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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。

    Heterocyclic inhibitors of an Hh-signal cascade, medicinal compositions based thereon and methods for treating diseases caused by the aberrant activity of an Hh-signal system
    8.
    发明授权
    Heterocyclic inhibitors of an Hh-signal cascade, medicinal compositions based thereon and methods for treating diseases caused by the aberrant activity of an Hh-signal system 失效
    Hh信号级联的杂环抑制剂，基于其的医药组合物和用于治疗由Hh信号系统的异常活性引起的疾病的方法

    公开(公告)号：US08486945B2

    公开(公告)日：2013-07-16

    申请号：US12808152

    申请日：2008-12-12

    申请人： Andrey Ivashchenko ,  Yan Lavrovsky ,  Sergey Malyarchuk ,  Ilya Okun ,  Nikolay Savchuk ,  Sergey Tkachenko ,  Alexander Khvat ,  Alexander Ivashchenko

    发明人： Andrey Ivashchenko ,  Yan Lavrovsky ,  Sergey Malyarchuk ,  Ilya Okun ,  Nikolay Savchuk ,  Sergey Tkachenko ,  Alexander Khvat ,  Alexander Ivashchenko

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D487/00

    CPC分类号： C07D487/04 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2059 ,  A61K9/4858 ,  C07D215/58 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

    摘要： The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]N-acidylated 3-azole derivatives.

    摘要翻译： 本发明涉及新颖的杂环化合物及其用途，含有所述化合物作为活性成分的药物组合物及其用于生产用于治疗由异常活性引起的疾病的人和温血动物的药物制剂的用途 刺猬（Hh） - 信号系统，特别是肿瘤疾病。 本发明还涉及以“分子药理学工具”形式的上述化合物用于检查（体外和体内）Hh信号系统的生化特征的用途，特别是Hh蛋白和 跨膜蛋白，即抑制剂Patched（Ptc）和原癌蛋白。 所要求保护的八个化合物组包括2,6-二氢-7H-吡唑并[3,4-d]哒嗪-7-酮和1,4-二氢吡唑并[3,4-b] [1,4] 噻嗪-5-酮; N-酸化的4-咪唑并[1,2-a]嘧啶-2-基]苯胺; （[4H-噻吩并[3,2-b]吡咯-5-基）羰基]哌啶-4-碳酸酰胺; 2-（4-氰基吡啶-1-基） - 异烟酰胺; N-磺酰基-1,2,3,4-四氢喹啉-6-碳酸酰胺; 和吡啶2-氨基-4,5,6,7-四氢噻吩并[2,3-c] N-酸化的3-唑衍生物。