首页> 外国专利> HETEROCYCLYLMETHYLPIPERIDINES AND -PIPERAZINES POSSESSING AFFINITY AT 5HT-1 TYPE RECEPTORS

HETEROCYCLYLMETHYLPIPERIDINES AND -PIPERAZINES POSSESSING AFFINITY AT 5HT-1 TYPE RECEPTORS

机译:5 HT-1型受体的杂环甲基哌啶和-哌嗪具有亲和力

摘要

Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CHSUB2 /SUBor oxygen and is a single bond; or X is nitrogen, Y is CHSUB2 /SUBand is a single bond; R 1 is halogen, cyano, or CSUB1-6 /SUBalkoxy; a is 0,1, 2 or 3 ; b is 0 or 1 ; R 2 is hydrogen, CSUB1-6 /SUBalkyl, CSUB1-6 /SUBalkanoyl, fluoroCSUB1-6 /SUBalkanoyl, CSUB1-6 /SUBalkylsulfonyl, fluoroCSUB1-6 /SUBalkylsulfonyl, carbamoyl, CSUB1-6 /SUBalkylcarbamoyl or arylCSUB1-6 /SUBalkyl; and R 3 , together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.
机译:公开了式(I)的化合物及其药学上可接受的盐:其中:A是任选取代的苯基,萘基,吲哚基,喹啉基,喹唑啉基,吲唑基,异喹啉基或苯并呋喃基; X为碳,Y为CH且为双键;或X为CH,Y为CH 2 或氧且为单键;或或X为氮,Y为CH 2 且为单键;或R 1是卤素,氰基或C 1-6 烷氧基; a是0,1、​​2或3; b为0或1; R 2是氢,C 1-6 烷基,C 1-6 烷酰基,氟C 1-6 烷酰基,C 1- 6 烷基磺酰基,氟代C 1-6 烷基磺酰基,氨基甲酰基,C 1-6 烷基氨基甲酰基或芳基C 1-6 烷基; R 3和与其相连的氮原子一起形成稠合到苯环上的任选取代的5至7元杂环基。还公开了所述化合物的制备方法和所述化合物在治疗中的用途,特别是用于中枢神经系统疾病例如抑郁或焦虑的治疗中。

著录项

  • 公开/公告号EP1480974A1

    专利类型

  • 公开/公告日2004-12-01

    原文格式PDF

  • 申请/专利权人 GLAXO GROUP LIMITED;

    申请/专利号EP20030704659

  • 发明设计人 WARD SIMON EGLAXOSMITHKLINE;

    申请日2003-02-17

  • 分类号C07D413/12;C07D401/12;C07D215/20;A61K31/47;A61K31/495;A61P25/00;

  • 国家 EP

  • 入库时间 2022-08-21 22:11:30

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