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：
US15963352
公开号：
US10370340B2
申请日:
2018.04.26
申请国别(地区):
US
年份:
2019
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, am
