Prostaglandin endoperoxide H synthase biosynthesis inhibitors

US6307047A · kind A · utility

Assignee

• Abbott Laboratories · US

Inventors

• Lawrence A. Black · Libertyville, US
• Anwer Basha · Lake Forest, US
• Teodozyj Kolasa · Lake Villa, US
• Michael E. Kort · Lake Bluff, US
• Huaqing Liu · Buffalo Grove, US
• Catherine M. McCarty · Brookline, US
• Meena Patel · Libertyville, US
• Jeffrey J. Rohde · Evanston, US
• Michael J. Coghlan · Fishers, US
• Andrew O. Stewart · Wildwood, US

Key dates

• Filing date: Oct 27, 1999
• Grant date: Oct 23, 2001
• Expiry date: Oct 27, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention describes pyridazinone compounds of formula I ##STR1## which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).