Alexander Vasillevich Ivashtchenko;Andrey Alexandrovich Ivashchenko;Nikolay Filippovich Savchuk
发明人:
Alexander Vasillevich Ivashtchenko,Andrey Alexandrovich Ivashchenko,Nikolay Filippovich Savchuk
申请号：
US13573818
公开号：
US08829009B2
申请日:
2012.10.09
申请国别(地区):
US
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-HT6 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-HT6 receptors.In general formula 1R1 and R3 independently of each other represent C1-C3 alkyl or phenyl； R2 represents hydrogen or C1-C3 alkyl； R41, R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41 and R42 together with the nitrogen atom they are attached to form optionally substituted heterocyclyl； Ar is aryl selected from phenyl, optionally substituted with Ri5 that is one or two optionally identical substituents selected from hydrogen, lower alkyl, trifluoromethyl or halogen； or optionally substituted 5-6-membered heteroaryl, containing as the heteroatom nitrogen or sulfur atom.
