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    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists
    1.
    发明授权
    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 有权
    含硫吡唑衍生物作为选择性大麻素CB1受体拮抗剂

    公开(公告)号：US08461184B2

    公开(公告)日：2013-06-11

    申请号：US12844156

    申请日：2010-07-27

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Bernard J. Vliet Van

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Bernard J. Vliet Van

    IPC分类号： A61K31/4155 ,  A61K31/4453 ,  C07D231/10 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D403/12

    摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB1 / CB2受体亚型选择性的选择性大麻素CB1受体拮抗剂，用于制备这些化合物的方法，可用于合成的新中间体 这些吡唑衍生物，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗精神和神经障碍的用途。 化合物具有通式（I），其中符号具有说明书中给出的含义。

    FLUORO-SUBSTITUTED 3,4-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY
    2.
    发明申请
    FLUORO-SUBSTITUTED 3,4-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1拮抗活性的氟取代的3,4-二基-4,5-二氢-1H-吡唑-1-羧酰胺衍生物

    公开(公告)号：US20110172274A1

    公开(公告)日：2011-07-14

    申请号：US12999494

    申请日：2009-06-15

    申请人： Josephus H.M. Lange ,  Bernard J. Vliet, Van

    发明人： Josephus H.M. Lange ,  Bernard J. Vliet, Van

    IPC分类号： A61K31/454 ,  C07D401/12 ,  A61P3/04 ,  A61P9/00 ,  A61P25/30 ,  A61P1/16 ,  A61P31/00

    CPC分类号： C07D401/12

    摘要： This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, methods for preparing these compounds, novel intermediates useful for the synthesis of said compounds, methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as active ingredient, as well as the use of these pharmaceutical compositions for the treatment of obesity and obesity-related cardiovascular disorders, drug addiction, cognition deficits, liver fibrosis and inflammatory disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明涉及作为大麻素-CB1受体拮抗剂的氟化3,4-二芳基-4,5-二氢-1H-吡唑-1-甲脒衍生物，制备这些化合物的方法，可用于合成所述化合物的新中间体， 这些中间体的制备，含有一种或多种这些二氢吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗肥胖和肥胖相关心血管疾病，药物成瘾，认知缺陷，肝纤维化和炎症的用途 疾病 化合物具有通式（I），其中符号具有说明书中给出的含义。

    4,5 Dihydro-(1H)-Pyrazole Derivatives as Cannabinoid CB1 Receptor Modulators
    3.
    发明申请
    4,5 Dihydro-(1H)-Pyrazole Derivatives as Cannabinoid CB1 Receptor Modulators 有权
    4,5二氢 - （1H） - 吡唑衍生物作为大麻素CB1受体调节剂

    公开(公告)号：US20080312276A1

    公开(公告)日：2008-12-18

    申请号：US12136986

    申请日：2008-06-11

    申请人： Josephus H.M. Lange ,  Hendrik C. Wals ,  Bernard J. Vliet Van ,  Mahmut Yildirim

    发明人： Josephus H.M. Lange ,  Hendrik C. Wals ,  Bernard J. Vliet Van ,  Mahmut Yildirim

    IPC分类号： A61K31/4709 ,  C07D231/06 ,  C07D401/12 ,  A61P25/28 ,  A61K31/415

    CPC分类号： C07D231/06 ,  C07D401/12 ,  C07D409/04

    摘要： The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders.Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.

    摘要翻译： 本发明涉及作为大麻素CB1受体调节剂的4,5-二氢 - （1H） - 吡唑（吡唑啉）衍生物，包含这些化合物的药物组合物，其合成方法，制备用于其合成的新中间体的方法， 以及制备组合物的方法。 本发明还涉及施用于患者的化合物和组合物在多发性硬化，创伤性脑损伤，疼痛，包括慢性疼痛，神经性疼痛，急性疼痛和炎性疼痛，骨质疏松症，食欲障碍，癫痫，阿尔茨海默病中的治疗效果的用途 ，Tourette综合征，脑缺血，呕吐，恶心和胃肠道疾病。 本公开的化合物涉及式（I）：其中取代基具有说明书中给出的定义。