HIV inhibiting pyrimidines derivatives
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, pir...
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Main Authors | , , , , , , , , , |
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Format | Patent |
Language | English |
Published |
24.10.2006
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Subjects | |
Online Access | Get full text |
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Summary: | 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 |
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Bibliography: | Application Number: US20040485636 |