NOVEL DERIVATIVE VITRONECTIN RECEPTOR ANTAGONISTS, SYNTHESIS METHOD THEREOF, USE THEREOF AS MEDICINAL AGENT AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID ANTAGONISTS

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to novel compounds of formula (I) in form of (R) or (S) isomers, separately or in a mixture, as well as their physiologically acceptable salts and hydrates, having vitronectin receptor antagonist properties. In formula (I) ; G denotes Het-NH-CO-, Het-NH-CH₂-, Het-; Het denotes a mono- or bicyclic system, where each ring is a 5- or 6-member aromatic or non-aromatic ring, where at least one of the rings contains 1-2 nitrogen atoms as heteroatoms, where Het is unsubstituted or substituted with R⁹ groups; R¹ denotes H, (C₆-C₁₄)-aryl, (C₆-C₁₄)aryl(C₁-C₄)alkyl; amino, unsubstituted, mono-or disubstituted with alkyl and/or acyl, containing 1-4 C atoms; R² denotes H, halogen, nitro-group; alkyl containing 1-4 C atoms; amino, unsubstituted, mono- or disubstituted with alkyl and/or acyl containing 1-4 C atoms; a -(CH₂)_0-2-OR⁵ group; R³ denotes H, -CO₂R⁵, -SO₂R⁵ or mono- or bicyclic system, where each ring denotes a 5- or 6-member aromatic or non-aromatic ring, where at least one of the rings contains 1-4 heteroatoms selected from N, O or S, unsubstituted or substituted with R9 radicals; R⁴ denotes OH, (C₁-C₈)alkoxy-; amino, unsubstituted, mono- or disubstituted with (C₁-C₄)alkyl; or an aminoacid residue; R⁵ denotes (C₁-C₈)alkyl; (C₆-C₁₄)aryl; (C₆-C₁₄)aryl(C₁-C₄)alkyl; (C₃-C₁₂)cycloalkyl or (C₃-C₁₂)cycloalkyl(C₁-C₄)alkyl; bi- and tricycloalkyl(C₁-C₄)alkyl. Aryls, alkyls, cycloalkyls are not substituted or substituted with R⁹ groups; R⁹ denotes halogen, amino, nitro, hydroxyl, (C¹-C⁴)alkyloxy-, carboxy, (C¹-C⁴)alkyloxycarbonyl-, (C₁-C₈)alkyl, unsubstituted or substituted with halogen atoms; phenyl. The invention also relates to a methods for synthesis of formula (I) compounds, a medicinal agent and a pharmaceutical composition containing said compounds, as well as use thereof in preparing the medicinal agent.;EFFECT: improved properties of the compound.;21 cl, 41 ex