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    (EN) SUBSTITUTED 2-AMINO-3-SULFONYL-PYRAZOLO[1,5-A] PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF
    2.
    发明申请
    (EN) SUBSTITUTED 2-AMINO-3-SULFONYL-PYRAZOLO[1,5-A] PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF 有权
    （EN）取代的2-氨基-3-磺酰基 - 吡唑并[1,5-A]嘧啶/硒酸5-HT6受体的拮抗剂，其生产方法及其用途

    公开(公告)号：US20100292245A1

    公开(公告)日：2010-11-18

    申请号：US12812733

    申请日：2009-01-23

    申请人： Andrey Alexandrovich IVASHCHENKO

    发明人： Andrey Alexandrovich IVASHCHENKO

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P3/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors. Ar represents optionally substituted aryl or optionally substituted heterocyclyl; R1 and R3 independently of each other represent C1-C3 alkyl or aryl; R2 represents hydrogen or C1-C3 alkyl; R41, and R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41, and R42 together with nitrogen atom they are attached to form optionally substituted heterocyclyl.

    摘要翻译： 本发明涉及通式1的新的取代的2-氨基-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，新药物和药物组合物，药物，方法 以及用于预防和治疗各种CNS疾病的方法，其发病机制与单胺能信号通路的紊乱相关，更具体地说是5-羟色胺5-HT 6受体的过激活或低激活。 Ar表示任选取代的芳基或任选取代的杂环基; R1和R3彼此独立地表示C1-C3烷基或芳基; R2代表氢或C1-C3烷基; R 41和R 42彼此独立地表示氢，任选取代的C 1 -C 3烷基或任选取代的苯基，或R 41和R 42与它们连接的氮原子一起形成任选取代的杂环基。

    (EN) 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO [1,5-A]PYRIMIDINES / ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF
    3.
    发明申请
    (EN) 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO [1,5-A]PYRIMIDINES / ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF 有权
    （EN）2-烷基亚氨基-3-磺酰氟环己基[e OR d]吡唑并[1,5-A]嘧啶/硒酸5-HT6受体的拮抗剂，其生产方法及其用途

    公开(公告)号：US20100292256A1

    公开(公告)日：2010-11-18

    申请号：US12812734

    申请日：2009-01-23

    申请人： Andrey Alexandrovich IVASHCHENKO

    发明人： Andrey Alexandrovich IVASHCHENKO

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/00 ,  A61P3/04

    CPC分类号： C07D487/04

    摘要： The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.

    摘要翻译： 本发明涉及5-羟色胺5-HT 6受体拮抗剂的取代的2-烷基氨基-3-（芳基磺酰基）环烷基[e或d]吡唑并[1,5-a]嘧啶，用于新药物和包含所述化合物的药物组合物 活性成分，以及用于治疗和预防各种CNS疾病的新药物和方法。 通式1的2-烷基氨基-3-芳基磺酰基环烷基[e]吡唑并[1,5-a]嘧啶和2-烷基氨基-3-芳基磺酰基环烷基[d]吡唑并[1,5-a]嘧啶，其中： R1是氢或C1-C3烷基; R2是C1-C3烷基; R 3是氢，一个或多个任选相同的卤原子，任选被C 1 -C 3烷基取代的C 1 -C 3烷基或羟基; n是整数1,2或3。