发明授权
- 专利标题: HIV INHIBITING PYRIMIDINES DERIVATIVES
- 专利标题(中): 抑制HIV嘧啶类衍生物
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申请号: EP02764839.3申请日: 2002-08-09
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公开(公告)号: EP1419152B1公开(公告)日: 2011-07-27
- 发明人: GUILLEMONT, Jérôme Emile Georges , PALANDJIAN, 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 , JANSSEN, Paul Adriaan Jan
- 申请人: Janssen Pharmaceutica NV
- 申请人地址: Turnhoutseweg 30 2340 Beerse BE
- 专利权人: Janssen Pharmaceutica NV
- 当前专利权人: Janssen Pharmaceutica NV
- 当前专利权人地址: Turnhoutseweg 30 2340 Beerse BE
- 优先权: EP01203090 20010813; EP02077748 20020610
- 国际公布: WO2003016306 20030227
- 主分类号: C07D403/12
- 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 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.
公开/授权文献
- EP1419152A1 HIV INHIBITING PYRIMIDINES DERIVATIVES 公开/授权日:2004-05-19
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