17-beta-hydroxysteroid dehydrogenase-II inhibitors

US6784167B2 · kind B2 · utility

Assignee

• Bayer Pharmaceuticals Corporation · US

Inventors

• Jill Wood · Hampton, US
• Jeremy Lee Baryza · Mountain View, US
• Catherine Brennan · Durham, US
• Soongyu Choi · Skillman, US
• James H. Cook, II · East Hampton, US
• Brian R. Dixon · Woodbridge, US
• Paul P. Ehrlich · Libertyville, US
• David Gunn · Waukegan, US
• Ian A. McAlexander · Pocatello, US
• Peiying Liu · Madison, US
• Derek Lowe · Scotch Plains, US
• Aniko Redman · Derby, US
• William Scott · Guilford, US
• Yamin Wang · Hubei, CN

Key dates

• Filing date: Sep 28, 2001
• Grant date: Aug 31, 2004
• Expiry date: Dec 10, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/06
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl. Pharmaceutically acceptable salts and N-oxides of these materials are also included. Also claimed are pharmaceutical compositions containing these materials and methods of using them.