HIV integrase inhibitors

US8513234B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Richard Isaacs · Harleysville, US
• Wayne Thompson · Lansdale, US
• Peter D. Williams · Harleysville, US
• Dai-Shi Su · New York, US
• Shankar Venkatraman · Lansdale, US
• Mark W. Embrey · North Wales, US
• Thorsten E. Fisher · Hatfield, US
• John S. Wai · Harleysville, US
• David C. Dubost · Collegeville, US
• Richard G. Ball · Edison, US
• Eric J. Choi · Libertyville, US
• Tao Pei · Morganville, US
• Sarah L. Trice · Glenside, US
• Neil Campbell · Liverpool, GB
• Matthew L. Maddess · Boston, US
• Peter E. Maligres · Fanwood, US
• Michael Shevlin · Plainfield, US
• Zhiguo Jake Song · Edison, US
• Dietrich P. Steinhuebel · Boston, US
• Neil A. Strotman · Flemington, US
• Jingjun Yin · Haddonfield, US

Key dates

• Filing date: Oct 2, 2009
• Grant date: Aug 20, 2013
• Expiry date: Jan 27, 2031

Classification

• Technology area (CPC H): Electricity
• CPC primary: H01L2924/0002
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication:wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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. Processes for making compounds of Formula I and intermediates thereof are also described.