TW200628155A - HIV replication inhibiting pyrimidines - Google Patents

Abstract

This invention concerns HIV replication inhibitors of formula, 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; mis 1 to 4; R1 is hydrogen; aryl; formyl; Cl-6alkylcarbonyl; C1-6alkyl; C1-6galkyloxycarbonyl; substituted Cl-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted Cl-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(=0)NHNH2, -NHC(=0)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 Ci-6aikyloxyC1-6alkyl; 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, Cl-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.