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    • 111. 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
    • 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
    • EP2351756A1
    • 2011-08-03
    • EP09819452.5
    • 2009-10-06
    • Ivashchenko, Andrey AlexandrovichAlla Chem, LLC.
    • IVASHCHENKO, Alexander VasilievichSAVCHUK Nikolay FilippovichLAVROVSKY YanMITKIN, Oleg DmitrievichKADIEVA Madina Georgievna
    • C07D487/04A61K31/519A61P25/28A61P25/18A61P25/26A61P25/16A61P25/08A61P9/10A61P3/04A61P3/08A61K9/48A61K9/08
    • C07D487/04
    • 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.
    • 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。