发明名称 OXAZOLIDINONE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND A METHOD OF ITS PREPARING
摘要 FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of oxazolidinone of the formula (I) <EMI ID=0.205 HE=27 WI=36 TI=CHI> where R means free or once substituted with CN, H<SB>2</SB>N-CH<SB>2</SB>,H<SB>2</SB>N-C(=NH)- or H<SB>2</SB>N-C(=NH)-NH-CH<SB>2</SB>, phenyl residue; X means O; B means a group of the formula (II) <EMI ID=0.206 HE=18 WI=42 TI=CHI> where A means alkyl with 1-6 C-atoms; R means H or A; R means H or (CH<SB>2</SB>)<SB>n</SB>-COOR ; 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) <EMI ID=0.207 HE=27 WI=39 TI=CHI> where R 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, NH<SB>2</SB>, NAH or salt-like residue produced from OH or SH; or compound of the formula (V): R -NH-CH<SB>2</SB>--CH(OH)-CH<SB>2</SB>-X-B where R , 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
申请公布号 RU2125560(C1) 申请公布日期 1999.01.27
申请号 RU19940034124 申请日期 1994.09.23
申请人 MERK PATENT GMBKH 发明人 JOAKHIM GANTE;KHORST JURASHIK;PETER RADDATTS;KHANNS VURTSIGER;GVIDO MEL'TSER;SABINE BERNOTAT-DANELOVSKI
分类号 A61K31/42;A61K31/421;A61K31/44;A61K31/496;A61K31/505;A61P7/02;A61P9/08;A61P9/10;A61P19/10;A61P29/00;A61P33/04;A61P35/00;A61P43/00;C07D263/20;C07D263/24;C07D413/12;(IPC1-7):C07D263/20 主分类号 A61K31/42
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