DERIVATIVES OF 2,3-BENZODIAZEPINE, INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS AND AGENT ELICITING INHIBITORY ACTIVITY WITH RESPECT TO AMPA-RECEPTORS

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes derivatives of 2,3-benzodiazepine of the general formula (I) where R¹ means hydrogen atom, nitro-group, halogen atom, NH₂; R² means hydrogen atom; R³ and R⁴ are similar or different and mean hydrogen, halogen atom, C_1-6-alkoxy-group, PO₃R¹³R¹⁴, C_1-6-alkanoyl-group that can be if necessary substituted with halogen atom or C_1-6-alkoxy-group, C_1-6-alkyl, C_3-7-cycloalkyl, phenyl or pyridyl; R¹³, R¹⁴ are similar or different and mean hydrogen atom or C_1-6-alkyl; X means hydrogen or halogen atom; Y means C_1-6-alkoxy- group, or X and Y in common mean -O-(CH₂)_n-O- where n = 1; A in common with nitrogen atom forms saturated or nonsaturated five-membered heterocycle that can include 1-3 nitrogen atoms or one nitrogen atom and one oxygen atom and/or one or two carbonyl groups, and also their isomers and physiologically acceptable salts; intermediate compounds (IIa) and (IIIa) used in their synthesis and agent eliciting inhibitory activity with respect to AMPA-receptors and containing the compound (I). Compounds (I) are inhibitors of AMPA-receptors and can be used for treatment of patients with diseases of central nervous system. EFFECT: valuable pharmacological and medicinal properties of compounds. 5 cl, 57 ex