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16 条记录 (耗时 0.011 秒)

    IMIDAZOLINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY
    1.
    发明申请
    IMIDAZOLINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1拮抗活性的咪唑啉衍生物

    公开(公告)号：WO2005080345A2

    公开(公告)日：2005-09-01

    申请号：PCT/EP2005/050680

    申请日：2005-02-16

    申请人： SOLVAY PHARMACEUTICALS B.V. ,  LANGE, Josephus, H., M. ,  KRUSE, Cornelis, G. ,  VAN STUIVENBERG, Herman, H.

    发明人： LANGE, Josephus, H., M. ,  KRUSE, Cornelis, G. ,  VAN STUIVENBERG, Herman, H.

    IPC分类号： C07D233/00

    CPC分类号： C07D233/16 ,  C07D233/50 ,  C07D233/52

    摘要： The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, 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1,2,4-三取代咪唑啉衍生物，制备这些化合物的方法，可用于合成所述咪唑啉衍生物的新中间体，制备这些中间体的方法，药物组合物 含有这些咪唑啉衍生物中的一种或多种作为活性成分，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
    2.
    发明申请
    1,3,5-TRISUBSTITUTED 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1拮抗活性的1,3,5-三唑并[4,5-d]二氢-1H-吡唑衍生物

    公开(公告)号：WO2005074920A1

    公开(公告)日：2005-08-18

    申请号：PCT/EP2005/050339

    申请日：2005-01-27

    申请人： SOLVAY PHARMACEUTICALS B.V. ,  LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  VAN STUIVENBERG, Herman H.

    发明人： LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  VAN STUIVENBERG, Herman H.

    IPC分类号： A61K31/4155

    CPC分类号： C07D231/06

    摘要： The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1 H-pyrazole derivatives as CB 1 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。

    1H-IMIDAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS
    4.
    发明申请
    1H-IMIDAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
    1H-咪唑衍生物作为CANNABINOID受体调节剂

    公开(公告)号：WO2005040130A1

    公开(公告)日：2005-05-06

    申请号：PCT/EP2004/052575

    申请日：2004-10-19

    申请人： SOLVAY PHARMACEUTICALS B.V. ,  LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  VAN STUIVENBERG, Herman H. ,  KEIZER, Hiskias G.

    发明人： LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  VAN STUIVENBERG, Herman H. ,  KEIZER, Hiskias G.

    IPC分类号： C07D233/90

    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, R 1 -R 4 and X have the meanings given in the specification.

    摘要翻译： 本发明涉及一组1H-咪唑衍生物，其是大麻素受体的调节剂，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。 所述化合物具有通式（I），其中R，R 1 -R 4和X具有说明书中给出的含义。

    BIFEPRUNOX DERIVATIVES
    8.
    发明申请
    BIFEPRUNOX DERIVATIVES 审中-公开
    BIFEPRUNOX衍生物

    公开(公告)号：WO2009090177A1

    公开(公告)日：2009-07-23

    申请号：PCT/EP2009/050336

    申请日：2009-01-14

    申请人： SOLVAY PHARMACEUTICALS B.V. ,  VAN STUIVENBERG, Herman H. ,  BARF, Gerrit A.

    发明人： VAN STUIVENBERG, Herman H. ,  BARF, Gerrit A.

    IPC分类号： C07D263/58 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16

    CPC分类号： C07D263/58

    摘要： The present invention relates to bifeprunox derivatives of the formula (I) wherein R1 is one substituent selected from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, a solvate or hydrate thereof, which are potent ligands for the dopamine D 2 receptor, exhibiting strong partial dopamine D 2 agonistic effects with a percentage agonism significantly higher than bifeprunox. The compounds of the invention may be used in the treatment, alleviation or prevention of dopamine D 2 receptor mediated diseases and conditions requiring dopamine D 2 agonistic effects.

    摘要翻译： 本发明涉及式（I）的二不饱和衍生物，其中R 1是选自3-OH，4-OH，3-OSO 3 H和4 -OSO 3 H的一个取代基; R2为H; 或作为多巴胺D2受体的有效配体的N-氧化物或其药学上可接受的盐，其溶剂合物或水合物，显示出比双歧杆菌明显高的百分比激动作用的强烈部分多巴胺D2激动作用。 本发明的化合物可用于治疗，缓解或预防多巴胺D2受体介导的疾病和需要多巴胺D2激动作用的病症。