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3- (Sulfonyl) pyrazolo 1,5-a pyrimidine-serotonin 5-HT6 receptor antagonists, methods of preparation and use thereof
3- (Sulfonyl) pyrazolo 1,5-a pyrimidine-serotonin 5-HT6 receptor antagonists, methods of preparation and use thereof
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机译：3-（磺酰基）吡唑并[1，5-a]嘧啶-5-羟色胺5-HT6受体拮抗剂，其制备方法和用途
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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-HT 6 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-HT 6 receptor activation. In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R 1 , R 2 and R 3 independently of each other represent hydrogen, C 1 -C 3 alkyl or phenyl; R 4 represents hydrogen, optionally substituted C 1 -C 5 alkyl, substituted hydroxyl group or substituted sulfanyl group.
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机译：本发明涉及新颖的通式1的取代的3-（芳基磺酰基）吡唑并[1,5-a]嘧啶药学上可接受的盐和/或水合物，涉及新颖的5-羟色胺5-HT 6受体拮抗剂，涉及新颖的药物，药物组合物，用于制备和用于治疗和预防中枢神经系统病理状态和疾病的药物和方法，其发病机理与5-羟色胺5-HT 6受体活化有关。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代表氢，任选取代的C 1 -C 5烷基，取代的羟基或取代的硫烷基。
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