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1. 发明申请

WO1993018002A1 QUATERNARY SALTS OF 4-SUBSTITUTED PIPERIDINES, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：四取代哌嗪的季铵盐，其制备方法和含有其的药物组合物
公开(公告)号：WO1993018002A1
公开(公告)日：1993-09-16
申请号：PCT/FR1993000215
申请日：1993-03-03
申请人： ELF SANOFI
发明人： ELF SANOFI , EMONDS-ALT, Xavier , PROIETTO, Vincenzo , VAN BROECK, Didier , BRELIERE, Jean-Claude
IPC分类号： C07D211/14
CPC分类号： C07D401/06 , C07D211/14 , C07D211/44 , C07D211/48 , C07D211/52 , C07D211/58 , C07D409/12
摘要： Quaternary ammonium salts of formula (I), wherein J is a Ar-CXX'-CX" group or a Ar-(CH2)xCX1 group wherein Ar is optionally substituted phenyl, cycloalkyl, pyridyl or thienyl; X is hydrogen; X' is hydrogen or combined with X" below to form a carbon-carbon bond, or X and X' together form an oxo group; x is 0 or 1; X1 is hydrogen (x=0), hydroxyl, alkoxy, acyloxy, carboxy, carbalkoxy, cyano, carbamoylalkyl, mercapto or alkylthio; Q is an alkyl or benzyl group; A is an anion; m is 2 or 3; Ar' is optionally substituted phenyl, thienyl, benzothienyl, naphthyl or optionally N-substituted indolyl; R is hydrogen or C1-6 alkyl; T is -CO- or -CW-NH-, wherein W is an oxygen or sulphur atom; and Z is either hydrogen or M or OM when T is the -CO- group, or M when T is the -CW-NH- group; M in particular is alkyl, alpha -hydroxybenzyl, alpha -hydroxybenzylalkyl, phenylalkyl, pyridylalkyl, naphthylalkyl, pyridylthioalkyl or styryl. The salts may be used particularly in drugs for treating pathological phenomena involving the neurokinin system.
摘要翻译：式（I）的季铵盐，其中J为Ar-CXX'-CX“基或Ar-（CH2）xCX1基，其中Ar为任选取代的苯基，环烷基，吡啶基或噻吩基; X为氢; X'为氢或与X“结合形成碳 - 碳键，或X和X'一起形成氧代基; x为0或1; X 1为氢（x = 0），羟基，烷氧基，酰氧基，羧基，烷氧羰基，氰基，氨基甲酰基烷基，巯基或烷硫基; Q是烷基或苄基; A < - >是阴离子; m为2或3; Ar'是任选取代的苯基，噻吩基，苯并噻吩基，萘基或任选的N-取代的吲哚基; R是氢或C 1-6烷基; T是-CO-或-CW-NH-，其中W是氧或硫原子; 当T为-CO-基团时，Z为氢或M或OM;当T为-CW-NH-基时，Z为M; M特别是烷基，α-羟基苄基，α-羟基苄基烷基，苯基烷基，吡啶基烷基，萘基烷基，吡啶基硫代烷基或苯乙烯基。盐可以特别用于治疗涉及神经激肽系统的病理现象的药物中。

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