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    2-AMINOQUINOLINES AS 5-HT5A RECEPTOR ANTAGONISTS
    3.
    发明申请
    2-AMINOQUINOLINES AS 5-HT5A RECEPTOR ANTAGONISTS 审中-公开
    2-AMINOQUINOLINES作为5-HT5A受体拮抗剂

    公开(公告)号：WO2009112395A1

    公开(公告)日：2009-09-17

    申请号：PCT/EP2009/052484

    申请日：2009-03-03

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KOLCZEWSKI, Sabine ,  RIEMER, Claus ,  ROCHE, Olivier ,  STEWARD, Lucinda ,  WICHMANN, Juergen ,  WOLTERING, Thomas

    Inventor： KOLCZEWSKI, Sabine ,  RIEMER, Claus ,  ROCHE, Olivier ,  STEWARD, Lucinda ,  WICHMANN, Juergen ,  WOLTERING, Thomas

    IPC: A61P3/06 ,  A61P25/00 ,  A61K31/4709 ,  C07D215/38 ,  C07D405/12

    CPC classification number: C07D405/12 ,  C07D215/38 ,  C07D491/08

    Abstract: The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general formula (I) wherein R and R are as described herein.

    Abstract translation: 本发明涉及作为5-HT5A受体拮抗剂的2-氨基喹啉衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，病症 饮食行为，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠道疾病。 特别地，本发明涉及通式（I）的化合物，其中R和R如本文所述。

    (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR
    7.
    发明申请
    (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR 审中-公开
    （3,4-DIHYDRO-喹唑啉-2-基） - （2-氰基乙基） - 胺在5-HT受体上具有活性

    公开(公告)号：WO2006117305A1

    公开(公告)日：2006-11-09

    申请号：PCT/EP2006/061779

    申请日：2006-04-24

    Applicant: F. HOFFMANN-LA ROCHE AG ,  ALANINE, Alexander ,  GOBBI, Luca Claudio ,  KOLCZEWSKI, Sabine ,  LUEBBERS, Thomas ,  PETERS, Jens-Uwe ,  STEWARD, Lucinda

    Inventor： ALANINE, Alexander ,  GOBBI, Luca Claudio ,  KOLCZEWSKI, Sabine ,  LUEBBERS, Thomas ,  PETERS, Jens-Uwe ,  STEWARD, Lucinda

    IPC: C07D239/84 ,  C07D409/04 ,  C07D413/04 ,  A61K31/517 ,  A61P25/24 ,  A61P25/18

    CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D409/04 ,  C07D413/04

    Abstract: The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R 1 and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R 2 is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R 3 is hydrogen, lower alkyl, phenyl, benzyl, lower alkenyl, lower alkoxy, phenyloxy, benzyloxy, S-lower alkyl, halogen, CN, lower alkyl substituted by halogen or O-lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl, aryl is phenyl or naphthyl; n is 1, 2 or 3; m is 1 or 2; and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. It has been found that the compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the manufacture of medicaments for the treatment of certain CNS disorders.

    Abstract translation: 本发明涉及其中R 1为氢，低级烷基，低级烷氧基，卤素或被卤素取代的低级烷基的式（I）化合物; R是氢或卤素; 或R 1和R 2与它们所连接的碳原子一起-CH = CH-CH = CH-; R 2是氢，低级烷基，任选被卤素取代的苯基，或者是杂芳基，任选被低级烷基取代; R 3是氢，低级烷基，苯基，苄基，低级烯基，低级烷氧基，苯氧基，苄氧基，S-低级烷基，卤素，CN，被卤素取代的低级烷基或被 卤素; R 4是氢或低级烷基，芳基是苯基或萘基; n为1,2或3; m为1或2; 和其药学上可接受的酸加成盐和互变异构体。 已经发现式I化合物对5-HT5A受体具有良好的活性。 因此，本发明提供式I化合物或其药学上可接受的盐在制备用于治疗某些CNS疾病的药物中的用途。

    PIPERAZINE D3 AND 5-HT2A RECEPTOR MODULATORS
    9.
    发明申请
    PIPERAZINE D3 AND 5-HT2A RECEPTOR MODULATORS 审中-公开
    哌啶D3和5-HT2A受体调节剂

    公开(公告)号：WO2010031735A1

    公开(公告)日：2010-03-25

    申请号：PCT/EP2009/061788

    申请日：2009-09-11

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GOBBI, Luca ,  JAESCHKE, Georg ,  RODRIGUEZ SARMIENTO, Rosa Maria ,  STEWARD, Lucinda

    Inventor： GOBBI, Luca ,  JAESCHKE, Georg ,  RODRIGUEZ SARMIENTO, Rosa Maria ,  STEWARD, Lucinda

    IPC: C07D261/20 ,  C07D413/12 ,  C07D493/08 ,  A61K31/496 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30

    CPC classification number: C07D261/20 ,  C07D413/12 ,  C07D493/08

    Abstract: The present invention relates to compounds of the general formula (I) (I) wherein X, n and R 1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, as well as their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT 2a and dopamine D 3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.

    Abstract translation: 本发明涉及通式（I）（I）的化合物，其中X，n和R 1如本文所述，以及其药学上可接受的盐和酯，以及它们的制备，含有它们的药物组合物及其用途 作为药物。 本发明的活性化合物是5-羟色胺5-HT2a和多巴胺D3受体的双重调节剂，可用于治疗和/或预防认知障碍，药物成瘾，抑郁，焦虑，药物依赖，痴呆，记忆障碍，精神病性 包括精神分裂症，分裂情感障碍，双相性精神障碍，躁狂症，精神病性抑郁症和包含偏执狂和妄想的精神病的疾病。

    6-SUBSTITUTED BENZOXAZINES
    10.
    发明申请
    6-SUBSTITUTED BENZOXAZINES 审中-公开
    6-取代苯并噻唑

    公开(公告)号：WO2010026110A2

    公开(公告)日：2010-03-11

    申请号：PCT/EP2009/061152

    申请日：2009-08-28

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KOLCZEWSKI, Sabine ,  ROCHE, Olivier ,  STEWARD, Lucinda ,  WICHMANN, Juergen ,  WOLTERING, Thomas

    Inventor： KOLCZEWSKI, Sabine ,  ROCHE, Olivier ,  STEWARD, Lucinda ,  WICHMANN, Juergen ,  WOLTERING, Thomas

    IPC: C07D265/18

    CPC classification number: C07D265/18 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D498/08

    Abstract: The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I), wherein X, Y, R 1 and R 2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are 5-HT 5A receptor antagonists, useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

    Abstract translation: 本发明涉及式（I）的6-取代苯并恶嗪衍生物，其中X，Y，R 1和R 2如本文所述，以及它们的制备，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物是可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，惊恐障碍，广场恐怖症，社交恐惧症，强迫症，强迫症，创伤后应激障碍，疼痛， 记忆障碍，痴呆，饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍，帕金森病，精神病或胃肠疾病。

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