| abstract |
FIELD: organic chemistry, amino acids, pharmacy. SUBSTANCE: invention relates to group of novel compounds heterocyclic derivatives of glycyl-beta-alanine of the general formula (I): or pharmaceutical salt of this compound wherein is 5-8-membered monocyclic heterocyclic, optionally saturated ring comprising from 1 to 4 heteroatoms taken among the group including nitrogen and sulfur atoms being X 1 is taken among the group including: CH, CH 2 , N, NH, O and S under condition that is not pyrrolidinyl when V means NH; A represents group of the formula: wherein Y 1 is taken among group including N-R 2 being R 2 means hydrogen atom; R 2 means hydrogen atom, R 7 when is not common with R 2 ; and R 8 means hydrogen atom, alkyl substituted with alkoxy-group, or R 2 in common with R 7 forms 4-12-membered heterocycle comprising 2 nitrogen atoms optionally substituted with one or some substituents taken among group including hydroxy-, C 1 -C 10 -alkyl, halide, spirodioxalane; A means the group: wherein R 2 in common with R 7 form 5-8-membered heterocycle comprising two nitrogen atoms; R 5 means hydrogen atom; R 8 means alkyl optionally substituted with alkoxy- group; or A means group: wherein R 2 in common with R 7 form 5-8-membered heterocycle comprising 2 nitrogen atoms optionally substituted with hydroxy-group; R 8 is alkyl substituted with alkoxy-group; V means N-(R 6 ); R 6 is hydrogen atom; Y and Z mean hydrogen atom; t = 0; n and p = 1, 2; R means X-R 3 wherein X is O-; R 3 is hydrogen atom, alkyl; R 1 is taken among group including aryl, alkyl optionally mono- or multiple-substituted with halide, alkyl, hydroxy-group; monocyclic heterocycle; halogenalkyl; R 11 means hydrogen atom, or pharmaceutically acceptable salt of this compound. Invention relates also to pharmaceutical composition eliciting properties of antagonist of α V β 3 -integrin and to method for treatment of diseases mediated by α V β 3 -integrin in mammals. EFFECT: valuable medicinal properties of compounds. 22 cl, 1 tbl, 60 ex |