2-ALKYLAMINO-3-ARYLSULFONYL-PYRAZOLO[1,5-a]PYRIMIDINES, SEROTONIN 5-HT RECEPTOR ANTAGONISTS, METHODS OF PRODUCING AND USING SAID COMPOUNDS Russian patent published in 2010 - IPC C07D487/04 A61K31/519 A61P25/28 A61P25/18 A61P25/24 A61P3/06 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 2-alkylamino-3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of general formula 1, their pharmaceutically acceptable salts and/or hydrates having serotonin 5-HT₆ receptor antagonist properties. The compounds can be used to treat and prevent development of various diseases of the central nervous system, pathogenesis of which is associated with 5-HT₆ receptors, particularly Alzheimer's disease, Parkinson's disease, Huntington disease, schizophrenia, other neurodegenerative diseases and cognitive disorders. In general formula 1 , R¹ is a hydrogen atom, C₁-C₃alkyl, C₁-C₃alkyloxyC₁-C₃alkyl, hydroxyC₁-C₃alkyl, adamantyl, optionally substituted phenyl, 5-6-member heterocyclyl containing a nitrogen or oxygen heteroatom, possibly condensed with a benzene ring; R² is a hydrogen atom, halogen atom, C₁-C₃alkyl, pyridyloxy; R³ is a hydrogen atom; C₁-C₃alkyl; optionally substituted amino group selected from amino, mono- or di(C₁-C₃alkyl)amino, di(C₁-C₃alkyl)aminoC₂-C₃alkylamino, N-[di(C₁-C₃alkyl)aminoC₂-C₃alkyl]-N-(C₁-C₃alkyl)-amino; C₁-C₃alkyloxy, C₁-C₃alkyloxyC₁-C₃alkyl, hydroxyC₁-C₃alkyl; 6-member azaheterocyclyl, possibly containing an extra nitrogen or oxygen atom, a -N(C₁-C₃alkyl) group; R⁴ is C₁-C₃alkyl; R⁵ is a hydrogen atom, one or two halogen atoms or C₁-C₃alkyl.

EFFECT: design of a method of obtaining compounds, a pharmaceutical composition and a medicinal agent for treating and preventing various diseases of the central nervous system.

25 cl, 12 dwg, 3 tbl, 20 ex