N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase

US7820660B2 · kind B2 · utility

Assignee

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

Inventors

• Benedetta Crescenzi · Roma, IT
• Cristina Gardelli · Pomezia, IT
• Ester Muraglia · Roma, IT
• Emanuela Nizi · Siena, IT
• Federica Orvieto · Roma, IT
• Paola Pace · Roma, IT
• Giovanna Pescatore · Cosenza, IT
• Alessia Petrocchi · Roma, IT
• Marco Poma · Grosseto, IT
• Michael Rowley · Roma, IT
• Rita Scarpelli · Pomezia, IT
• Vincenzo Summa · Pomezia, IT

Key dates

• Filing date: Jun 20, 2008
• Grant date: Oct 26, 2010
• Expiry date: Dec 23, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula:are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.