Bisaryl derivatives having FSH modulatory activity

US6900213B2 · kind B2 · utility

Assignee

• Pharmacopeia Drug Discovery, Inc. · US

Inventors

• Tao Guo
• Koc-Kan Ho · Mount Kisco, US
• Edward McDonald · Plymouth, US
• Roland E. Dolle · King of Prussia, US
• Kurt W. Saionz · Cranford, US
• Steven G. Kultgen · Hillsborough Township, US
• Ruiyan Liu · Yardley, US
• Guizhen Dong
• Peng Geng · Fryeburg, US
• Anton Egbert Peter Adang · Eindhoven, NL
• Nicole Corine Renee Van Straten · Berghem, NL

Key dates

• Filing date: Jul 21, 2003
• Grant date: May 31, 2005
• Expiry date: Jul 21, 2023

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyland A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.