SUBSTITUTED 2-ALKYLSULFANYL-3-SULFONYL-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 A61P25/24 A61P25/16 A61P25/18 A61P3/04 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel substituted 2-alkylsulfanyl-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. In general formula 1 , R¹ and R³ independently denote optionally identical C₁-C₃ alkyl, and R² is a -(CH₂)_nX group or R¹ and R³ independently denote different substitutes selected from C₁-C₃ alkyl or a -(CH₂)_nX group, and R² is a hydrogen atom or C₁-C₃ alkyl; R⁴ is C₁-C₃ alkyl; R_i ⁵ is a hydrogen atom, one or two identical or different halogen atoms, C₁-C₃ alkyl; equals 0, 1 or 2; n equals 0, 1, 2 or 3; X is a carboxyl CO₂H, C₁-C₃ alkyloxycarbonyl, aminocarbonyl CONR⁶R⁷ or amino group NR⁶R⁷; except compounds in which R³ is a -(CH₂)_nX group, where X is an amino group NR⁶R⁷ and n equals 0; R⁶ and R⁷ are optionally identical and denote a hydrogen atom, optionally substituted C₁-C₅ alkyl or R⁶ and R⁷ together with the nitrogen atom with which they are bonded form an optionally substituted 6-member azaheterocyclyl containing 1-2 nitrogen atoms in the ring, where the substitute is selected from C₁-C₃ alkyl.

EFFECT: obtaining compounds which can be used in treating diseases of the central nervous system during prevention or treatment of cognitive disorders, neurodegenerative diseases, psychiatric disorders, have anxiolytic and nootropic effect and can be used to prevent and treat anxiety disorders and enhance mental capacity.

25 cl, 2 tbl, 12 ex