发明名称 DERIVATIVES OF 2-DEOXY-2,3-DIDEHYDRO-N-ACETYLNEURAMINIC ACID, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT
摘要 FIELD: organic chemistry. SUBSTANCE: invention proposes derivatives of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid of the formula (I) <EMI ID=0.53 HE=36 WI=57 TI=CHI> where R is azide or group -NR<SP>6b</SP>R being R is hydrogen, C<SB>1-6</SB>--alkyl or allyl; R is NHCOR where R is C<SB>1-6</SB>-alkyl, or their pharmaceutically acceptable salts and ester salts. Method of synthesis of compounds of the formula (I) involves interaction of derivative of the formula (III) <EMI ID=0.54 HE=27 WI=63 TI=CHI> protected by carboxy- and hydroxy-groups where R has above indicated value; OL - group to be removed with nucleophilic group followed by conversion to amine, guanidine, salt, ester of ester salt. Invention proposes also pharmaceutical composition showing antiviral activity with respect to ortho-paramyxoviruses that contains a compound of the formula (I) as an active component taken at effective amount. Invention proposes also a method of treatment of mammals including human with viral infections by administration of compounds of the formula (I) at the dose 0.01-750 mg/kg body mass/day in respiratory ways or by intranasal route. EFFECT: improved method of synthesis, enhanced effectiveness of compounds synthesized. 15 cl, 15 dwg, 3 tbl, 24 ex
申请公布号 RU2119487(C1) 申请公布日期 1998.09.27
申请号 RU19920016283 申请日期 1991.04.24
申请人 BIOTA SAJENTIFIK MENEDZHMENT PTI LTD. 发明人 LORENS MARK FON ITSSHTEJN;VEN-JANG VU;TO VAN FAN;BAZIL' DANILEK;BETTI DZHIN
分类号 C07D309/30;A61K31/00;A61K31/196;A61K31/34;A61K31/35;A61K31/351;A61K31/38;A61K31/382;A61K31/41;A61K31/435;A61K31/44;A61K31/505;A61K31/7012;A61P31/00;A61P31/12;A61P31/14;C07C47/225;C07C47/42;C07C225/20;C07C233/52;C07C309/25;C07C317/12;C07C321/22;C07D;C07D211/70;C07D211/72;C07D211/74;C07D211/78;C07D211/84;C07D239/26;C07D257/02;C07D257/04;C07D309/20;C07D309/22;C07D309/26;C07D309/28;C07D335/02;C07D401/04;C07D401/14;C07D405/04;C07D405/14;C07D409/04;C07D409/14;C07D498/04;C07F9/655;C07H7/033;(IPC1-7):C07D309/30 主分类号 C07D309/30
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