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    2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-A]pyrido-pyrimidine antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof
    1.
    发明授权
    2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-A]pyrido-pyrimidine antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof 有权
    5-羟色胺5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶并 - 嘧啶拮抗剂，其制备方法和用途

    公开(公告)号：US08552017B2

    公开(公告)日：2013-10-08

    申请号：US12937718

    申请日：2009-04-30

    申请人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    发明人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00

    CPC分类号： C07D471/14 ,  A61K31/519

    摘要： The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases.Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is hydrogen, optionally substituted C1-C3 alkyl, C1-C4 alkyloxycarbonyl; R2 is hydrogen, halogen or optionally substituted C1-C3 alkyl; R13 and R23 represent optionally alike: hydrogen, optionally substituted C1-C3 alkyl or R13 and R23 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.

    摘要翻译： 本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基 -3-芳基磺酰基-5,6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，药物物质和药物组合物，其包含作为所述化合物的所述药物物质， 预防和治疗人类和动物的中枢神经系统的各种疾病，其发病机制与血清素5-HT6受体（包括认知和神经变性疾病）相关。 通式1的取代的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基-3-芳基磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，及其药学上可接受的盐和/或水合物。 其中：Ar是任选取代的芳基或任选取代的杂芳基; R 1是氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2是氢，卤素或任选取代的C 1 -C 3烷基; R 13和R 23任选地相似：氢，任选取代的C 1 -C 3烷基或R 13和R 23与它们所连接的氮原子一起形成任选取代的杂环。

    (EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
    2.
    发明授权
    (EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof 有权
    （EN）3-磺酰基 - 吡唑并[1,5-a]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，生产方法及其用途

    公开(公告)号：US08552005B2

    公开(公告)日：2013-10-08

    申请号：US12812728

    申请日：2009-01-23

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

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

    IPC分类号： A01N43/90 ,  A01N43/00 ,  A61K31/519 ,  A61K31/33 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation.In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.

    摘要翻译： 本发明涉及通式1的药学上可接受的盐和/或水合物的新的取代的3-（芳基磺酰基）吡唑并[1,5-a]嘧啶新颖的5-羟色胺5-HT 6受体拮抗剂，新药物，药物组合物， 药物及其制备方法，用于治疗和预防CNS的病理状态和疾病，其发病机制与血清素5-HT6受体激活的干扰有关。 在通式1的化合物中Ar表示任选取代的芳基或杂环基; R 1，R 2和R 3彼此独立地表示氢，C 1 -C 3烷基或苯基; R 4表示氢，任选取代的C 1 -C 5烷基，取代的羟基或取代的硫烷基。

    (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
    3.
    发明授权
    (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/ 5-羟色胺5-HT 6受体的拮抗剂，其制备方法及用途

    公开(公告)号：US08309559B2

    公开(公告)日：2012-11-13

    申请号：US12812733

    申请日：2009-01-23

    申请人： Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    发明人： Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

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

    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。

    Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof
    5.
    发明授权
    Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof 有权
    四氢吡唑并[1,5-a]吡啶并嘧啶作为5-羟色胺5-HT 6受体的拮抗剂，其生产和使用方法

    公开(公告)号：US08569318B2

    公开(公告)日：2013-10-29

    申请号：US12937720

    申请日：2009-04-30

    申请人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    发明人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00

    CPC分类号： C07D471/14 ,  A61K31/519

    摘要： The present invention relates to serotonin 5-HT6 receptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors.In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group; R2 is hydrogen or optionally substituted C1-C3 alkyl; R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.

    摘要翻译： 本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型取代的3-磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的3-磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，包含上述化合物的药物的药物和药物组合物，以及各种条件的预防和治疗方法 人类的中枢神经系统疾病和温血动物，其发病机制与血清素5-HT6受体有关。 在式1和2中Ar是任选取代的芳基或任选取代的杂环基; R1是氢，任选取代的低级C 1 -C 3烷基，取代的羟基，取代的硫烷基; R2是氢或任选取代的C 1 -C 3烷基; R3是氢，任选取代的C 1 -C 3烷基或叔丁氧基羰基。

    (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
    7.
    发明授权
    (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-烷基氨基-3-芳基磺酰基 - 环硫烷基[e OR d]吡唑并[1,5-A]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，其制备方法及用途

    公开(公告)号：US08471009B2

    公开(公告)日：2013-06-25

    申请号：US12812734

    申请日：2009-01-23

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

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

    IPC分类号： A61K31/519 ,  C07D487/04

    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。

    LIGANDS OF 5-HT6 RECEPTORS, A PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF
    9.
    发明申请
    LIGANDS OF 5-HT6 RECEPTORS, A PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
    5-HT6受体的配体，药物组合物，其生产和使用方法

    公开(公告)号：US20110046368A1

    公开(公告)日：2011-02-24

    申请号：US12741006

    申请日：2007-11-15

    申请人： Andrey Alexandrovich Ivashchenko ,  Alexander Vasilievich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk

    发明人： Andrey Alexandrovich Ivashchenko ,  Alexander Vasilievich Ivashchenko ,  Sergey Yevgenievich Tkachenko ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk

    IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D473/04

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

    摘要： The invention relates to novel ligands of 5-HT6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT6 receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT6 receptors are playing an essential role.Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT6 ligands. Wherein R2 and R3 independently of each other represent an amino group substituent selected from hydrogen; substituted carbonyl; substituted aminocarbonyl; substituted aminothiocarbonyl; substituted sulphonyl; C1-C5-alkyl optionally substituted by: C6-C10-arylaminocarbonyl, heterocyclyl, C6-C10-arylaminocarbonyl, C6-C10-arylaminothiocarbonyl, C5-C10-azaheteroaryl, optionally substituted carboxyl, nitryl group, optionally substituted aryl; R1k represents from 1 to 3 substituents of cyclic system, independent of each other and selected from hydrogen, optionally substituted C1-C5-alkyl, C1-C5-alkoxy, C1-C5-alkenyl, C1-C5-alkynyl, halogen, trifluoromethyl, CN-group, carboxyl, optionally substituted aryl, optionally substituted heterocyclyl, substituted sulfonyl, optionally substituted carboxyl; the solid line accompanied by the dotted line represents a single or a double bond; n=1, 2 or 3.

    摘要翻译： 本发明涉及含有5-HT 6受体作为活性成分的所述新型配体的药物组合物和用于人和用于治疗中枢神经系统疾病和病症的温血动物的新型药物的5-HT 6受体的新配体， 在5-HT6受体诱导的神经调节因子的发病机理中起着重要的作用。 通式1的氮杂环化合物或其外消旋体或光学或几何异构体或其药学上可接受的盐和/或水合物用作5-HT 6配体。 其中R2和R3彼此独立地表示选自氢的氨基取代基; 取代羰基; 取代的氨基羰基; 取代的氨基硫代羰基; 取代磺酰基; 任选被C 6 -C 10芳基氨基羰基，杂环基，C 6 -C 10 - 芳基氨基羰基，C 6 -C 10 - 芳基氨基硫代羰基，C 5 -C 10 - 氮杂杂芳基，任选取代的羧基，硝基，任选取代的芳基取代的C 1 -C 5 - 任选取代的C 1 -C 5 - 烷基，C 1 -C 5 - 烷氧基，C 1 -C 5 - 烯基，C 1 -C 5 - 炔基，卤素，三氟甲基， CN-基团，羧基，任选取代的芳基，任选取代的杂环基，取代的磺酰基，任选取代的羧基; 伴随虚线的实线表示单键或双键; n = 1,2或3。

    2-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF
    10.
    发明申请
    2-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
    丝氨酸5-HT6受体的2-氨基-3-磺酰基 - 四氢吡喃并[1,5-A]吡啶并 - 吡咯烷酮拮抗剂，其生产方法及其用途

    公开(公告)号：US20110046149A1

    公开(公告)日：2011-02-24

    申请号：US12937718

    申请日：2009-04-30

    申请人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    发明人： Andrey Alexandrovich Ivashchenko ,  Volodymyr Mikhailovich Kysil ,  Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    IPC分类号： A61K31/519 ,  C07D471/14 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P3/04 ,  C12N5/02

    CPC分类号： C07D471/14 ,  A61K31/519

    摘要： The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases.Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is hydrogen, optionally substituted C1-C3 alkyl, C1-C4 alkyloxycarbonyl; R2 is hydrogen, halogen or optionally substituted C1-C3 alkyl; R13 and R23 represent optionally alike: hydrogen, optionally substituted C1-C3 alkyl or R13 and R23 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.

    摘要翻译： 本发明涉及5-羟色胺5-HT 6受体拮抗剂 - 新型2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基 -3-芳基磺酰基-5,6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，药物物质和药物组合物，其包含作为所述化合物的所述药物物质， 预防和治疗人类和动物的中枢神经系统的各种疾病，其发病机制与血清素5-HT6受体（包括认知和神经变性疾病）相关。 通式1的取代的2-氨基-3-芳基磺酰基-6,7,8,9-四氢吡唑并[1,5-a]吡啶并[4,3-e]嘧啶和取代的2-氨基-3-芳基磺酰基-5 ，6,7,8-四氢吡唑并[1,5-a]吡啶并[4,3-d]嘧啶，及其药学上可接受的盐和/或水合物。 其中：Ar是任选取代的芳基或任选取代的杂芳基; R 1是氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2是氢，卤素或任选取代的C 1 -C 3烷基; R 13和R 23任选地相似：氢，任选取代的C 1 -C 3烷基或R 13和R 23与它们所连接的氮原子一起形成任选取代的杂环。