SUBSTITUTED 2-AMINO-3-SULFONYL-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIDO-PYRIMIDINES-ANTAGONISTS OF SEROTONIN 5-HT RECEPTORS, METHODS OF PRODUCING AND USING SAID COMPOUNDS Russian patent published in 2010 - IPC C07D471/14 A61K31/519 A61P25/18 A61P25/22 A61P25/24 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to novel antagonists of serotonin 5-HT₆ receptors - substituted 2-amino-3-sulfonyl-6,7,8,9-tetrahydro-pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines of general formula 1 and substituted 2-amino-3-sulfonyl-5,6,7,8-tetrahydro-pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of general formula 2 or their pharmaceutically acceptable salts and/or hydrates, method of producing said compounds and pharmaceutical compositions, medicinal agents and treatment method. In compounds of formula 1 and general formula 2 , Ar is phenyl which is possibly substituted with halogen atoms, or a 6-member nitrogen-containing heteroaryl; R¹ is a hydrogen atom, C₁-C₃alkyl which is possibly substituted with phenyl, C₁-C₅alkoxycarbonyl; R² is a hydrogen atom, halogen or C₁-C₃alkyl; R₁ ³ and R₂ ³ are optionally identical substitutes selected from a hydrogen atom, optionally substituted C₁-C₃alkyl or R₁ ³ and R₂ ³ together with the nitrogen atom with which they are bonded form a nitrogen-containing 6-member saturated heteroaryl optionally substituted with C₁-C₅alkoxycarbonyl, where the said heteroaryl has 1-2 heteroatoms selected from nitrogen.

EFFECT: compounds can be used to prevent and treat diseases of the central nervous system, pathogenesis of which is associated with 5-HT₆ receptors for enhancing mental capacity.

14 cl, 3 tbl, 19 dwg, 16 ex