HIV inhibiting pyrimidines derivatives

• Main Authors: LEWI PAULUS JOANNES, VINKERS HENDRIK MAARTEN, DAEYAERT FREDERIK FRANS DESIRE, HEERES JAN, KOYMANS LUCIEN MARIA HENRICUS, PALANDJIAN PATRICE, ARTS, LEGAL REPRESENTATIVE FRANK XAVIER JOSEF HERWIG, DE JONGE MARC RENE, GUILLEMONT JEROME EMILE GEORGES, VAN AKEN KOEN JEANNE ALFONS
• Format: Patent
• Language: English
• Published: 24.10.2006
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4-and -b1=b2-b3=b4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(-O)pR6, -NH-S(-O)pR6, -C(-O)R6, -NHC(-O)H, -C(-O)NHNH?2?, -NHC(-O)R6, -C(-NH)R6 or a 5-membered hetrocycl; X1 is -NR5-, -NH-NH-, -N-N-, -O-, -C(-O)-, C1-4alkanediyl, -CHOH-, -S-, -S(-O)p-, -X2-C1-4alkanediyl- or -C1-4alkanediyl-X2-; R3 is NHR13, NR13R14; -C(-O)-NHR13; -C(-O)-NR13R14; -C(-O)-R15; -CH-N-NH-C(-O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; substituted C2-6alkylenyl; C1-6alkyl substituted with hydroxy and a second substituent; -C(-N-O-R8)-C1-4alkyl; R7; or -X3-R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them