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109 条记录 (耗时 0.075 秒)

    1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mGluR2-receptors
    1.
    发明授权
    1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mGluR2-receptors 有权
    1,4-二取代的3-氰基 - 吡啶酮衍生物及其作为mGluR2受体的正变构调节剂的用途

    公开(公告)号：US09067891B2

    公开(公告)日：2015-06-30

    申请号：US13610000

    申请日：2012-09-11

    申请人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens

    发明人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens

    IPC分类号： A61K31/443 ,  C07D401/04 ,  C07D213/85 ,  A61K31/198 ,  A61K31/444

    CPC分类号： C07D213/85 ,  A61K31/198 ,  A61K31/444

    摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

    摘要翻译： 本发明涉及新化合物，特别是包括其任何立体化学异构形式的式（I）的新型吡啶酮衍生物或其药学上可接受的盐或其溶剂合物，其中所有基团在本申请和权利要求书中定义。 根据本发明的化合物是代谢型谷氨酸受体亚型2（“mGluR2”）的正变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病学障碍以及涉及代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及药物组合物和制备这些化合物和这些组合物的方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

    Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
    3.
    发明授权
    Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists 有权
    Thia（dia）zoles作为快速解离的多巴胺2受体拮抗剂

    公开(公告)号：US08933101B2

    公开(公告)日：2015-01-13

    申请号：US12597164

    申请日：2008-04-18

    申请人： Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda ,  Michiel Luc Maria Van Gool

    发明人： Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda ,  Michiel Luc Maria Van Gool

    IPC分类号： A61K31/454 ,  C07D417/12 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07D417/12

    摘要： The present invention relates to [1-(benzyl)-piperidin-4-yl]-([1,3,4]thiadiazol-2-yl)-amine and [1-(benzyl)-piperidin-4-yl]-(thiazol-2-yl)-amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

    摘要翻译： 本发明涉及[1-（苄基） - 哌啶-4-基] - （[1,3,4]噻二唑-2-基） - 胺和[1-（苄基） - 哌啶-4-基] - （I）的（噻唑-2-基） - 胺衍生物，其是快速解离的多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。