GUILLEMONT JEROME EMILE GEORGES,PALANDJIAN PATRICE,DE JONGE,KOYMANS LUCIEN MARIA HENRICUS,VINKERS HENDRIK MAARTEN,DAEYAERT FREDERIK FRANS DESIRE,HEERES JAN,VAN AKEN,LEWI PAULUS JOANNES,JANSSEN PAUL AD
申请号：
HU0401346
公开号：
HU230192B1
申请日:
2002.08.09
申请国别(地区):
HU
年份:
2015
代理人:
摘要：
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 -a 1 =a 2 -a 3 =a 4 - and -b 1 =b 2 -b 3 =b 4 - represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl；n is 0 to 5； m is 1 to 4； R 1 is hydrogen； aryl； formyl； C 1-6 alkylcarbonyl； C 1-6 alkyl； C 1-6 alkyloxycarbonyl； substituted C 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyloxy； substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl； R 2 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, - S(=O) p R 6 , -NH-S(=O) p R 6 , -C(=O)R 6 , -NHC(=O)H, -C(=O)NHNH 2 , -NHC(=O)R 6 -C(=NH)R 6 or a 5-membered heterocycle； X 1 is -NR 5 -, -NH-NH-, -N=N-, -O-, -C(=O)-, C 1-4 alkanediyl, -CHOH-, -S-, -S(=O) p -, -X 2 -C 1-4 alkanediyl- or -C 1-4 alkanediyl-X 2 -； R 3 is NHR 13 ； NR 13 R 14 ； -C(=O)-NHR 13 ； -C(=O)-NR 13 R 14 ； -C(=O)-R 15 ； -CH=N-NH-C(=O)-R 16 ； substituted C 1-6 alkyl； optionally substituted C 1-6 alkyloxyC 1-6 alkyl； substituted C 2-6 alkenyl； substituted C 2-6 alkynyl； C 1-6 alkyl substituted with hydroxy and a second substituent； -C(=N-O-R 8 )-C 1-4 alkyl； R 7 ； or -X 3 -R 7 ； R 4 is halo, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, polyhaloC 1-6 alkyl, polyhatoC 1-6 alkyloxy, aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyl, formyl, amino, mono- or di(C 1-4 alkyl)amino； their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
