DERIVATIVES OF XANTHINE WITH TERMINAL AMINATED ALKYNOL SIDE CHAINS AND MEDICINAL AGENT Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of xanthine with terminal aminated alkynol side chains of the formula (I) as individual stereoisomers or mixtures of stereoisomers exhibiting neuroprotective effect. Indicated compounds show the large therapeutical potential. In compounds of the general formula (I) R¹ and R³ mean alkynol residue of the formula (Ia) ; R² means: a) linear or branched C_1-5-alkyl; b) C_3-6-cycloalkyl; c) C_4-8-cycloalkylalkyl; R⁴ means hydrogen atom or C_1-3-alkyl; R⁵ and R⁶ mean independently each of other: a) hydrogen atom; b) C_1-6-alkyl; c) phenyl-C_1-5-alkyl; or R⁵ and R⁶ in common with nitrogen atom to which they are linked form 5-6-membered saturated cycle; or R⁵ and R⁶ in common with nitrogen atom to which they are linked form 5-6-membered saturated cycle where one -CH₂-group in cycle is replaced with a residue among group O, NR¹³ where R¹³ means hydrogen atom, (C_1-3)-alkylcarbonyl, (C_1-4)-alkyl; A means linear or branched (C_1-6)-alkylene; or R¹ means alkynol residue of the formula (Ib) where R⁷ means (C_1-6)-alkyl; Z^- means anion of physiologically acceptable inorganic or organic acid; R²-R⁶ have the above-indicated values; or R¹ means alkynol residue of the formula (Ia); R³ means: a) hydrogen atom or b) R⁸ where R⁸ means linear or branched (C_1-6)-alkyl; R²-R⁷, A and Z^- have the above-indicated values. Invention relates also to medicinal agent comprising therapeutically effective dose of at least one compound of the formula (I) in the form of individual stereoisomers or as mixtures of stereoisomers. EFFECT: valuable medicinal and therapeutic potential and properties of compounds. 9 cl, 3 tbl