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    N-Substituted-1H-Quinoline-2,4-Diones, Preparation Method Thereof, And Pharmaceutical Composition Containing The Same
    2.
    发明申请
    N-Substituted-1H-Quinoline-2,4-Diones, Preparation Method Thereof, And Pharmaceutical Composition Containing The Same 审中-公开
    N-取代的1H-喹啉-2,4-二酮，其制备方法和含有它的药物组合物

    公开(公告)号：US20080275058A1

    公开(公告)日：2008-11-06

    申请号：US12065565

    申请日：2005-11-23

    申请人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Wookyu Park ,  Jaeyang Kong ,  Chulmin Park

    发明人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Wookyu Park ,  Jaeyang Kong ,  Chulmin Park

    IPC分类号： A61K31/496 ,  C07D401/04 ,  A61P25/28 ,  A61P25/24

    CPC分类号： C07D215/38

    摘要： The present invention relates to compounds of N-substituted -1H-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of N-substituted-1H-quinoline-2,4-diones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by methamphetamine and don't show rotatod deficit in mice. Thereof the compounds according to the present invention may be valuably used for treatment if a 5HT6 receptor relating disorder

    摘要翻译： 本发明涉及作为5HT6受体拮抗剂的N-取代的-1H-喹啉-2,4-二酮的化合物及其制备方法，以及含有该化合物的治疗中枢神经系统病症的药物组合物。 根据本发明的N-取代-1H-喹啉-2,4-二酮的化合物对5HT6受体具有优异的结合亲和力，对5HT6受体的选择性优于其他受体。 此外，化合物反转甲基苯丙胺对PPI的破坏，并且在小鼠中不显示旋转异物。 根据本发明的化合物可以有价值地用于治疗，如果5HT6受体相关疾病

    Indol carboxylic acid bispyridyl carboxamide derivatives, pharmaceutically acceptable salt thereof, preparation method and composition containing the same as an active ingredient
    3.
    发明授权
    Indol carboxylic acid bispyridyl carboxamide derivatives, pharmaceutically acceptable salt thereof, preparation method and composition containing the same as an active ingredient 有权
    吲哚羧酸双吡啶甲酰胺衍生物，其药学上可接受的盐，含有其作为活性成分的制备方法和组合物

    公开(公告)号：US08324246B2

    公开(公告)日：2012-12-04

    申请号：US12393528

    申请日：2009-02-26

    申请人： Churlmin Seong ,  Chul Min Park ,  Soyoung Kim ,  Wookyu Park ,  Nosang Park

    发明人： Churlmin Seong ,  Chul Min Park ,  Soyoung Kim ,  Wookyu Park ,  Nosang Park

    IPC分类号： A01N43/40 ,  A61K31/445 ,  C07D211/30 ,  C07D233/00

    CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12

    摘要： Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.

    摘要翻译： 本文公开了一种新的吲哚羧酸双吡啶羧酰胺衍生物及其制备方法，以及用于预防或治疗肥胖，尿失调和CNS障碍的组合物，其含有活性成分。 因为根据本发明的吲哚羧酸双吡啶甲酰胺衍生物对5-HT 2C受体具有高亲和力，因此选择性地对5-HT 2C受体起作用，所以衍生物很少具有由其它受体引起的不良作用。 由于衍生物有效抑制5-羟色胺活性，因此可用于治疗或预防肥胖症; 尿失禁如尿失禁，早泄，勃起功能障碍和前列腺增生; 与5-HT2c受体相关的诸如抑郁症，焦虑症，忧虑症，惊恐障碍，癫痫症，强迫症，偏头痛，睡眠障碍，药物滥用戒断，阿尔茨海默病和精神分裂症等CNS疾病。

    NOVEL SUBSTITUTED-1, 1-DIOXO-BENZO[1,2,4]THIADIAZIN-3ONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
    4.
    发明申请
    NOVEL SUBSTITUTED-1, 1-DIOXO-BENZO[1,2,4]THIADIAZIN-3ONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
    新的取代的1,1-二氧代苯并[1,2,4]噻二嗪-3-酮，其制备方法和含有其的药物组合物

    公开(公告)号：US20100035866A1

    公开(公告)日：2010-02-11

    申请号：US12293965

    申请日：2006-03-28

    申请人： Churlmin Seong ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong ,  Sunhee Kang ,  Chimin Park

    发明人： Churlmin Seong ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong ,  Sunhee Kang ,  Chimin Park

    IPC分类号： A61K31/5415 ,  C07D285/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/24 ,  A61P25/22 ,  A61P25/32

    CPC分类号： C07D285/24

    摘要： The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.

    摘要翻译： 本发明涉及作为5HT6受体拮抗剂的取代-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物，其制备方法和含有该化合物的药物组合物，其用于治疗 中枢神经系统疾病。 根据本发明的取代的-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物对5HT6受体具有优异的结合亲和力，对其它受体的5HT6受体的选择性优异。 此外，化合物反转了阿朴吗啡对PPI的破坏，并且在小鼠中不显示旋转异位缺陷。 因此，根据本发明的化合物可以有价值地用于治疗5HT6受体相关疾病。

    NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
    6.
    发明申请
    NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT 有权
    新型吲哚羧酸二异氰酸酯衍生物，其药物可接受的盐，其制备方法和组合物作为活性成分

    公开(公告)号：US20090258876A1

    公开(公告)日：2009-10-15

    申请号：US12393528

    申请日：2009-02-26

    申请人： Churlmin SEONG ,  Chul Min PARK ,  Soyoung KIM ,  Wookyu PARK ,  Nosang PARK

    发明人： Churlmin SEONG ,  Chul Min PARK ,  Soyoung KIM ,  Wookyu PARK ,  Nosang PARK

    IPC分类号： A61K31/53 ,  C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  C07D401/14 ,  C07D403/12 ,  A61P3/04

    CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12

    摘要： Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.

    摘要翻译： 本文公开了一种新的吲哚羧酸双吡啶羧酰胺衍生物及其制备方法，以及用于预防或治疗肥胖，尿失调和CNS障碍的组合物，其含有活性成分。 因为根据本发明的吲哚羧酸双吡啶甲酰胺衍生物对5-HT 2C受体具有高亲和力，因此选择性地对5-HT 2C受体起作用，所以衍生物很少具有由其它受体引起的不良作用。 由于衍生物有效抑制5-羟色胺活性，因此可用于治疗或预防肥胖症; 尿失禁如尿失禁，早泄，勃起功能障碍和前列腺增生; 与5-HT2c受体相关的诸如抑郁症，焦虑症，忧虑症，惊恐障碍，癫痫症，强迫症，偏头痛，睡眠障碍，药物滥用戒断，阿尔茨海默病和精神分裂症等CNS疾病。