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    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use
    4.
    发明授权
    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use 失效
    吡咯衍生物和含有它们的药物组合物和药理学方法

    公开(公告)号：US4960779A

    公开(公告)日：1990-10-02

    申请号：US360122

    申请日：1989-06-01

    申请人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    发明人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    IPC分类号： C07D209/46 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D221/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： Pyrrole derivatives of formula (I): ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system, Het.dbd.naphthyridinyl, pyridyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3, Y.dbd.CO, C.dbd.NOH or CHOH and R.dbd.(3 to 10 C) alkenyl, alkyl which is unsubstituted or substituted with OH, alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, piperazinyl, piperidyl, 1-azetidinyl, morpholino, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, pyrrolidinocarbonyl, phenyl, pyridyl, 1-imidazolyl or alternatively R.dbd.2- or 3-pyrrolididnyl, 2-, 3- or 4-piperidyl, (3 to 6 C) cycloalkyl or phenyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, the said alkyl radicals and portions containing, except where specifically stated, 1 to 10 C, and the piperazinyl, piperidino, piperidyl, pyrrolidinyl, azetidinyl radicals being unsubstituted or substituted at any position by alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and their salts and optical isomers are useful as anxiolytics.

    摘要翻译： 式（I）的吡咯衍生物：其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6,7 - 四氢-5H- [1,4]氧硫杂环[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二噻唑并[2,3-c]吡咯环体系， Het =未被取代或被卤素取代的（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基或CF3，Y = CO，C = NOH或CHOH的萘啶基，吡啶基或喹啉 （3〜6）环烷基，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基，哌嗪基，哌啶基，1-氮杂环丁烷基，吗啉代，吗啉代， 吡咯烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，吡咯烷基羰基，苯基，吡啶基，1-咪唑基或R = 2-或3-吡咯烷二基，2-，3-或4-哌啶基 6 C）未被取代或被卤素取代的环烷基或苯基，（1-4C）烷基，（1-4C） 烷氧基，（1〜4个C）烷硫基，所述烷基及其部分除特别说明为1-10个以外，其中哌嗪基，哌啶子基，哌啶基，吡咯烷基，氮杂环丁烷基在任意位置未被取代或被烷基取代， 烷基羰基，苄基或羟基烷基，或者可以与环的氮原子形成内酰胺基，其盐和旋光异构体可用作抗焦虑剂。