PYRAZOLO[1,5-A]PYRIMIDINES AND PYRAZOLO[1,5-A]- TRIAZINES AND MEDICINAL AGENTS Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new and eliciting selective affinity to 5HT₆-receptors pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5- a]triazines wherein X means =C(R⁴)- or = N-; R¹ means phenyl optionally substituted with one or some radicals of lower alkyl, halogen atom, lower alkoxy-group, tolyl, pyridyl or thiophenyl; R² means hydrogen atom, lower alkyl, lower thioalkyl or hydroxy-lower alkoxy-group; R³ means amino-lower alkylamino-group, di-lower alkylamino-group, piperazinyl optionally substituted with one or some radicals of lower alkyl, benzyl, phenyl or hydroxy-lower alkyl, morpholinyl, imidazolyl, (CH₃)₂N(CH₂)_nNH-, (CH₃)₂N(CH₂)_nO- or morpholinyl-(CH₂)_nO- wherein n = 2 or 3; R⁴ means hydrogen atom, lower alkyl or hydroxy-lower alkyl; R⁵ means hydrogen, halogen atom, lower alkyl, C₃-C₆-cycloalkyl, lower alkyl-lower alkoxy-group, hydroxy-lower alkyl-lower alkoxy-group, (CH₃)₂N(CH₂)_nNH-, piperazinyl optionally substituted with lower alkyl, piperazinylmethyl optionally substituted with lower alkyl, morpholinyl, morpho- linylmethyl, di-(lower)-alkylamino-group or di-lower alkylamino- -lower alkyl; or R⁴ and R⁵ in common mean group -(CH₂)_m- or -CH₂-S-CH₂-; m = 3 or 4; X means =C(R⁴)- or = N-; R¹ means phenyl optionally substituted with one or some radicals of (lower)-alkyl, halogen atom, (lower)-alkoxy- -group, tolyl, pyridyl, naphthyl or thiophenyl and also their pharmaceutically acceptable salts. Compounds of the formula (I) wherein R³ means amino-group, piperazinyl, methylpiperazinyl are preferable. Medicinal agent comprises compound of the formula (I) and therapeutically inert carrier. EFFECT: valuable medicinal properties of compounds. 11 cl, 3 sch, 1 tbl, 1 ex