IP Library Granted Patent US 8,030,318
Granted Patent B2
US 8,030,318 · App. 11/909,118 · Granted Oct 4, 2011

Fused bicyclic inhibitors of HCV

Assignee: Tibotec Pharmaceuticals Ltd.
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Quick Facts
Patent No.
US 8,030,318
App. No.
11/909,118
Granted
Oct 4, 2011
Kind
B2
Abstract

Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.

Claims (24)

1. A compound, or pharmaceutically acceptable salt thereof, selected from the group consisting of:

4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-methylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-dimethylamino-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-dimethylamino-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-(2-hydroxy-propyl)-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-methoxy-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(4-methoxy-benzylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-cyclopropyl-nicotinamide;

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-cyclopropyl-nicotinamide; and

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-(2-hydroxy-propyl)-nicotinamide.

2. A method of treating conditions associated with hepatitis C virus in a warm-blooded animal, comprising administering an effective amount of a compound, or pharmaceutically acceptable salts thereof, selected from the group consisting of:

4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-methylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-dimethylamino-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-dimethylamino-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-(2-hydroxy-propyl)-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(2-methoxy-ethylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-methyl-nicotinamide;

4-[2-(5-Chloro-2-fluoro-phenyl)-7-(4-methoxy-benzylamino)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-cyclopropyl-nicotinamide;

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-cyclopropyl-nicotinamide; and

4-[7-Amino-2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-N-(2-hydroxy-propyl)-nicotinamide, and

wherein said conditions are characterized by high levels of transforming growth factor-beta (TGFβ) activity and wherein said effective amount treats said conditions.

3. The method of claim 1 , wherein the compound is 4-[2-(5-Chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamino]-nicotinamide or a pharmaceutically acceptable salt thereof.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 16, 2009
From: SIMMEN, KENNETH A.; SURLERAUX, DOMINQUE LOUIS NESTOR GHISLAIN; LIN, TSE-I; LENZ, OLIVER; RABOISSON, PIERRE JEAN-MARIE BERNARD
To: TIBOTEC BVBA
Reel/Frame 023664/0198 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 16, 2009
From: CHAKRAVARTY, SARVAJIT; HART, BARRY PATRICK
To: SCIOS INC.
Reel/Frame 023664/0246 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 16, 2009
From: TIBOTEC BVBA
To: TIBOTEC PHARMACEUTICALS LTD.
Reel/Frame 023664/0252 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 16, 2009
From: SCIOS INC.
To: TIBOTEC PHARMACEUTICALS LTD.
Reel/Frame 023664/0261 →
Continuity (3)
Provisional Application 60665151 · Mar 25, 2005
Provisional Application 60680405 · May 12, 2005
Related Publication 20080182863A1 · Jul 31, 2008