HIV INHIBITING PYRIMIDINES DERIVATIVES

• Main Authors: DE JONGE, MARC RENE, VINKERS, HENDRIK MAARTEN, JANSSEN, PAUL ADRIAAN JAN, PALANDJIAN, PATRICE, DAEYAERT, FREDERIK FRANS DESIRE, HEERES, JAN, KOYMANS, LUCIEN MARIA HENRICUS, GUILLEMONT, JEROME EMILE GEORGES, VAN AKEN, KOEN JEANNE ALFONS, LEWI, PAULUS JOANNES
• Format: Patent
• Language: English; French
• Published: 27.02.2003
• Edition: 7
• 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 amine s and the stereochemically isomeric forms thereof, wherein the ring containing - a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formy l; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C 1- 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 heterocycle; X1 is -NR5-, -NH-NH-, -N= N- , -O-, -C(=O)-, C1-4alkanediyl, -CHOH-, -S-, -S(=O)p-, -X2-C1-4alkanediyl- o r - 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; C1- 6alkyl substituted with hydroxy and a second substituent; -C(=N-O-R8)-C1- 4alkyl; R7; or -X3-R7; R4 ishalo, 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.