Peptidase inhibitors

US5849866A · kind A · utility

Assignee

• Merrell Pharmaceuticals, Inc. · US

Inventors

• H. Michael Kolb · Cincinnati, US
• Joseph P. Burkhart · Plainfield, US
• Michel Jung · Illkirch-Graffenstaden, FR
• Fritz Gerhart · Kehl, DE
• Eugene L. Giroux · Strasbourg, FR
• Bernhard Neises · Griesheim, DE
• Daniel Schirlin · Schiltigheim, FR

Key dates

• Filing date: Jun 7, 1995
• Grant date: Dec 15, 1998
• Expiry date: Jun 7, 2015

Classification

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

Abstract

This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.