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Piperidyl - urea, - thiourea and - guanidine derivatives, and intermediates therefor, processes for preparing them and pharmaceutical compositions containing the derivatives.

机译:哌啶基-脲,-硫脲和-胍衍生物及其中间体,其制备方法和含有该衍生物的药物组合物。

摘要

The invention concerns compounds of formula IMAGE (I) and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula IMAGE (Ia) in which Q is O,S,-CR7=CR8-, -N=CR8- and -N=N- R4, R5 and R6, and R7 and R8 when present, each represent hydrogen or defined substituents and additionally either R4 and R5 when adjacent or R6 and R8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms R1, R2, R3 and R9 are each hydrogen or a lower alkyl group n is 0 or 1 X is =O, =S or =NH Y is -O- or a direct bond and Z is -CO- or -CH2- with the proviso that when Ar is unsubstituted phenyl and R9 is hydrogen then Y is -O-. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants. Processes for preparing the compounds and pharmaceutical compositions containing them are disclosed.
机译:本发明涉及式(I)的化合物及其酸加成盐和季铵盐,其中虚线表示任选的键,Ar表示式(Ia)的环系统,其中Q为O,S R 4,R 5和R 6以及R 7和R 8(当存在时)各自代表氢或定义的取代基,并且另外R 4和R 5(当相邻时)或R 6和R 8(当存在时)。相邻的以及与其连接的碳原子一起还代表稠合的五或六元碳环或杂环,其任选地带有一个或多个定义的取代基R是任选取代的芳基或杂芳基或含有5至7个碳原子的环烷基R 1,R 2,R 3和R 9各自为氢或低级烷基,n为0或1 X为= O,= S或= NH Y为-O-或直接键且Z为-CO-或-CH2-条件是当Ar为未取代的苯基且R 9为氢时,Y为-O-。式I化合物表现出精神活性并且可用作抗抑郁药。公开了制备化合物和包含它们的药物组合物的方法。

著录项

  • 公开/公告号ES8302656A1

    专利类型

  • 公开/公告日1983-02-01

    原文格式PDF

  • 申请/专利权人 JOHN WYETH & BROTHER LIMITED;

    申请/专利号ES19820509163

  • 发明设计人

    申请日1982-01-29

  • 分类号C07D211/58;A61K31/445;

  • 国家 ES

  • 入库时间 2022-08-22 10:45:48

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