Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors

US7414045B2 · kind B2 · utility

Assignee

• Istituto di Recerche di Biologia Molecolare P. Angeletti S.R.L. · IT

Inventors

• Benedetta Crescenzi · Roma, IT
• Olaf Kinzel · Heidelberg, DE
• Ester Muraglia · Roma, IT
• Federica Orvieto · Roma, IT
• Giovanna Pescatore · Cosenza, IT
• Michael Rowley · Roma, IT
• Vincenzo Summa · Pomezia, IT

Key dates

• Filing date: Dec 18, 2003
• Grant date: Aug 19, 2008
• Expiry date: Aug 13, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These 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.