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    SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND USE THEREOF
    2.
    发明公开
    SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR THE PRODUCTION AND USE THEREOF 有权
    替代物2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚，VERFAHRENFÜRIHRE HERSTELLUNG UND VERWENDUNG

    公开(公告)号：EP2145887A2

    公开(公告)日：2010-01-20

    申请号：EP08753899.7

    申请日：2008-04-01

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

    发明人： IVASHCHENKO, Andrey Alexandrovich ,  IVACHTCHENKO, Alexandre Vasilievich ,  TKACHENKO, Sergey Yevgenievich ,  FROLOV, Evgueni Borisovich ,  MITKIN, Oleg Dmitrievich ,  KRAVCHENKO, Dmitri Vladimirovich ,  OKUN, Ilya Matusovich ,  SAVCHUK, Nikolay Filippovich ,  LAVROVSKY, Yan

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P37/08 ,  A61P37/02

    CPC分类号： A61K31/437 ,  A61K31/444 ,  C07D471/04

    摘要： The invention relates to antagonists of serotonin 5-HT 6 receptors simultaneously regulating homeostasis of Ca +2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1:

    R 1 represents amino group substituent selected from optionally substituted C 1 -C 5 alkyl; R 2 i is one or more substituents selected from hydrogen, halogen, C 1 -C 3 alkyl, CF 3 , OCF 3 ; Ar is phenyl optionally substituted with halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, substituted amino group, or CF 3 ; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group -CH 2 -CH 2 -, ethenyl group -CH=CH-, or ethynyl group -C≡C-. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.

    摘要翻译： 本发明涉及同时调节细胞中Ca 2+离子的体内平衡的5-羟色胺5-HT 6受体的拮抗剂，代表通式中取代的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚 1，其药学上可接受的盐和/或水合物。 在通式1中：R 1表示选自任选取代的C 1 -C 5烷基的氨基取代基; R 2 i是一个或多个选自氢，卤素，C 1 -C 3烷基，CF 3，OCF 3的取代基; Ar是任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，取代的氨基或CF 3取代的苯基; 或在该循环中任选取代的包含1-2个氮原子的芳族6-元杂环; W表示亚乙基-CH 2 -CH 2 - ，乙烯基-CH = CH-或乙炔基-C¡C-。 本发明还涉及选自通式1的化合物，其制备方法，药物组合物及其用途的新型化合物。