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    Substitute 2-amino-3-(Sulfony)pyrazol[1,5-a]pyramidines - serotonin 5-ht6 receptor antagonists, method for us thereof
    4.
    发明申请
    Substitute 2-amino-3-(Sulfony)pyrazol[1,5-a]pyramidines - serotonin 5-ht6 receptor antagonists, method for us thereof 有权
    替代2-氨基-3-（磺酰基）吡唑[1,5-a]吡啶并 - 5-羟色胺5-ht6受体拮抗剂，其方法

    公开(公告)号：US20130079350A1

    公开(公告)日：2013-03-28

    申请号：US13573818

    申请日：2012-10-09

    申请人： Alexander Vasilievich Ivashtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk

    发明人： Alexander Vasilievich Ivashtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk

    IPC分类号： C07D487/04

    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.In general formula 1 R1 and R3 independently of each other represent C1-C3 alkyl or phenyl; R2 represents hydrogen or C1-C3 alkyl; R41, R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41 and R42 together with the nitrogen atom they are attached to form optionally substituted heterocyclyl; Ar is aryl selected from phenyl, optionally substituted with Ri5 that is one or two optionally identical substituents selected from hydrogen, lower alkyl, trifluoromethyl or halogen; or optionally substituted 5-6-membered heteroaryl, containing as the heteroatom nitrogen or sulfur atom.

    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。 在通式1中，R 1和R 3彼此独立地表示C 1 -C 3烷基或苯基; R2代表氢或C1-C3烷基; R 41，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; Ar是选自苯基的芳基，任选被R 15取代，R 15是选自氢，低级烷基，三氟甲基或卤素的一个或两个任选相同的取代基; 或含有杂原子氮或硫原子的任选取代的5-6元杂芳基。

    LIGANDS OF ALPHA-ADRENOCEPTORS, DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THEIR USE
    5.
    发明申请
    LIGANDS OF ALPHA-ADRENOCEPTORS, DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THEIR USE 审中-公开
    ALPHA-ADRENOCEPTORS，DOPAMINE，HISTAMINE，IMIDAZOLINE和SEROTONIN受体的配体及其用途

    公开(公告)号：US20110039825A1

    公开(公告)日：2011-02-17

    申请号：US12810013

    申请日：2008-12-19

    申请人： Andrey Alexandrovich Ivashchenko ,  Vasilievich Ivashchenko ,  Yan Vadimovich Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun

    发明人： Andrey Alexandrovich Ivashchenko ,  Vasilievich Ivashchenko ,  Yan Vadimovich Lavrovsky ,  Oleg Dmitrievich Mitkin ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun

    IPC分类号： A61K31/55 ,  C07D471/04 ,  A61K31/437 ,  A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  A61P25/28 ,  A61P25/24

    CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4858 ,  A61K31/407 ,  A61K31/437 ,  A61K31/55 ,  C07D487/04

    摘要： The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously α-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C1-C4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH2)m group, optionally substituted CH═CH group, optionally substituted CH2—CH═CH group, C≡C group, SO2 group; n=1, 2; m=1, 2, 3; solid line accompanied by dotted line, i.e. may represent single or double bond. The invention also relates to active ingredients, pharmaceutical compositions comprising the said ligands as active ingredients; to novel medicaments useful for treatment of diseases and conditions of central nervous system (CNS) of humans and warm-blooded animals.

    摘要翻译： 本发明涉及其具有广谱生物活性的新配体，其包括同时α-肾上腺素受体，多巴胺受体，组胺受体，咪唑啉受体和5-羟色胺受体，其中5-羟色胺5-HT 7受体是通式1的化合物，其形式为 游离碱，几何异构体，外消旋混合物或单独的光学异构体，药学上可接受的盐和/或水合物，其中：R1是氨基的取代基，其选自氢，任选取代的C 1 -C 4烷基，酰基，杂环基，烷氧基羰基，取代的 磺酰基 R2是选自氢，卤素，任选取代的C 1 -C 4烷基，CF 3，CN，烷氧基，烷氧基羰基，羧基，杂环基或取代的磺酰基的环状体系的取代基。 Ar是任选取代的芳基，不一定与杂环基或任选取代的芳族杂环基取代; W是任选取代的（CH 2）m基团，任选取代的CH = CH基团，任选取代的CH 2 -CH = CH基团，C≡C基团，SO 2基团; n = 1,2; m = 1,2,3。 伴有虚线的实线即可表示单键或双键。 本发明还涉及活性成分，包含所述配体作为活性成分的药物组合物; 用于治疗人类和温血动物的中枢神经系统（CNS）的疾病和病症的新型药物。