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    N-ARYL ACETYL CYCLIC AMINE DERIVATIVES AS OREXIN ANTAGONISTS
    3.
    发明申请
    N-ARYL ACETYL CYCLIC AMINE DERIVATIVES AS OREXIN ANTAGONISTS 审中-公开
    N-ARYL ACETYL循环胺衍生物作为OREXIN ANTAGONISTS

    公开(公告)号：WO2004041791A1

    公开(公告)日：2004-05-21

    申请号：PCT/EP2003/012407

    申请日：2003-11-04

    Applicant: GLAXO GROUP LIMITED ,  CHAN, Wai, Ngor ,  NASH, David, John ,  PORTER, Roderick, Alan ,  STEAD, Rachel, Elizabeth, Anne

    Inventor： CHAN, Wai, Ngor ,  NASH, David, John ,  PORTER, Roderick, Alan ,  STEAD, Rachel, Elizabeth, Anne

    IPC: C07D241/44

    CPC classification number: C07D401/12 ,  C07D405/14

    Abstract: The present invention provides N -aryl acetyl cyclic amine derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors. In particular, theses compounds are of potential use in the treatment of obesity, including obesity observed in Type 2 (non-insulin-dependent) diabetes patients, and/or sleep disorders. Additionally these compounds are useful in the treatment of stroke, particularly ischemic or haemorrhagic stroke, and/or blocking the emetic response, i.e. useful in the treatment of nausea and vomiting. (I) wherein: Y represents a bond, oxygen, NQ or a group (CH 2 ) n , wherein n represents 1, 2 or 3 m is 0 or 1; X is NR, wherein R is H or (C 1-4 )alkyl; Q is H or (C 1-4 )alkyl; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents optionally substituted phenyl, an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S, or an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 4 heteroatoms selected from N, O and S; R 1 and R 2 independently represent hydrogen, optionally substituted amino, optionally substituted (C 1-6 )alkyl or optionally substituted phenyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供作为人食欲素受体的非肽拮抗剂的N-芳基乙酰基环胺衍生物，特别是食欲素-1受体。 特别地，这些化合物可用于治疗肥胖症，包括在2型（非胰岛素依赖性）糖尿病患者中观察到的肥胖症和/或睡眠障碍。 另外，这些化合物可用于治疗中风，特别是缺血性或出血性中风，和/或阻断催吐反应，即可用于治疗恶心和呕吐。 （I）其中：Y表示键，氧，NQ或基团（CH 2）n，其中n表示1,2或3m为0或1; X是NR，其中R是H或（C 1-4）烷基; Q是H或（C 1-4）烷基; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示任选取代的苯基，任选取代的含有至多4个选自N，O和S的杂原子的5-或6-元杂环基，或含有至多4个选自以下的杂原子的任选取代的双环芳族或双环杂芳族基团： N，O和S; R 1和R 2独立地表示氢，任选取代的氨基，任选取代的（C 1-6）烷基或任选取代的苯基; 或其药学上可接受的盐。

    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
    5.
    发明申请
    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    在NK3受体中具有活性的化合物及其在医学中的用途

    公开(公告)号：WO2006050991A1

    公开(公告)日：2006-05-18

    申请号：PCT/EP2005/012207

    申请日：2005-11-10

    Applicant: SMITHKLINE BEECHAM CORPORATION ,  BRADLEY, Daniel Marcus ,  PORTER, Roderick, Alan ,  SMITH, Paul William ,  STEAD, Rachel Elizabeth Anne ,  VONG, Antonio, Kuok, Keong

    Inventor： BRADLEY, Daniel Marcus ,  PORTER, Roderick, Alan ,  SMITH, Paul William ,  STEAD, Rachel Elizabeth Anne ,  VONG, Antonio, Kuok, Keong

    IPC: C07D215/52 ,  A61K31/47 ,  A61P25/18 ,  A61P25/24

    CPC classification number: C07D409/04 ,  C07D215/52

    Abstract: The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R 1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R 2 is C 1-6 alkyl or C 3-6 cycloalkyl; n is 1 or 2; R 3 is hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl; X is -(C=O)- or -SO 2 -; R 4 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 haloalkoxy, amino, monoC 1-6 alkylamino or diC 1-6 alkylamino, or R 4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy or C 1-6 haloalkoxy; R 5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK 3 receptor, compositions containing the derivatives and processes for their preparation.

    Abstract translation: 本发明还涉及式（I）化合物，其药学上可接受的盐，溶剂合物或前药：其中R 1是苯基或环己基，其任一个任选被1,2或3个卤素 原子，其原子可以相同或不同; R 2是C 1-6烷基或C 3-6环烷基; n为1或2; R 3是氢，C 1-6烷基或C 3-6环烷基; X是 - （C = O） - 或-SO 2 - 。 R 4是C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基，C C 1-6烷氧基C 1-6烷基，C 1-6卤代烷氧基，氨基，一C 1-6烷基氨基 或二C 1-6烷基氨基或R 4是杂环基或碳环基，其中任一个可以任选被一个或多个卤素C 1-6独立地取代， C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或C 1-6卤代烷氧基; R 5是苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代; y为0,1或2; 其中当y为1或2时，Y为卤素原子，当y为2时，卤素原子可以相同或不同。 还公开了这些化合物在治疗由活化NK 3受体介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

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