Substituted 2-amino-3- (sulfonyl) pyrazolo [1,5-a] pyrimidine-serotonin 5-HT6 receptor antagonists, methods for their preparation and uses

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专利权人:

アンドレイ・アレクサンドロビッチ・イワシェンコ;アラ・ケム・エルエルシー;アンドレイ・アレクサンドロビッチ・イワシェンコ

发明人:

アンドレイ・アレクサンドロビッチ・イワシェンコ,イワシェンコ，アレクサンドル・バシリエビッチ,サブチュク，ニコライ・フィリッポビッチ,イワシェンコ,アレクサンドル・バシリエビッチ,サブチュク,ニコライ・フィリッポビッチ

申请号：

JP2010543610

公开号：

JP5575663B2

申请日:

2009.01.23

申请国别(地区):

JP

年份:

2014

代理人:

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-HT 6 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-HT 6 receptors. In general formula 1 Ar represents optionally substituted aryl or optionally substituted heterocyclyl； R 1 and R 3 independently of each other represent C 1 -C 3 alkyl or aryl； R 2 represents hydrogen or C 1 -C 3 alkyl； R 4 1, and R 4 2 independently of each other represent hydrogen, optionally substituted C 1 -C 3 alkyl or optionally substituted phenyl, or R 4 1 and R 4 2 together with nitrogen atom they are attached to form optionally substituted heterocyclyl.

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