| 摘要 |
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, beta-Ala, Asp, Phe, Tyr, Tyr(OMe), N-phenethyl-beta-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
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