公开(公告)号：EP1192122A1

公开(公告)日：2002-04-03

申请号：EP00940462.5

申请日：2000-06-08

申请人： SANOFI-SYNTHELABO

发明人： BOIGEGRAIN, Robert ,  BOURRIE, Bernard ,  BOURRIE, Martine ,  CASELLAS, Pierre ,  HERBERT, Jean, Marc ,  LAIR, Pierre ,  NISATO, Dino ,  PAUL, Raymond ,  VERNIERES, Jean, Claude

IPC分类号： C07C211/35 ,  A61K31/135 ,  A61P37/00 ,  A61P35/00 ,  A61P9/00

CPC分类号： C07C211/40 ,  C07C2601/14 ,  C07C2603/74

摘要： The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in Claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.

摘要翻译： 本发明涉及式（I）化合物worin A，X，Y，N，R 1，R 2和R 3如claimsoft 1中定义所述化合物特异性地结合于σ受体的特别是那些外周神经系统的。

公开(公告)号：EP1226137B1

公开(公告)日：2004-07-21

申请号：EP00969646.9

申请日：2000-10-19

申请人： SANOFI-SYNTHELABO

发明人： BARONI, Marco ,  BOURRIE, Bernard ,  CARDAMONE, Rosanna ,  CASELLAS, Pierre ,  GUZZI, Umberto

IPC分类号： C07D401/06 ,  A61K31/4709 ,  A61K31/4725 ,  A61P9/00 ,  C07D401/14 ,  C07D217/02 ,  C07D215/14

CPC分类号： C07D401/06 ,  A43B7/125 ,  A43B9/02 ,  B29C2045/14844 ,  B29D35/0045 ,  B29D35/06 ,  B29D35/062 ,  B29D35/122 ,  B29D35/128 ,  B29D35/142 ,  C07D215/14 ,  C07D217/02 ,  C07D401/14

摘要： The invention concerns compounds of formula (I) wherein: X represents N or CH; R1 represents a hydrogen or halogen atom, or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents a group of formula (a) or (b) wherein: R4 represents a hydrogen or halogen atom, a C1-C4 alkyl group, a CF3 group, an amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino; R5 represents a hydrogen or halogen atom, a (C1-C4)alkoxy group, a (C1-C4)alkyl group or a CF3 group; R6 represents a hydrogen atom, a (C1-C4)alkyl group or a (C1-C4)alkoxy group; and their salts or solvates, pharmaceutical compositions containing them, a method for preparing them and the synthesis intermediates in said method.

摘要翻译： 本发明涉及式（I）的化合物，其中：X代表N或CH; R1代表氢或卤素原子或CF3基团; R2和R3独立地表示氢原子或甲基; n是0或1; A表示式（a）或（b）的基团，其中：R 4表示氢或卤素原子，C 1 -C 4烷基，CF 3基，氨基，单（C 1 -C 4）烷基氨基，二 ）烷基氨基; R5代表氢或卤素原子，（C1-C4）烷氧基，（C1-C4）烷基或CF3基团; R6代表氢原子，（C1-C4）烷基或（C1-C4）烷氧基; 及其盐或溶剂化物，含有它们的药物组合物，其制备方法和所述方法中的合成中间体。

公开(公告)号：EP1385513A1

公开(公告)日：2004-02-04

申请号：EP02735502.3

申请日：2002-04-26

申请人： SANOFI-SYNTHELABO

发明人： BOURRIE, Bernard ,  CASELLAS, Pierre ,  DEROCQ, Jean-Marie

IPC分类号： A61K31/437 ,  A61P35/00 ,  A61K45/06

CPC分类号： A61K31/437 ,  A61K31/435 ,  A61K45/06 ,  A61K2300/00

摘要： The invention concerns the combination of compounds of formula (I) with several anticancer agents.

公开(公告)号：EP0979079A1

公开(公告)日：2000-02-16

申请号：EP98921552.0

申请日：1998-04-17

申请人： SANOFI-SYNTHELABO

发明人： BOURRIE, Bernard ,  CASELLAS, Pierre ,  MAFFRAND, Jean-Pierre

IPC分类号： A61K31/44

CPC分类号： A61K31/444 ,  A61K31/4418

摘要： The invention concerns the use of tetrahydropyridine derivatives of formula (I) in which: R1 represents a halogen or a CF3, (C1-C4) alkyl or (C1-C4)alkoxy group; Y represents a nitrogen atom or a CH group; Z' and Z' represent each hydrogen or a (C1-C3) alkyl group, or one represents hydrogen and the other a hydroxy group, or both together represent an oxo group; Z represents a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being (a) a (C1-C6)alkyl, (C1-C6)alkoxy (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)-alkoxycarbonyl(C1-C6) alkoxy group; (b) a group selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl group, said group capable of being substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino, mono- or di-(C1-C4)alkylamino; or (c) a group selected among a phenyl, phenoxy, phenylamino, N-(C1-C3)alkylphenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl or styryl group, said group can be mono- or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifuoromethyl group and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; a 1-naphthyl or 2-naphthyl radical, substituted in positions 5, 6, 7 and/or 8 by one or two hydroxyl groups, one or two (C1-C4) alkoxy groups, or a 6,7-methylenedioxy group; or Z' is hydrogen and Z and Z' represent, each independently, a phenyl group non-substituted or mono-, di- or trisubstituted; or one of its pharmaceutically acceptable salts or solvates, for preparing pharmaceutical compositions to fight against diseases causing demyelination.