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    Novel compounds as metabotropic glutamate receptor antagonists
    3.
    发明申请
    Novel compounds as metabotropic glutamate receptor antagonists 失效
    新型化合物作为代谢型谷氨酸受体拮抗剂

    公开(公告)号：US20070072879A1

    公开(公告)日：2007-03-29

    申请号：US11524135

    申请日：2006-09-20

    申请人： Silvia McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Silvia McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.

    摘要翻译： 本发明涉及式（I）的化合物，其中A，EG，J，L，M，R 1，R 2和R 3， SUP>如说明书和权利要求中所定义。 本发明还涉及含有这些化合物的药物组合物和用于制备化合物和组合物的方法。 化合物是代谢型谷氨酸受体拮抗剂，可用于治疗各种CNS疾病。

    Pharmaceutical composition comprising an AChE inhibitor and a mGluR2 antagonist
    4.
    发明申请
    Pharmaceutical composition comprising an AChE inhibitor and a mGluR2 antagonist 有权
    包含AChE抑制剂和mGluR2拮抗剂的药物组合物

    公开(公告)号：US20050049243A1

    公开(公告)日：2005-03-03

    申请号：US10896494

    申请日：2004-07-22

    申请人： Theresa Ballard ,  Silvia McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Theresa Ballard ,  Silvia McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： A61K31/4535 ,  A61K31/473 ,  A61K31/55 ,  A61K31/551 ,  A61K31/662 ,  A61K31/7068 ,  A61K45/06 ,  A61K31/5513

    CPC分类号： A61K45/06 ,  A61K31/4535 ,  A61K31/473 ,  A61K31/55 ,  A61K31/551 ,  A61K31/662 ,  A61K31/7068 ,  A61K2300/00

    摘要： The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist) and a pharmaceutically acceptable excipient. The invention also relates to a method of treating and/or preventing acute and/or chronic neurological disorders comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said AChE inhibitor and mGluR2 antagonist as well as a kit comprising said AChE inhibitor and mGluR2 antagonist. In particular, the mGluR2 antagonist relates to the compound of formula I wherein, R1, R2, R3, X and Y are described hereinabove. The combination of the AChE inhibitor and mGluR2 antagonist is useful for treating and/or preventing chronic neurological disorders. These disorders include Alzheimer's disease and mild cognitive impairment.

    摘要翻译： 本发明涉及包含乙酰胆碱酯酶（AChE抑制剂）抑制剂和代谢型谷氨酸受体2拮抗剂（mGluR2拮抗剂）和药学上可接受的赋形剂的药物组合物。 本发明还涉及治疗和/或预防急性和/或慢性神经障碍的方法，包括向需要这种治疗和/或预防的患者施用治疗有效量的所述AChE抑制剂和mGluR2拮抗剂以及试剂盒 包括所述AChE抑制剂和mGluR2拮抗剂。 特别地，mGluR2拮抗剂涉及式I化合物，其中R 1，R 2，R 3，X和Y如上所述。 AChE抑制剂和mGluR2拮抗剂的组合可用于治疗和/或预防慢性神经障碍。 这些疾病包括阿尔茨海默病和轻度认知障碍。

    Pyrrazolo-pyrimidine derivatives
    5.
    发明申请
    Pyrrazolo-pyrimidine derivatives 失效
    吡唑并嘧啶衍生物

    公开(公告)号：US20060183756A1

    公开(公告)日：2006-08-17

    申请号：US11348105

    申请日：2006-02-06

    申请人： Silvia Gatti McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Silvia Gatti McArthur ,  Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R1 to R4 and A are as defined in the specification, a process for the manufacture thereof, their use for treating or preventing metabotropic glutamate receptors mediated disorders, their use for the preparation of medicaments for treating such disorders and pharmaceutical compositions containing said derivatives.

    摘要翻译： 本发明涉及式（I）的吡唑并嘧啶衍生物：其中R 1至R 4和A如说明书中所定义，其制备方法 ，它们用于治疗或预防代谢型谷氨酸受体介导的病症，其用于制备用于治疗这种病症的药物的用途和含有所述衍生物的药物组合物。

    Pyrazolo-pyrimidine derivatives
    6.
    发明申请
    Pyrazolo-pyrimidine derivatives 失效
    吡唑并嘧啶衍生物

    公开(公告)号：US20050282827A1

    公开(公告)日：2005-12-22

    申请号：US11156974

    申请日：2005-06-20

    申请人： Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Erwin Goetschi ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： C07D487/04 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and p are as defined in the description and to pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, to the manufacture of such compounds and compositions, and to methods of treating or preventing acute and/or chronic central nervous system disorders by administering such compounds.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， R 5和p如说明书及其药学上可接受的盐所定义，含有这些化合物的药物组合物，以及制备这些化合物和组合物，以及治疗或预防急性和/ /或通过施用这些化合物的慢性中枢神经系统疾病。

    6-substituted benzoxazines
    10.
    发明授权
    6-substituted benzoxazines 失效
    6-取代的苯并恶嗪

    公开(公告)号：US08163740B2

    公开(公告)日：2012-04-24

    申请号：US12549745

    申请日：2009-08-28

    申请人： Sabine Kolczewski ,  Olivier Roche ,  Lucinda Steward ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Sabine Kolczewski ,  Olivier Roche ,  Lucinda Steward ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： C07D265/02 ,  C07D413/04 ,  A61K31/536

    CPC分类号： C07D265/18 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D498/08

    摘要： The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) wherein X, Y, R1 and R2 are as described herein, their manufacture, and pharmaceutical compositions containing them. The active compounds of the present invention are 5-HT5A 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.

    摘要翻译： 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，其制备和含有它们的药物组合物。 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。