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    Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists
    6.
    发明授权
    Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists 有权
    芳基磺酰基吡唑啉甲脒衍生物作为5-HT6拮抗剂

    公开(公告)号：US08563723B2

    公开(公告)日：2013-10-22

    申请号：US12933182

    申请日：2009-03-17

    申请人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Axel Stoit ,  Agatha A. M. Rensink ,  Jennifer Venhorst ,  Martina A. W. Van Der Neut ,  Martin De Haan ,  Cornelis G. Kruse

    发明人： Arnold Van Loevezijn ,  Wouter I. Iwema Bakker ,  Axel Stoit ,  Agatha A. M. Rensink ,  Jennifer Venhorst ,  Martina A. W. Van Der Neut ,  Martin De Haan ,  Cornelis G. Kruse

    IPC分类号： C07D231/06 ,  C07D231/54 ,  C07D403/12 ,  C07D471/10 ,  C07D491/10

    CPC分类号： C07D231/06 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/635 ,  A61K45/06 ,  C07D231/00 ,  C07D231/54 ,  C07D403/12 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107

    摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

    摘要翻译： 本发明涉及作为5-HT 6受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，制备这些化合物的方法和用于它们合成的新型中间体。 本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途， 情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用 ，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。 化合物具有通式（1），其中符号具有说明书中给出的含义。

    AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION
    7.
    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。

    1H-imidazole derivatives as cannabinoid receptor modulators
    8.
    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。

    1 H-imidazole derivatives as cannabinoid receptor modulators
    9.
    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。

    USE OF 5-HT6 ANTAGONISTS TO PREVENT RELAPSE INTO ADDICTION
    10.
    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。