.alpha.-heteroaryloxymethyl ketones as interleukin - 1 .beta. converting enzyme inhibitors

US5677283A · kind A · utility

Assignee

• Sanofi · FR

Inventors

• Roland E. Dolle · King of Prussia, US
• Jasbir Singh · Gilbertsville, US
• David A. Whipple · New London, US
• Catherine P. Prouty · Doylestown, US
• Prasad V. Chaturvedula · Exton, US
• Stanley J. Schmidt · Chester Springs, US
• Mohamed M. A. Awad · Westerly, US
• Denton W. Hoyer · West Haven, US
• Tina Morgan Ross · Limerick, US

Key dates

• Filing date: Oct 16, 1996
• Grant date: Oct 14, 1997
• Expiry date: Oct 16, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-4-(pyridyl)methyl!, N-4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; and R.sub.8, R.sub.9 and R.sub.10 are as defined below.