Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors

US7435735B2 · kind B2 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• John S. Wai · Harleysville, US
• Thorsten E. Fisher · Hatfield, US
• Linghang Zhuang · Doylestown, US
• Donnette D. Staas · Harleysville, US
• Terry A. Lyle · Lederach, US
• Boyoung Kim · Lexington, US
• Mark W. Embrey · North Wales, US
• Catherine M. Wiscount · Allentown, US
• Lekhanh O. Tran · West Chester, US
• Melissa Egbertson · Ambler, US
• Kelly L. Savage · Schwenksville, US

Key dates

• Filing date: Oct 18, 2004
• Grant date: Oct 14, 2008
• Expiry date: Sep 29, 2025

Classification

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

Abstract

Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 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.