公开(公告)号：EP1419152B1

公开(公告)日：2011-07-27

申请号：EP02764839.3

申请日：2002-08-09

申请人： Janssen Pharmaceutica NV

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

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

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

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(公告)号：EP1597242B1

公开(公告)日：2008-07-23

申请号：EP04708367.0

申请日：2004-02-05

申请人： Janssen Pharmaceutica NV

发明人： LEWI, Paulus Joannes ,  JANSSEN, Paul Adriaan, Jan ,  DE JONGE, Marc René ,  KOYMANS, Lucien Maria Henricus ,  VINKERS, Hendrik Maarten ,  DAEYAERT, Frederik Frans Desiré ,  HEERES, Jan ,  LEENDERS, Ruben Gerardus George ,  HOORNAERT, Georges Joseph Cornelius ,  KILONDA, Amuri ,  LUDOVICI, Donald W., Janssen Pharmaceutica Inc.

IPC分类号： C07D253/06 ,  A61K31/53

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D253/075

摘要： The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

公开(公告)号：EP1442019B8

公开(公告)日：2013-10-30

申请号：EP02790304.6

申请日：2002-10-29

申请人： Janssen Pharmaceutica NV

发明人： FREYNE, Eddy Jean Edgard ,  BUIJNSTERS, Peter Jacobus Johannes Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner Constant Johan ,  LACRAMPE, Jean Fernand Armand, Janssen-Cilag ,  JANSSEN, Paul Adriaan Jan (deceased) ,  LEWI, Paulus Joannes ,  HEERES, Jan ,  DE JONGE, Marc René ,  KOYMANS, Lucien Maria Henricus ,  DAEYAERT, Frederik Frans Desire ,  KUKLA, Michael Joseph ,  GEERTS, Hugo, Alfons, Gabriel ,  NUYDENS, Rony Maria ,  MERCKEN, Marc Hubert ,  LUDOVICI, Donald William, Janssen Pharmac. Inc. ,  JANSSEN, Paul, Peter, Maria ,  JANSSEN, Graziella, Maria, Constantina ,  JANSSEN, Jasmin, Josee, Werner ,  JANSSEN, Maroussia, Godelieve, Frank ,  JANSSEN, Herwig, Josephus, Margareta ,  ARTS, Theodora, Joanna, Francisca

IPC分类号： C07D213/82 ,  C07D239/42 ,  C07D413/12 ,  C07D413/14 ,  C07D407/12 ,  C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  A61K31/505 ,  A61P3/10 ,  A61P25/28

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12