TRITERPENE DERIVATIVES OF LUPEOL TYPE AS ANTIVIRAL PREPARATIONS Russian patent published in 2015 - IPC C07J63/00 A61K31/56 A61P31/12 A61P31/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel triterpene derivatives of formula

and formula

active with respect to HIV, as well as HIV-mediated diseases, and to an intermediate compound of formula

In the general formula (I) R stands for H, substituted or non-substituted C_1-6 alkyl, benzyl or substituted or non-substituted C_4-5 cycloalkyl and preferably R is substituted with R^a; R' stands for H, substituted or non-substituted C_1-6 alkyl, substituted or non-substituted C_4-5 cycloalkyl, substituted or non-substituted C_4-5 cycloalkenyl, substituted piperazinyl, substituted piperidinyl, substituted 8-azabicyclo[3.2.1]octane, 4-ethyl-2,2,6-trimethyl-1.3-dioxane, hexane-2,4-diol or (S)-1-((4aS,8aS)-octahydroisoquinolin-2(1H)-yl)-4-phenylbutan-2-ol and preferably R′ can be substituted with R^a; X is selected from a bond and -C(O)-; X₁ is selected from -C(O)-, -C(O)₂- or -C(O)NR"-; Z stands for -O-; Z₁ stands for a bond; Z' stands for H; n equals 0; m equals 1,

″″ stands for a single bond; R₁ stands for H; R₂ stands for -C(=CH₂)(CH₃); R^a stands for cyano, phenyl, benzyl, ethyl, 3-isopropyl-5-methyl-1,2,4-triazole, -C(O)₂R", -C(O)R", -CH₂OR", -C(O)N(R)"₂ or substituted or non-substituted C_1-6 alkyl, where the substituent is selected from -OH, morpholinyl, benzyl, -COOMe, piperazinyl, optionally substituted with ethyl, piperidinyl, optionally substituted with methyl, -COOH, or benzyl; and each R" is independently selected from H, substituted or non-substituted C_1-6 alkyl, methyl 3-methylbutanoate, 3-methylbutanic acid, 4-methylpentanic acid, methyl 4-methylpentanoate, methyl propionate, propanoic acid, 1-morpholinopropan-1-one, 1-(pyrrolidin-1-yl)propan-1-one, 4-ethylpiperazinyl, morpholinyl, piperidinyl, optionally substituted with -COOEt, pyrrolidinyl or benzyl. In formula (2A) X^A1 stands for a bond or -C(O)-; X^A2 stands for a bond, O or NH; R^A1 stands for

Rb stands for substituted or non-substituted C_1-6 alkyl; R^A2 stands for substituted or non-substituted amine, substituted or non-substituted C_4-5 cycloalkyl, substituted or non-substituted C_4-5 cycloalkenyl, 4-ethyl-2,2,6-trimethyl-1,3-dioxane, hexane-2,4-diol, (S)-1-((4aS,8aS)-octahydroisoquinolin-2(1H)-yl)-4-phenylbutan-2-ol or substituted piperazinyl, substituted piperidinyl, substituted 8-azabicyclo[3.2.1]octane, and R^A2 is preferably substituted with R'"; and each R'" represents substituted nitrogen-containing heterocycloalkyl (where alkyl is bound to a nitrogen atom in a heterocycle), where the substituent is selected from methyl, ethyl, -CN, phenyl, benzyl, 3-isopropyl-5-methyl-1,2,4-triazole, -COOH, -COOEt, -COOtBu, -CONHtBu, -CH₂OH or phenyl.

EFFECT: obtaining novel triterpene derivatives.

14 cl, 1 tbl, 105 ex