Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents

US5608095A · kind A · utility

Assignee

• Hoechst Marion Roussel · FR

Inventors

• Roger A. Parker · Cincinnati, US
• Michael L. Edwards · Cincinnati, US
• Mark Vaal · Baltimore, US
• James Edward Matt · Indianapolis, US
• Kim S. Chen · San Diego, US
• Mark T. Yates · Cincinnati, US
• Paul S. Wright · New Hope, US
• Steven J. Busch · Stewartsville, US

Key dates

• Filing date: Apr 30, 1996
• Grant date: Mar 4, 1997
• Expiry date: Apr 30, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to compounds of the formula ##STR1## wherein R.sub.1 and R.sub.6 are each independently C.sub.1 -C.sub.6 alkyl; PA1 R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; PA1 R is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4; PA1 Z is a thio, oxy or methylene group; PA1 A is a C.sub.1 -C.sub.4 alkylene group; PA1 R.sub.5 and R.sub.7 are each independently a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, or --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; with the proviso that when R.sub.2 and at least one of R.sub.5 or R.sub.7 is C.sub.1 -C.sub.6 alkyl, and Ar is not substituted with trifluoromethyl or --NR.sub.8 R.sub.9, then R is --C(O)--(CH.sub.2).sub.m --Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflam…