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289 条记录 (耗时 0.029 秒)

    Process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one and salts and solvates thereof
    72.
    发明授权
    Process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one and salts and solvates thereof 有权
    制备3-氨基-8-（1-哌嗪基）-2H-1-苯并吡喃-2-酮及其盐和溶剂合物的方法

    公开(公告)号：US07776860B2

    公开(公告)日：2010-08-17

    申请号：US11085136

    申请日：2005-03-22

    申请人： Cornelis Bakker

    发明人： Cornelis Bakker

    IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D295/00

    CPC分类号： C07D311/18

    摘要： The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relates to novel salts and solvates, in particular hydrates of salts of said compound, as well as to their use as medicaments.The invention relates the compounds with the formula (7)

    摘要翻译： 本发明涉及一种制备3-氨基-8-（1-哌嗪基）-2H-1-苯并吡喃-2-酮的新方法，具有强力5-HT1A激动作用的广谱5-HT受体结合配体为 以及5-HT1D拮抗活性。 本发明还涉及新的盐和溶剂合物，特别是所述化合物的盐的水合物，以及它们作为药物的用途。 本发明涉及具有式（7）的化合物，

    N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs
    73.
    发明授权
    N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs 有权
    文拉法辛和o-去甲基文拉法辛的N-氧化物作为前药

    公开(公告)号：US07696383B2

    公开(公告)日：2010-04-13

    申请号：US12143919

    申请日：2008-06-23

    申请人： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th. M. Tulp

    发明人： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th. M. Tulp

    IPC分类号： C07C291/04 ,  A61K31/13

    CPC分类号： C07C291/04

    摘要： Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.

    摘要翻译： 本发明的实施方案涉及式（1）的化合物或其互变异构体，立体异构体，水合物或溶剂合物，其中R 1为H或CH 3。 本发明的其它实施方案涉及含有这些化合物的药物组合物，制备这些化合物的方法以及制备含有这些化合物的组合物的方法。 本发明的其它实施方案涉及这些化合物和含有它们的组合物的用途，例如用于制备用于治疗选自抑郁症，重度抑郁障碍，广泛性焦虑症，强迫症，社会焦虑症的药物和药物组合物 障碍，恐慌症，一般抑郁障碍，糖尿病性神经病，偏头痛和潮热。

    1 H-imidazole derivatives as cannabinoid receptor modulators
    79.
    发明授权
    1 H-imidazole derivatives as cannabinoid receptor modulators 失效
    1 H-咪唑衍生物作为大麻素受体调节剂

    公开(公告)号：US07498348B2

    公开(公告)日：2009-03-03

    申请号：US11842657

    申请日：2007-08-21

    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： A61K31/4523 ,  A61K31/4178 ,  A61K31/4166

    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。 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。

    Imidazoline derivatives having CB1-antagonistic activity
    80.
    发明授权
    Imidazoline derivatives having CB1-antagonistic activity 失效
    具有CB1拮抗活性的咪唑啉衍生物

    公开(公告)号：US07495108B2

    公开(公告)日：2009-02-24

    申请号：US11652582

    申请日：2007-01-12

    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： C07D233/00 ,  C07D233/22 ,  A01N43/50

    CPC分类号： C07D233/26

    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。