Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors

US6436967B1 · kind B1 · utility

Assignee

• Pharmacia Corporation · SE

Inventors

• John J. Talley · Chesterfield, US
• James W. Malecha · Libertyville, US
• Stephen R. Bertenshaw · Brentwood, US
• Matthew J. Graneto · Chesterfield, US
• Jeffery Carter · Chesterfield, US
• Jinglin Li · Chesterfield, US
• Srinivasan Nagarajan · Arlington Heights, US
• David L. Brown · Chesterfield, US
• Donald J. Rogier, Jr. · Chesterfield, US
• Thomas D. Penning · Elmhurst, US
• Ish Khanna · Vernon Hills, US
• Xiangdong Xu · Gurnee, US
• Richard M. Weier · Lake Bluff, US

Key dates

• Filing date: Sep 14, 2000
• Grant date: Aug 20, 2002
• Expiry date: Sep 14, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2.The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.