| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes derivatives of 2,3-benzodiazepine of the general formula (I) where R 1 means hydrogen atom, nitro-group, halogen atom, NH 2 ; R 2 means hydrogen atom; R 3 and R 4 are similar or different and mean hydrogen, halogen atom, C 1-6 -alkoxy-group, PO 3 R 13 R 14 , 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; R 13 , R 14 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-(CH 2 ) 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 |