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US 6,387,911 B1Granted
Pyrazinone thrombin inhibitors
AssigneeMerck & Co., Inc.
InventorsChristopher Burgey, Richard C. Isaacs, Bruce D. Dorsey, Kyle A. Robinson, Donnette Staas, Philip E. Sanderson, James Barrow
Life of this patent
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Abstract
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein A is
Claims14
A compound having the formula:
- wherein
- A is
- n=0-1;
- R is
- hydrogen,
- R2 is
- hydrogen,
- C1-4 alkyl,
- CF3,
- halogen,
- cyano, or
- cyclo C3-7 alkyl;
- R3, P7, R8, and R13 are independently chosen from
- hydrogen,
- halogen,
- C1-4 alkyl;
- R14 and R15 are independently chosen from
- hydrogen,
- C1-2 alkyl, and
- C1-2 alkyl substituted with OR16 or COOR16, wherein R16 is hydrogen or C1-4 alkyl;
- and
- R4, R5 and R6 are independently chosen from
- hydrogen,
- halogen,
- hydroxy,
- C1-4 alkyl,
- C1-4 alkoxy,
- cyano,
- CF3O,
- CHF2O,
- CF3CH2O,
- SR10,
- SOR10,
- SO2R10,
- OR11,
- SR11,
- NHR11
- wherein
- R10 is C1-4 alkyl unsubstituted or substituted with C(CH3)2NH2, C(CH3)2OH, C(CH3)2NHCOCF3, or CF3, and
- R11 is phenyl unsubstituted or substituted with one or more of C1-4 alkyl, C1-4 alkoxy, halogen, hydroxy, COOH, CONH2, CH2OH, or CO2R12, wherein R12 is C1-4 alkyl.
37 more elements
Dependencies are inferred from the claim text.