发明名称 -CYCLODEXTRINE CLATHRATE COMPLEX WITH 5-HYDROXY-4-AMINOMETHYL-1 -CYCLOHEXYL(OR CYCLOHEPTYL)-3-ALKOXYCARBONYLINDOLE DERIVATIVE, METHOD FOR PREPARING IT (VERSIONS), PHARMACEUTICAL COMPOSITION AND DRUG
摘要 FIELD: medicine, pharmaceutics. ^ SUBSTANCE: invention refers to a new -cyclodextrine clathrate complex (an inclusion compound) with 5-hydroxy-4-aminomethyl-1-cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative: -cyclodextrine 1:1 to 1:5, preferentially at the relation of 1:1 to 1:3 of general formula (I): wherein X means - hydrogen, chlorine, iodine, n=1 or 2, R3-C1-C3 alkyl, ALK means C1-C6 alkyl group, R1, R2 are independently specified in C1-C4-alkyl, preferentially methyl, or R1 and R2 together with a nitrogen atom (i.e. group - NR1R2) means the groups described by formulas: wherein Bn is benzyl, a Ph is phenyl with the molar ratio of 5-hydroxy-4-aminomethyl-1-cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative: -cyclodextrine 1:1 to 1:5, preferentially 1:1 to 1:3, especially preferentially in the relation of 1:2. The clathrate complex may represent nanoparticles of size not less than 100 nm. There are preferential clathrate complexes wherein 5-hydroxy-4-aminomethyl-1-cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative represents 1-cyclohexyl-4-aminomethyl-5-hydroxy-2-methyl-1H-indole-3-carboxylic acid ethyl ester. The new clathrate complexes possess antiviral action and exhibit high activity versus influenza viruses. The invention also involves a pharmaceutical composition and a drug based on the clathrate complexes. Besides, the invention refers to liquid-phase and solid-phase synthesis of the clathrate complexes. ^ EFFECT: preparing the compounds which possess antiviral action and exhibit high activity versus influenza viruses. ^ 20 cl, 2 ex, 2 tbl, 8 dwg
申请公布号 RU2464042(C1) 申请公布日期 2012.10.20
申请号 RU20110112073 申请日期 2011.03.31
申请人 OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOST'JU "NAUCHNO-ISSLEDOVATEL'SKAJA KOMPANIJA "MEDBIOFARM" 发明人 VOROB'EV IL'JA VLADIMIROVICH;KHOMICHENOK VIKTOR VLADIMIROVICH;PODGORODNICHENKO VLADIMIR KONSTANTINOVICH;TSYB ANATOLIJ FEDOROVICH;ROZIEV RAKHIMDZHAN AKHMETDZHANOVICH;GONCHAROVA ANNA JAKOVLEVNA
分类号 A61K31/404;A61K31/724;A61K47/48;A61P31/12;A61P31/16;B82B3/00;C07D209/42;C08B37/16 主分类号 A61K31/404
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