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    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists
    2.
    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：US07786144B2

    公开(公告)日：2010-08-31

    申请号：US11754544

    申请日：2007-05-29

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

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

    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。

    Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
    4.
    发明授权
    Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition 有权
    具有大麻素CB1拮抗作用和5-羟色胺再摄取抑制作用的化合物

    公开(公告)号：US08138174B2

    公开(公告)日：2012-03-20

    申请号：US11970229

    申请日：2008-01-07

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse

    IPC分类号： A61K31/55

    CPC分类号： C07D403/12 ,  C07D231/06 ,  C07D233/90

    摘要： Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed.In at least one embodiment, the invention relates to compounds of the general formula (1): wherein the substitutents have the definitions given in the specification.

    摘要翻译： 具有大麻素CB1拮抗作用和5-羟色胺再摄取抑制作用的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，制备用于它们合成的新中间体的方法和制备这些组合物的方法。 这些化合物和组合物的用途，特别是它们在给予患者以在精神病，焦虑症，抑郁症，注意力缺陷，认知障碍，肥胖症，药物依赖，帕金森病，阿尔茨海默病，疼痛障碍，神经性疼痛障碍中治疗效果方面的用途 并且公开了性障碍。 在至少一个实施方案中，本发明涉及通式（1）的化合物：其中取代基具有说明书中给出的定义。

    1H-imidazole derivatives as cannabinoid receptor modulators
    6.
    发明授权
    1H-imidazole derivatives as cannabinoid receptor modulators 有权
    1H-咪唑衍生物作为大麻素受体调节剂

    公开(公告)号：US07271189B2

    公开(公告)日：2007-09-18

    申请号：US10965155

    申请日：2004-10-15

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Herman H. Van Stuivenberg ,  Hiskias G. Keizer

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Herman H. Van Stuivenberg ,  Hiskias G. Keizer

    IPC分类号： A61K31/4164 ,  C07D233/60

    CPC分类号： C07D233/90

    摘要： The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved.The compounds have the general formula (I) wherein R, R1-R4 and X have the meanings given in the specification.

    摘要翻译： 本发明涉及一组作为大麻素受体的调节剂的1H-咪唑衍生物，制备这些化合物的方法，可用于合成所述咪唑衍生物的新中间体，制备这些中间体的方法，药物 含有这些1H-咪唑衍生物中的一种或多种作为活性成分的组合物，以及这些药物组合物用于治疗涉及大麻素受体的精神病和神经障碍的用途。 化合物具有通式（I），其中R 1，R 1 -R 4和X具有说明书中给出的含义。

    4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
    8.
    发明授权
    4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
    具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物

    公开(公告)号：US06476060B2

    公开(公告)日：2002-11-05

    申请号：US09814694

    申请日：2001-03-23

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Bernard J. Van Vliet

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Bernard J. Van Vliet

    IPC分类号： A61K31415

    CPC分类号： C07D231/06 ,  C07D231/08 ,  C07D401/04 ,  C07D409/04

    摘要： The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor. The compounds have the formula (I) wherein R and R1 are the same or different and represent unsubstituted or substituted phenyl, thienyl, or pyridyl, or naphthyl. naphthyl R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v) as defined herein, Bb represents sulfonyl or carbonyl, and R3 represents benzyl, phenyl, thienyl or pyridyl, each of which is unsubstituted or substituted, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphthyl.

    摘要翻译： 本发明涉及新的4,5-二氢-1H-吡唑化合物，其可以是大麻CB1-受体的有效拮抗剂。化合物具有式（I），其中R和R 1相同或不同， 代表未取代或取代的苯基，噻吩基或吡啶基或​​萘基。 萘基R 2表示氢，羟基，C 1-3 - 烷氧基，乙酰氧基或丙酰氧基，A a表示如本文所定义的基团（ⅰ），（ⅱ），（ⅲ），（ⅳ）或（Ⅴ）中的一个，Bb表示磺酰基或羰基 ，R 3表示苄基，苯基，噻吩基或吡啶基，其各自为未取代或取代的，或R3表示C1-8支链或非支链烷基或C3-8环烷基，或R3表示萘基。

    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists
    9.
    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。

    1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
    10.
    发明授权
    1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
    具有CB1拮抗活性的1,3,5-三取代的4,5-二氢-1H-吡唑衍生物

    公开(公告)号：US07745476B2

    公开(公告)日：2010-06-29

    申请号：US11033683

    申请日：2005-01-13

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Herman H. Van Stuivenberg

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Herman H. Van Stuivenberg

    IPC分类号： A61K31/415 ,  C07D231/06

    CPC分类号： C07D231/06

    摘要： The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives as CB1 antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect.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CB1拮抗剂的1,3,5-三取代的4,5-二氢-1H-吡唑衍生物，用于制备这些化合物的方法和用于合成所述吡唑衍生物的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 化合物具有通式（I），其中符号具有说明书中给出的含义。