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β-cyclodextrine clathrate complex with 5-hydroxy-4-aminomethyl-1 -cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative, method for preparing it (versions), pharmaceutical composition and drug. RU patent 2464042.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new β-cyclodextrine clathrate complex (an inclusion compound) with 5-hydroxy-4-aminomethyl-1-cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative: β-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: β-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

IPC classes for russian patent β-cyclodextrine clathrate complex with 5-hydroxy-4-aminomethyl-1 -cyclohexyl(or cycloheptyl)-3-alkoxycarbonylindole derivative, method for preparing it (versions), pharmaceutical composition and drug. RU patent 2464042. (RU 2464042):

C08B37/16 - Cyclodextrin; Derivatives thereof

C07D209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

B82B3 - Manufacture or treatment of nano-structures by manipulation of individual atoms or molecules, or limited collections of atoms or molecules as discrete units

A61P31/16 - for influenza or rhinoviruses

A61P31/12 - Antivirals

A61K47/48 - the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

A61K31/724 -

A61K31/404 -

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