Prodrugs of HIV replication inhibiting pyrimidines

US7034019B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Michael Joseph Kukla · Masontown, US
• Donald Ludovici · Quakertown, US
• Robert W. Kavash · Glenside, US
• Bart De Corte · Southampton, US
• Jan Heeres · Vosselaar, BE
• Paul Adriaan Jan Janssen · Vosselaar, BE
• Lucien Maria Henricus Koymans · Retie, BE
• Marc René de Jonge · Tilburg, NL
• Koen Jeanne Alfons Van Aken · Kortrijk, BE
• Alain Krief · Wépion, BE

Key dates

• Filing date: May 3, 2001
• Grant date: Apr 25, 2006
• Expiry date: Oct 17, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula