Aromatic sulfone hydroxamic acid metalloprotease inhibitor

US6750228B1 · kind B1 · utility

Assignee

• Pharmacia Corporation · SE

Inventors

• Thomas E. Barta · Evanston, US
• Daniel P. Becker · Glenview, US
• Louis Bedell · Rantoul, US
• Terri Boehm · Ballwin, US
• Jeffrey N. Carroll · Columbia, US
• Gary A. DeCrescenzo · Holden, US
• Yvette M. Fobian · Labadie, US
• John N. Freskos · Clayton, US
• Daniel P. Getman · Chesterfield, US
• Joseph McDonald · Ballwin, US
• Madeleine Li · Vernon Hills, US
• Susan L. Hockerman · Kirkwood, US
• Susan C. Howard · Fenton, US
• Steve Kolodziej · Ballwin, US
• Deborah A. Mischke · Defiance, US
• Joseph G. Rico · Ballwin, US
• Nathan Stehle · Ballwin, US
• Michael B. Tollefson · Dardenne Prairie, US
• William Vernier · Chesterfield, US
• Clara I. Villamil · Glenview, US

Key dates

• Filing date: May 12, 2000
• Grant date: Jun 15, 2004
• Expiry date: May 12, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,