N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors

US7323460B2 · kind B2 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Melissa Egbertson · Ambler, US
• H. Marie Langford · Marlboro, US
• Jeffrey Melamed · North Wales, US
• John S. Wai · Harleysville, US
• Wei Han · Beaverton, US
• Debbie S. Perlow · East Greenville, US
• Linghang Zhuang · Doylestown, US
• Mark W. Embrey · North Wales, US

Key dates

• Filing date: Mar 12, 2003
• Grant date: Jan 29, 2008
• Expiry date: Apr 6, 2024

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I):wherein R1′, R2′ and R3′ are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.