Thrombin inhibitors

US6610692B1 · kind B1 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Philip E. Sanderson · Philadelphia, US
• Bruce D. Dorsey · Ambler, US
• Terry A. Lyle · Lederach, US
• Matthew G. Stanton · Marlton, US
• Donnette D. Staas · Harleysville, US
• Adel M. Naylor-Olsen · Lansdale, US
• Craig A. Coburn · Royersford, US
• Matthew Morrissette · Las Vegas, US

Key dates

• Filing date: Oct 28, 1999
• Grant date: Aug 26, 2003
• Expiry date: Oct 28, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

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 b is NY or O; c is CY2 or N;d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy;A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.