HIV integrase inhibitors

US7598264B2 · kind B2 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Wei Han · Beaverton, US
• Melissa Egbertson · Ambler, US
• John S. Wai · Harleysville, US
• Linghang Zhuang · Doylestown, US
• Rowena D. Ruzek · North Wales, US
• Debra S. Perlow · East Greenville, US
• Mark Cameron · Mississauga, CA
• Bruce S. Foster · Scotch Plains, US
• Ulf H. Dolling · Westfield, US
• R. Scott Hoerrner · Westfield, US
• Philip Pye · Guttenberg, US
• Remy Angelaud · San Francisco, US
• Danny Mancheno · New York, US
• David Askin · Hackettstown, US

Key dates

• Filing date: Mar 9, 2005
• Grant date: Oct 6, 2009
• Expiry date: Sep 20, 2025

Classification

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

Abstract

Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? 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.