DERIVATIVES OF OXAZOLIDINONE CARBOXYLIC ACID, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 2000 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of oxazolidinone carboxylic acid of the formula (I) where R¹ is CN, CSN-R⁶R⁷, C(=NH)SA, C(=NH)-R⁶R⁷, CH₂NR⁶R⁷, C(=NH)NHOH, CH₂-NHCOPh-E, CH₂-NHCONHPh-E or D, ; R² is OH, CH₂Cl or where E is CN, CSNH₂, C(=NH)SA, C(=NH)NH₂; X is OH, OA, AS, and where Y is CH₂ or C=O; R³ is (CH₂)_m-COOR⁵; m = 1, 2; R⁴ is (CH₂)_p-COOR⁵ or (CH₂)_q O (CH₂)_r COOR⁵ where n = 3; p = 0, 1; q = 0; r = 1 or 2; Ph is phenylene; AS is amino acid residue taken among the group consisting of Ala, β-Ala, Asp, Phe, Tyr, Tyr(OMe), N-phenethyl-β-Ala; R⁵ is H, A; R⁶ and R⁷ each is hydrogen atom; A is C₁-C₆-alkyl and their physiologically acceptable salts, enantiomers or diastereomers. These compounds inhibit fibrinogen binding with corresponding receptors and can be used for treatment of patients with thrombosis, osteoporosis, tumor diseases, apoplexy, heart infarction, inflammations, arteriosclerosis and osteolytic diseases. Invention describes method of their synthesis, pharmaceutical composition and method of its preparing. EFFECT: new compounds indicated above, improved method of synthesis and preparing, valuable medicinal and pharmacological properties. 5 cl, 34 ex