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    Compound possessing affinity at 5ht1-type receptors and use thereof in therapy of cns disorders
    5.
    发明申请
    Compound possessing affinity at 5ht1-type receptors and use thereof in therapy of cns disorders 审中-公开
    在5ht1型受体具有亲和力的化合物及其在治疗cns病症中的用途

    公开(公告)号：US20050107410A1

    公开(公告)日：2005-05-19

    申请号：US10503833

    申请日：2003-02-17

    申请人： Paul Smith ,  Kevin Thewlis ,  Antonio Vong ,  Simon Ward

    发明人： Paul Smith ,  Kevin Thewlis ,  Antonio Vong ,  Simon Ward

    IPC分类号： A61K31/4709 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/04 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P15/00 ,  A61P15/06 ,  A61P15/10 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/36 ,  A61P29/00 ,  A61P43/00 ,  C07D215/20 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D41/02 ,  C07D43/02

    CPC分类号： C07D401/12 ,  C07D215/20 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    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 CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4; and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.

    摘要翻译： 公开了式（I）化合物及其药学上可接受的盐：其中：A为任选取代的苯基，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是碳，Y是CH并且是双键; 或X是CH，Y是CH 2或氧并且是单键; 或X是氮，Y是CH 2，并且是单键; 是卤素，羟基，氰基，C 1-6烷基，卤代C 1-6烷基或C 1-6烷氧基; a是0，1，2，3或4; R2和R3与它们所连接的氮原子一起形成硝基或任选取代的3至7元杂环基，或R 2和R 3独立地是氢，芳酰基，C 1-6 烷基，C 1-6烷酰基，氟代C 1-6烷酰基，C 1-6烷基磺酰基，氟代C 1-6烷基， 烷基磺酰基，氨基甲酰基，C 1-6烷基氨基甲酰基，芳基C 1-6 - 烷基或基团CO（CH 2）2 bRR 4 R 5，其中b 是1，2，3或4; 并且R 4和R 5独立地为氢或C 1-6烷基，或者R 4和R 5与它们连接的氮原子一起形成任选取代的3至7元杂环基的一部分。 还公开了制备化合物的方法和化合物在治疗中的用途，特别是CNS障碍如抑郁和焦虑。