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41 条记录 (耗时 0.037 秒)

    D3 and 5-HT2A receptor modulators
    5.
    发明授权
    D3 and 5-HT2A receptor modulators 失效
    D3和5-HT2A受体调节剂

    公开(公告)号：US07858630B2

    公开(公告)日：2010-12-28

    申请号：US12560459

    申请日：2009-09-16

    申请人： Luca Gobbi ,  Georg Jaeschke ,  Rosa Maria Rodriguez Sarmiento ,  Lucinda Steward

    发明人： Luca Gobbi ,  Georg Jaeschke ,  Rosa Maria Rodriguez Sarmiento ,  Lucinda Steward

    IPC分类号： A61K31/496 ,  C07D261/20 ,  C07D413/12

    CPC分类号： C07D261/20 ,  C07D413/12 ,  C07D493/08

    摘要： The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for 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-HT2a and dopamine D3 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.

    摘要翻译： 本发明提供了通式（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，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。

    Substituted triazole derivatives
    7.
    发明申请
    Substituted triazole derivatives 失效
    取代的三唑衍生物

    公开(公告)号：US20070021475A1

    公开(公告)日：2007-01-25

    申请号：US11488837

    申请日：2006-07-18

    申请人： Luca Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    发明人： Luca Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    IPC分类号： A61K31/4192 ,  C07D249/16 ,  C07D407/02

    CPC分类号： C07D249/04 ,  C07D403/12

    摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the specification and to pharmaceutically suitable acid addition salts thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are selective allosteric positive modulators of the human NK-3 receptor for the treatment of anxiety, depression, bipolar disorders, Parkinson's disease, schizophrenia and pain.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2和R 3 3如说明书中所定义，并且与药学上 其合适的酸加成盐。 本发明包括所有的异构异构体形式，包括式（I）化合物的单独非对映异构体和对映异构体，以及其外消旋和非外消旋混合物。 已经发现，本发明化合物是用于治疗焦虑，抑郁，双相情感障碍，帕金森病，精神分裂症和疼痛的人NK-3受体的选择性变构的阳性调节剂。

    Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
    10.
    发明授权
    Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors 失效
    苯甲酰哌啶衍生物作为5-HT2A和D3受体的双重调节剂

    公开(公告)号：US08097637B2

    公开(公告)日：2012-01-17

    申请号：US12184272

    申请日：2008-08-01

    申请人： Luca Gobbi ,  Georg Jaeschke ,  Rosa Maria Rodriguez Sarmiento ,  Lucinda Steward

    发明人： Luca Gobbi ,  Georg Jaeschke ,  Rosa Maria Rodriguez Sarmiento ,  Lucinda Steward

    IPC分类号： A61K31/445 ,  C07D211/32

    CPC分类号： C07D211/32 ,  C07D405/12

    摘要： The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1和A如说明书中定义为5-羟色胺5-HT2a和多巴胺D3受体的双重调节剂，其制备方法，含有它们的药物组合物及其作为药物的用途。 通式（I）的化合物对多巴胺D3和5-羟色胺（5-羟色胺，5-HT）5-HT 2A受体具有高亲和力，并且有效治疗精神病，以及其它疾病如抑郁和焦虑， 药物依赖，痴呆和记忆障碍。