OXAZOLIDINONE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND A METHOD OF ITS PREPARING Russian patent published in 1999 - IPC

Abstract RU 2125560 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of oxazolidinone of the formula (I) where R1 means free or once substituted with CN, H2N-CH2,H2N-C(=NH)- or H2N-C(=NH)-NH-CH2, phenyl residue; X means O; B means a group of the formula (II) where A means alkyl with 1-6 C-atoms; R2 means H or A; R3 means H or (CH2)n-COOR2; E means CH; m = 1; n = 0 or 1. Invention proposes also a method of synthesis of compounds of the general formula (I) and their salts. Compound of the formula (III) where R1 is indicated above and Z - Cl, Br, J, OH or reactive esterified OH-group is interacted with compound of the formula (IV): Y-B where B is indicated above; Y - OH, SH, NH2, NAH or salt-like residue produced from OH or SH; or compound of the formula (V): R1-NH-CH2--CH(OH)-CH2-X-B where R1, B and X are indicated above. Invention relates to also a method of preparing pharmaceutical compositions showing activity that inhibits fibrin binding with fibrinogenic receptors and platelet aggregation. Compound of the formula (I) is converted to useful dosing form by treatment with solid, liquid or semiliquid carrier. Synthesized compounds show valuable properties and can be used in medicine for treatment of patients with tumors, thrombosis, inflammations. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 6 cl, 1 tbl

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RU 2 125 560 C1

Authors

Joakhim Gante

Khorst Jurashik

Peter Raddatts

Khanns Vurtsiger

Gvido Mel'Tser

Sabine Bernotat-Danelovski

Dates

1999-01-27Published

1994-09-23Filed