HETEROCYCLIC DERIVATIVES OF GLYCYL-BETA-ALANINE AS ANTAGONISTS OF VITRONECTIN Russian patent published in 2003 - IPC

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 X¹ is taken among the group including: CH, CH₂, N, NH, O and S under condition that is not pyrrolidinyl when V means NH; A represents group of the formula: wherein Y¹ is taken among group including N-R² being R² means hydrogen atom; R² means hydrogen atom, R⁷ when is not common with R²; and R⁸ means hydrogen atom, alkyl substituted with alkoxy-group, or R² in common with R⁷ forms 4-12-membered heterocycle comprising 2 nitrogen atoms optionally substituted with one or some substituents taken among group including hydroxy-, C₁-C₁₀-alkyl, halide, spirodioxalane; A means the group: wherein R² in common with R⁷ form 5-8-membered heterocycle comprising two nitrogen atoms; R⁵ means hydrogen atom; R⁸ means alkyl optionally substituted with alkoxy- group; or A means group: wherein R² in common with R⁷ form 5-8-membered heterocycle comprising 2 nitrogen atoms optionally substituted with hydroxy-group; R⁸ is alkyl substituted with alkoxy-group; V means N-(R⁶); R⁶ is hydrogen atom; Y and Z mean hydrogen atom; t = 0; n and p = 1, 2; R means X-R³ wherein X is O-; R³ is hydrogen atom, alkyl; R¹ is taken among group including aryl, alkyl optionally mono- or multiple-substituted with halide, alkyl, hydroxy-group; monocyclic heterocycle; halogenalkyl; R¹¹ means hydrogen atom, or pharmaceutically acceptable salt of this compound. Invention relates also to pharmaceutical composition eliciting properties of antagonist of α_Vβ₃-integrin and to method for treatment of diseases mediated by α_Vβ₃-integrin in mammals. EFFECT: valuable medicinal properties of compounds. 22 cl, 1 tbl, 60 ex