SUBSTITUTED 4-SULPHONYL-PYRAZOLES AND 3-SULPHONYL-PYRAZOLO[1,5-a]PYRIMIDINES-ANTAGONISTS OF SEROTONIN 5-HT RECEPTORS, ACTIVE COMPONENT, PHARMACEUTICAL COMPOSITION, MEDICINAL AGENT AND METHOD OF OBTAINING THEM Russian patent published in 2009 - IPC C07D231/18 C07D487/04 A61K31/519 A61K31/415 A61K31/4155 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to antagonists of serotonin 5-HT6 receptors - substituted 4-sulphonylpyrazoles and 3-sulphonyl-pyrazolo[1,5-a]pyrimidines of general formula 1 or general formula 1.2. These compounds can be used for treating and preventing development of different cognitive and neurodegenerative diseases of the central nervous system. In general formulae 1 and 1.2, 1 1.2 respectively, Ar is optionally substituted phenyl or optionally substituted 5-6-member heteroaryl, containing a nitrogen, oxygen or sulphur atom as a heteroatom; R¹ is a hydrogen atom, optionally substituted C₁-C₅ alkyl, lower acyl or optionally substituted phenyl; R² is an optionally substituted amino group or substituted hydroxy group or R¹, together with the nitrogen atom to which it is bonded, and R², together with the carbon atom to which it is bonded, form a substituted pyrimidine ring; R³ is a hydrogen atom, optionally substituted C₁-C₅alkyl, substituted hydroxyl group or substituted sulphanyl group, R⁵ is a hydrogen atom, optionally substituted C₁-C₅alkyl, substituted hydroxyl group or substituted sulphanyl group, R⁷ and R⁹ independently represent a hydrogen atom, C₁-C₃alkyl or phenyl, R⁸ is a hydrogen atom.

EFFECT: new compounds have useful biological properties.

13 cl, 2 dwg, 4 tbl, 7 ex