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    HIV REPLICATION INHIBITING PYRIMIDINES
    7.
    发明公开
    HIV REPLICATION INHIBITING PYRIMIDINES 审中-公开

    公开(公告)号：EP3808743A1

    公开(公告)日：2021-04-21

    申请号：EP20165399.5

    申请日：2002-08-09

    申请人： Janssen Pharmaceutica NV

    发明人： Guillemont, Jerôme, Emile, Georges ,  Janssen, Paul, Adriaan, Jan ,  Palandijan, Patrice ,  de Jonge, Marc, René ,  Koymans, Lucien, Maria, Henricus ,  Vinkers, Hendrik, Maarten ,  Daeyaert, Frederik, Frans, Desiré ,  Heeres, Jan ,  Van Aken, Koen, Jeanne, Alfons ,  Lewi, Paulus, Joannes

    IPC分类号： C07D403/12 ,  C07D401/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D403/14 ,  C07D233/96 ,  A61K31/505 ,  C07D239/46 ,  C07D239/48 ,  C07C211/00

    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 l - 6 alkyloxyC l - 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)-NER 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, polyhaloC 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.