Substituted diamino-1,3,5-triazine derivatives

US6858609B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Paul Adriaan Jan Janssen · Vosselaar, BE
• Jan Heeres · Vosselaar, BE
• Henri E. L. Moereels · Ekeren, BE
• Michael Joseph Kukla · Masontown, US
• Donald Ludovici · Quakertown, US

Key dates

• Filing date: Nov 15, 2001
• Grant date: Feb 22, 2005
• Expiry date: Jan 16, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and …