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138 条记录 (耗时 0.034 秒)

    AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION
    31.
    发明申请
    AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION 有权
    具有部分NICOTINIC乙酰胆碱受体激动剂和多巴胺反复抑制组合的联合衍生物

    公开(公告)号：US20110053962A1

    公开(公告)日：2011-03-03

    申请号：US12940271

    申请日：2010-11-05

    申请人： Axel Stoit ,  Hein K.A.C. Coolen ,  Martina A.W. Van Der Neut ,  Cornelis G. Kruse

    发明人： Axel Stoit ,  Hein K.A.C. Coolen ,  Martina A.W. Van Der Neut ,  Cornelis G. Kruse

    IPC分类号： A61K31/519 ,  A61K31/437 ,  A61P25/00 ,  A61P29/00 ,  A61P27/02 ,  A61P9/00 ,  A61P3/00 ,  A61P1/04

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

    摘要翻译： 描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途 以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过这些受体的操纵来治疗。

    Process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one and salts and solvates thereof
    33.
    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
    34.
    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。

    Imidazoline derivatives having CB1-antagonistic activity
    38.
    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。

    N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS
    39.
    发明申请
    N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS 有权
    芬太尼氧化物和邻苯二甲酸氧氟沙星作为PRODRUGS

    公开(公告)号：US20090005455A1

    公开(公告)日：2009-01-01

    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： A61K31/135 ,  C07C217/74 ,  A61P25/00 ,  C07C215/56

    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。

    USE OF 5-HT6 ANTAGONISTS TO PREVENT RELAPSE INTO ADDICTION
    40.
    发明申请
    USE OF 5-HT6 ANTAGONISTS TO PREVENT RELAPSE INTO ADDICTION 审中-公开
    5-HT6拮抗剂的使用，以防止患者继续使用

    公开(公告)号：US20080171779A1

    公开(公告)日：2008-07-17

    申请号：US12013898

    申请日：2008-01-14

    申请人： Natasja M.W.J. De Bruin ,  Arnold Van Loevezijn ,  Johan Wijnen ,  Arnoldus H.J. Herremans ,  Cornelis G. Kruse

    发明人： Natasja M.W.J. De Bruin ,  Arnold Van Loevezijn ,  Johan Wijnen ,  Arnoldus H.J. Herremans ,  Cornelis G. Kruse

    IPC分类号： A61K31/415 ,  A61P25/30

    CPC分类号： A61K31/415

    摘要： A novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT6 antagonists, are disclosed. In one embodiment, the invention relates to the use of these compounds or pharmaceutical compositions comprising these compounds for preventing relapse into addiction, for example, relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, relapse into addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and relapse into certain addictive behaviors, including gambling.

    摘要翻译： 公开了其作为5-HT 6拮抗剂的化合物及其药学上可接受的盐的新用途。 在一个实施方案中，本发明涉及这些化合物或包含这些化合物的药物组合物用于预防复发成瘾的用途，例如复发成瘾物质，包括阿片剂，致幻剂，吸入剂，苯环利定，苯丙胺，可卡因，大麻 ，尼古丁和酒精，对某些药物，包括镇静剂，催眠药和抗焦虑药物复发，并复发到某些令人上瘾的行为，包括赌博。