Jérôme Emile Georges Guillemont,Patrice Palandjian,Marc René de Jonge,Lucien Maria Henricus Koymans,Hendrik Maarten Vinkers,Frederik Frans Desiré Daeyaert,Jan Heeres,Koen Jeanne Alfons Van Aken,Paulus
申请号：
US15406918
公开号：
US20170121292A1
申请日:
2017.01.16
申请国别(地区):
US
年份:
2017
代理人:
摘要：
This invention concerns HIV replication inhibitors of formulathe 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.
