SUBSTITUTED 3,5-DIAMINO-4-SULFONYL-PYRAZOLES AND 2-AMINO-3-SULFONYL-PYRAZOLO-[1,5-a]PYRIMIDINES-ANTAGONISTS OF SEROTONIN 5-HT RECEPTORS, METHODS FOR THEIR PRODUCTION AND USE Russian patent published in 2009 - IPC C07D231/44 C07D487/04 A61K31/415 A61K31/4155 A61K31/519 A61P25/24 A61P25/22 A61P25/28 

FIELD: medicine.

SUBSTANCE: invention is related to antagonists of serotonin 5-HT₆ receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R¹ represents atom of hydrogen, unnecessarily substituted C₁-C₅ alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R¹ represents atom of hydrogen, which is unnecessarily substituted C₁-C₅ alkyl; R² ₁,R² ₂, R³ ₁, R³ ₂ independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C₁-C₄ alkyl, unnecessarily substituted phenyl, or R³ ₁ and R³ ₂ together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R¹ together with atom of nitrogen, to which it is bound, and R² ₁ and R² ₂ together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R⁴, R⁵ and R⁶ independently from each other represent atom of hydrogen, unnecessarily substituted C₁-C₃ alkyl or phenyl.

EFFECT: compounds of invention may find application for treatment and prevention of development of conditions and disorders of central nervous system.

13 cl, 11 dwg, 4 tbl, 11 ex