SUBSTITUTED 2-ALKYLMINO-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 A61P25/16 A61P25/18 A61P25/24 A61P3/06 

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 2-alkylamino-3-sulfonyl-pyrazolo[1,5-a]pyrimidines, their pharmaceutically acceptable salts and/or hydrates which have serotonin 5-HT₆ receptor antagonist properties and can be used in treating or preventing development of various central nervous system diseases, whose pathogenesis is related to 5-HT₆ receptors, particularly Alzheimer's disease, Parkinson's disease, Huntington disease, schizophrenia, other neurodegenerative diseases, cognitive and anxiety disorders and obesity. In general formula (I):

R¹ and R³ independently denote optionally identical C₁-C₃alkyl, 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-C₃alkyl; R⁴ is C₁-C₃alkyl; R_i ⁵ is a hydrogen atom, one or two identical or different halogen atoms, C₁-C₃alkyl; i is equal to 0, 1 or 2; n is equal to 0, 1, 2 or 3; X is a carboxyl CO₂H, C₁-C₃alkyloxycarbonyl, aminocarbonyl CONR⁶R⁷ or a NR⁶R⁷ amino group; R6 and R7 denote optionally identical hydrogen atom, optionally substituted C₁-C₃ alkyl, C₃-C₇cycloalkyl or an optionally substituted 5-7-member azaheterocyclyl containing 1-2 nitrogen atoms in the ring, where the substitutes are selected from C₁-C₃alkyl; or R⁶ and R⁷ together with the nitrogen atom to which they are bonded form an optionally substituted 5-6-member azaheterocyclyl containing 1-2 nitrogen atoms in the ring, where the substitutes are selected from C₁-C₃alkyl.

EFFECT: obtaining new biologically active compounds.

26 cl, 12 dwg, 4 tbl, 14 ex