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    Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof
    3.
    发明授权
    Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof 有权
    取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，5-羟色胺5-HT 6受体拮抗剂及其生产和使用方法

    公开(公告)号：US08618114B2

    公开(公告)日：2013-12-31

    申请号：US13122152

    申请日：2009-10-06

    申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

    发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X=S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X=S or X=NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.

    摘要翻译： 本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及 预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍 和肥胖。 在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基， 金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。

    SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF
    4.
    发明申请
    SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF 有权
    取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，丝氨酸5-HT6受体拮抗剂及其生产和使用方法

    公开(公告)号：US20110178078A1

    公开(公告)日：2011-07-21

    申请号：US13122152

    申请日：2009-10-06

    申请人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

    发明人： Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko ,  Yan Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Madina Georgievna Kadieva

    IPC分类号： A61K31/5377 ,  A61K31/497 ,  A61K31/519 ,  C07D487/04 ,  A61P3/04 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P3/10

    CPC分类号： C07D487/04

    摘要： The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.In the general formula 1: wherein: X═S, SO or NH; R1 represents hydrogen, optionally substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R2 represents hydrogen, halogen, optionally substituted C1-C3alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R3 represents hydrogen, optionally substituted C1-C3alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X═S or X═NH, at least one of R1, R2 or R3 represent substituted C1-C3alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R1, R2 or R3 represent hydrogen; R4 represents C1-C3alkyl; R5 represents hydrogen, one or two halogens, C1-C3alkyl or optionally substituted hydroxyl.

    摘要翻译： 本发明涉及通式1的新的取代的3-芳基磺酰基 - 吡唑并[1,5-a]嘧啶，其药学上可接受的盐和/或水合物，5-羟色胺5-HT 6受体拮抗剂和药物组合物，还涉及 预防和治疗人类和温血动物的各种中枢神经系统疾病，其发病机制与血清素5-HT6受体，特别是阿尔茨海默病，帕金森病，亨廷顿病，精神分裂症和其他神经变性疾病，认知障碍 和肥胖。 在通式1中：其中：X = S，SO或NH; R 1表示氢，任选取代的C 1 -C 3烷基，环烷基，金刚烷基，芳基或杂环基; R 2表示氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，芳基二氮烯基或任选取代的氨基; R 3表示氢，任选取代的C 1 -C 3烷基，取代的羟基，吡啶基或任选取代的氨基，此外，在X = S或X = NH的情况下，R 1，R 2或R 3中的至少一个表示取代的C 1 -C 3烷基，环烷基， 金刚烷基，芳基，杂环基，卤素，取代的羟基，任选取代的氨基，芳基二氮烯基或R 1，R 2或R 3中的至少两个表示氢; R4代表C1-C3烷基; R5表示氢，一个或两个卤素，C1-C3烷基或任选取代的羟基。