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    LIGANDS OF ALPHA-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF
    2.
    发明公开
    LIGANDS OF ALPHA-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF 审中-公开
    ALPHA-肾上腺素和多巴胺，组胺，咪唑啉和血清素受体及其使用配体

    公开(公告)号：EP2236511A2

    公开(公告)日：2010-10-06

    申请号：EP08864305.1

    申请日：2008-12-19

    申请人： Alla Chem, LLC. ,  Ivashchenko, Andrey Alexandrovich

    发明人： IVASHCHENKO, Andrey Alexandrovich ,  IVASHCHENKO, Alexander Vasilievich ,  LAVROVSKY, Yan Vadimovich ,  MITKIN, Oleg Dmitrievich ,  SAVCHUK, Nikolay Filippovich ,  TKACHENKO, Sergey Yevgenievich ,  OKUN, Ilya Matusovich

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/43 ,  A61K31/519 ,  A61P25/00

    CPC分类号： C07D471/04 ,  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-HT 7 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 C 1 -C 4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C 1 -C 4 alkyl, CF 3 , 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 (CH 2 ) m group, optionally substituted CH=CH group, optionally substituted CH 2 -CH=CH group, C≡C group, SO 2 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： 本发明涉及新的配体的生物学活性的广谱都包括同时±肾上腺素能受体，多巴胺受体，组胺受体，咪唑啉受体和血清素受体，其中血清素5-HT 7种受体，它们是在通式1的化合物 的游离碱，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，形式worin：R 1是氨基，选自氢，任选取代的C 1 -C 4烷基，酰基，杂环基的取代基， 烷氧基羰基，取代的磺酰基; R2是环体系，选自氢，卤素，任选取代的C 1个-C 4烷基，CF 3中选择的取代基，CN，烷氧基，烷氧基羰基，羧基，杂环基或取代的磺酰基; Ar是芳基OPTIONALLY substituiertem不一定安娜迟来与杂环基，或任选取代的芳族杂环基; W是任选substituiertem（CH 2）M基，任选substituiertem CH = CH基团，任选substituiertem CH 2 -CH = CH基团，C‰¡C组，SO 2基团; n = 1时，2; M = 1，2，3; solidLine陪同下虚线，即 （---）可以代表单键或双键。 因此，本发明涉及活性成分，药物组合物包含所述的配位体作为活性成分; 用于治疗的疾病和人类和温血动物的中枢神经系统（CNS）的条件下有用的新的药物。

    LIGAND WITH A BROAD SPECTRUM OF PHARMACOLOGICAL ACTIVITY, A PHARMACEUTICAL COMPOSITION, A MEDICINAL AGENT AND A METHOD OF TREATMENT
    4.
    发明公开
    LIGAND WITH A BROAD SPECTRUM OF PHARMACOLOGICAL ACTIVITY, A PHARMACEUTICAL COMPOSITION, A MEDICINAL AGENT AND A METHOD OF TREATMENT 审中-公开
    具有广泛的活动范围药理，药物组合物，药物和治疗方法的配体

    公开(公告)号：EP2327703A1

    公开(公告)日：2011-06-01

    申请号：EP09810284.1

    申请日：2009-08-03

    申请人： IVASHCHENKO, Andrey Alexandrovich ,  Alla Chem, LLC.

    发明人： IVASHCHENKO, Alexander Vasilievich ,  SAVCHUK, Nikolay Filippovich

    IPC分类号： C07D471/02 ,  A61K31/437 ,  A61P25/28

    CPC分类号： A61K31/437 ,  C07D471/04

    摘要： The present invention is directed to the novel ligand with wide range of pharmacological activity including activity to GPCR receptors, ion channels and monoamine transporters representing 3-methyl-9-benzyl-1,2,3,4-tetrahydrocarboline naphthalene-1,5-disulfonate of formula 1

    The invention is also directed to the novel drug substance, Pharmaceutical formulation comprising the novel drug substance, and to the method for its preparation, to the novel medicaments, and method for treatment of CNS diseases including neurodegenerative diseases and cognitive disorders at humans and warm blooded animals.

    摘要翻译： 本发明是针对新颖的配体与广泛的药理学活性，包括活性GPCR受体，离子通道和单胺转运蛋白代表3-甲基9-苄基-1,2,3,4-四氢萘-1,5-二咔啉 因此式1的本发明的二磺酸被引导到新的药物物质，药物制剂，包括新颖的药物物质，和其制备的方法中，对新颖的药物，以及用于治疗CNS疾病的方法，包括神经变性疾病和在认知障碍 人和温血动物。

    SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF
    7.
    发明公开
    SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开
    取代的3-芳基磺酰基 - 吡唑并[1,5-A]嘧啶，血清素5-HT6受体拮抗剂和方法的生产和使用

    公开(公告)号：EP2351756A1

    公开(公告)日：2011-08-03

    申请号：EP09819452.5

    申请日：2009-10-06

    申请人： Ivashchenko, Andrey Alexandrovich ,  Alla Chem, LLC.

    发明人： IVASHCHENKO, Alexander Vasilievich ,  SAVCHUK Nikolay Filippovich ,  LAVROVSKY Yan ,  MITKIN, Oleg Dmitrievich ,  KADIEVA Madina Georgievna

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/18 ,  A61P25/26 ,  A61P25/16 ,  A61P25/08 ,  A61P9/10 ,  A61P3/04 ,  A61P3/08 ,  A61K9/48 ,  A61K9/08

    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-HT 6 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-HT 6 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; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; R 2 represents hydrogen, halogen, optionally substituted C 1 -C 3 alkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; R 3 represents hydrogen, optionally substituted C 1 -C 3 alkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X = S or X = NH, at least one of R 1 , R 2 or R 3 represent substituted C 1 -C 3 alkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R 1 , R 2 or R 3 represent hydrogen; R 4 represents C 1 -C 3 alkyl; R 5 represents hydrogen, one or two halogens, C 1 -C 3 alkyl or optionally substituted hydroxyl.

    摘要翻译： 本发明涉及新颖的substituiertem 3-芳基磺酰基 - 吡唑并[1,5-A]通式1的嘧啶，其药学上可接受的盐和/或水合物，五羟色胺5-HT 6受体拮抗剂和药物组合物，并且因此方法 用于特别是在人类和温血动物的所有发病预防和治疗中枢神经系统的各种疾病的，其与血清素5-HT 6个受体相关的疾病，阿尔茨海默氏症，帕金森氏病，亨廷顿氏病，精神分裂症，以及其它神经变性疾病， 认知障碍和肥胖。 在通式1：其中：X = S，SO或NH; 的R 1 darstellt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 darstellt氢，卤素，任选取代的C 1 -C 3烷基，取代的羟基，或aryldiazenyl任选取代的氨基; ，R 3 darstellt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基团，此外，在情况下，当X = S或X = NH，R 1，R中的至少一个2或R 3代表 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，aryldiazenyl，或至少两个R 1，R 2或R 3表示氢; ，R 4 darstellt C 1 -C 3烷基; 的R 5 darstellt氢，一个或两个卤素，C 1 -C 3烷基或任意取代的羟基。

    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.
    发明公开
    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
    血清素5-HT6受体的2-氨基-3-磺酰基 - 四氢 - 吡唑并[1,5-A]吡啶 - 嘧啶拮抗剂，其生产方法和用途

    公开(公告)号：EP2287163A1

    公开(公告)日：2011-02-23

    申请号：EP09742910.4

    申请日：2009-04-30

    申请人： Ivashchenko, Andrey Alexandrovich ,  Alla Chem, LLC.

    发明人： KYSIL, Volodymyr Mikhailovich ,  SAVCHUK, Nikolay Filippovich ,  IVASHCHENKO, Alexander Vasilievich

    IPC分类号： C07D471/14 ,  A61P25/22 ,  A61K31/519 ,  A61P25/24 ,  A61P25/18 ,  A61P25/28 ,  A61P25/08 ,  A61P3/08 ,  A61P25/26 ,  A61P9/10 ,  A61P25/16 ,  A61P3/04

    CPC分类号： C07D471/14 ,  A61K31/519

    摘要： The invention relates to serotonin 5-HT 6 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-HT 6 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 represents optionally substituted aryl or optionally substituted heteroaryl; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, C 1 -C 4 alkyloxycarbonyl; R 2 represents hydrogen, halogen or optionally substituted C 1 -C 3 alkyl ; R 1 3 and R 2 3 represent optionally alike: hydrogen, optionally substituted C 1 -C 3 alkyl or R 1 3 and R 2 3 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.

    摘要翻译： 本发明涉及血清素5-HT 6受体拮抗剂 - 新的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，含有所述药物作为所述化合物的药物和药物组合物， 预防和治疗人和动物中中枢神经系统的各种疾病的发病机理与血清素5-HT 6受体相关，包括认知和神经退行性疾病。 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 ，通式2的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代表任选取代的芳基或任选取代的杂芳基; R 1代表氢，任选取代的C 1 -C 3烷基，C 1 -C 4烷氧基羰基; R2代表氢，卤素或任选取代的C1-C3烷基; R13和R23任选相同：氢，任选取代的C1-C3烷基或R13和R23与它们所连接的氮原子一起形成任选取代的氮杂杂环。