HIV REPLICATION INHIBITING PYRIMIDINES

• Main Authors: Heeres Jan, Vinkers Hendrik Maarten, Daeyaert Frederik Frans Desiré, Palandjian Patrice, Koymans Lucien Maria Henricus, Van Aken Koen Jeanne Alfons, Janssen Paul Adriaan Jan, de Jonge Marc René, Lewi Paulus Joannes, Guillemont Jérôme Emile Georges
• Format: Patent
• Language: English
• Published: 09.11.2017
• 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

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=b4- represents phenyl, 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, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; 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)NHNH2, -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- 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; 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.