen, alkyl-, alkoxy, halo, hydroxyl, nitro, cyano, or amino;

R 14 is imidazo[1,2-a]pyridin-2-yl optionally substituted with one or two groups chosen from lower alkyl, halo, acyl, trifluoromethyl, aminomethyl, and lower alkyl substituted with hydroxy; and

R 15 is chosen from hydrogen, halo, hydroxyl, and lower alkyl.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 15 is hydrogen.

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 11 is chloro or cyano.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 12 is propoxy or 2,2,2-trifluoro-1-methyl-ethoxy.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 13 is hydrogen.

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen.

7. A composition comprising a pharmaceutical excipient and at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof.

8. A compound of Formula V

or a pharmaceutically acceptable salt thereof wherein

R 2 is hydrogen or lower alkyl:

R 3 is —CH 2 CH 2 OH, —CH 2 NHC(O)CH 2 N(CH 3 ) 2 or —CH 2 NHC(O)C(CH 3 ) 2 NH 2

R 11 is hydrogen, cyano, nitro, or halo;

R 12 is lower alkoxy or 2,2,2-trifluoro-1-methyl-ethoxy;

R 13 is hydrogen, alkyl-, alkoxy, halo, hydroxyl, nitro, cyano, or amino;

R 14 is imidazo[1,2-a]pyridin-2-yl optionally substituted with one or two groups chosen from lower alkyl, halo, acyl, trifluoromethyl, aminomethyl, and lower alkyl substituted with hydroxy; and

R 15 is chosen from hydrogen, halo, hydroxyl, and lower alkyl.

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 14 is 8-methyl-imidazo[1,2-a]pyridin-2-yl, 8-ethyl-imidazo[1,2-a]pyridin-2-yl, 8-chloro-imidazo[1,2-a]pyridin-2-yl, 8-trifluoromethyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-acetyl-imidazo[1,2-a]pyridin-2-yl, 8-isopropyl-imidazo[1,2-a]pyridin-2-yl, 8-acetyl-5-methyl-imidazo[1,2-a]pyridin-2-yl, 8-hydroxymethyl-imidazo[1,2-a]pyridin-2-yl, 5-methyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-methyl-1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxypropyl)-imidazo[1,2-a]pyridin-2-yl, 8-(aminomethyl)imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridin-2-yl, 8-[(1R)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, 8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, 3-fluoro-8-methylimidazo[1,2-a]pyridin-2-yl, 8-ethyl-5-methylimidazo[1,2-a]pyridin-2-yl, or 3-chloro-8-methylimidazo[1,2-a]pyridin-2-yl.

10. The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein R 14 is 8-methyl-imidazo[1,2-a]pyridin-2-yl, 8-ethyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-hydroxymethyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-methyl-1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxypropyl)-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridin-2-yl, 8-[(1R)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, or 8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl.

11. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 15 is hydrogen.

12. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 11 is chloro or cyano.

13. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 12 is propoxy or 2,2,2-trifluoro-1-methyl-ethoxy.

14. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 13 is hydrogen.

15. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen.

16. A composition comprising a pharmaceutical excipient and at least one compound of claim 8 , or a pharmaceutically acceptable salt thereof.

17. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 14 is 8-methyl-imidazo[1,2-a]pyridin-2-yl, 8-ethyl-imidazo[1,2-a]pyridin-2-yl, 8-chloro-imidazo[1,2-a]pyridin-2-yl, 8-trifluoromethyl-imidazo[1,2-a]pyridin-2-yl, 8-( 1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-acetyl-imidazo[1,2-a]pyridin-2-yl, 8-isopropyl-imidazo[1,2-a]pyridin-2-yl, 8-acetyl-5-methyl-imidazo[1,2-a]pyridin-2-yl, 8-hydroxymethyl-imidazo[1,2-a]pyridin-2-yl, 5-methyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-methyl-1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxypropyl)-imidazo[1,2-a]pyridin-2-yl, 8-(aminomethyl)imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridin-2-yl, 8-[(1R)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, 8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, 3-fluoro-8-methylimidazo[1,2-a]pyridin-2-yl, 8-ethyl-5-methylimidazo[1,2-a]pyridin-2-yl, or 3-chloro-8-methylimidazo[1,2-a]pyridin-2-yl.

18. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein R 14 is 8-methyl-imidazo[1,2-a]pyridin-2-yl, 8-ethyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-hydroxymethyl-imidazo[1,2-a]pyridin-2-yl, 8-(1-methyl-1-hydroxy-ethyl)-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxypropyl)-imidazo[1,2-a]pyridin-2-yl, 8-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridin-2-yl, 8-[(1R)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl, or 8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2010
From: GLAXOSMITHKLINE LLC
To: CYTOKINETICS, INCORPORATED
Reel/Frame 024245/0434 →
CHANGE OF NAME Recorded Mar 29, 2010
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 024140/0964 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 8, 2007
From: DUFFY, KEVIN; FITCH, DUKE; TEDESCO, ROSANNA
To: SMITHKLINE BEECHAM CORPORATION
Reel/Frame 018722/0327 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2005
From: DHANAK, DASHYANT; KNIGHT, STEVEN D.; ADAMS, NICHOLAS D.; PARRISH, CYNTHIA A.
To: SMITHKLINE BEECHAM CORPORATION
Reel/Frame 016790/0190 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2005
From: QIAN, XIANGPING; ZHOU, HAN-JIE; ASHCRAFT, LUKE W.; YAO, BING; JIANG, HONG; HUANG, JENNIFER KUO CHEN; WANG, JIANCHAO; MORGANS, DAVID J. JR.; MORGAN, BRADLEY PAUL; BERGNES, GUSTAVE
To: CYTOKINETICS, INC.
Reel/Frame 016790/0192 →
Continuity (2)
Provisional Application 6056951000 · May 6, 2004
Related Publication 20060094708A1 · May 4, 2006