Pyrazinone thrombin inhibitors

US6455532B1 · kind B1 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Christopher S. Burgey · Philadelphia, US
• Kyle Robinson · Cheltenham, US
• Peter D. Williams · Harleysville, US
• Craig A. Coburn · Royersford, US
• Terry A. Lyle · Lederach, US
• Philip E. Sanderson · Philadelphia, US

Key dates

• Filing date: Jun 1, 2000
• Grant date: Sep 24, 2002
• Expiry date: Jun 1, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is  wherein Y1 and Y2 are independentlyhydrogen,C1-4 alkyl,C1-4 alkoxy,FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1,C3-7 cycloalkyl,thio C1-4 alkyl,C1-4 sulfinylalkyl,C1-4 sulfonylalkyl,halogencyano, ortrifluoromethyl, andwherein b is 0 or 1.