Rary-specific retinobenzoic acid derivatives

US5624957A · kind A · utility

Assignee

• Bristol-Myers Squibb Company · US

Inventors

• R. Thomas Swann · Hamden, US
• Daniel S. Smith · Columbia, US
• Kenneth M. Tramposch · East Amherst, US
• Fred Zusi · Hamden, US

Key dates

• Filing date: Jun 6, 1995
• Grant date: Apr 29, 1997
• Expiry date: Jun 6, 2015

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein X is F, Cl, OH or CH.sub.3, Y is H or F, R.sub.1 -R.sub.6 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, n is an integer of 1 to 4 and R.sub.7 is hydrogen or a carboxyl-protecting group, and pharmaceutically acceptable salts thereof. The compounds of formula I selectively interact with the retinoic acid subtype RAR.gamma. and have been found to lack the liver toxicity associated with systemic administration of non-selective retinoids.