Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 .beta. inventory enzyme

US5411985A · kind A · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Gerald F. Bills · Clark, US
• Otto D. Hensens · Red Bank, US
• Jerrold M. Liesch · Princeton Junction, US
• Russel B. Lingham · Watchung, US
• Jon D. Polishook · Cranford, US
• Michael J. Salvatore · Greenwich, US
• Susan L. Raghoobar · Fords, US

Key dates

• Filing date: May 17, 1993
• Grant date: May 2, 1995
• Expiry date: May 17, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12R2001/645
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##