CYCLOALKENYLARYLIC DERIVATIVES FOR INHIBITING TRANSPORT PROTEIN CHOLESTERIN ESTERS Russian patent published in 2016 - IPC C07D263/16 C07D263/22 C07D413/10 C07D417/12 A61K31/421 A61P9/00 A61P3/06 A61K31/427 A61K31/422 

FIELD: chemistry.

SUBSTANCE: invention is related to cycloalkenylarylic derivatives of formula 1 or their isomers, in which B¹ and B² each independently are N or C, Note here that both B¹ and B² cannot be N, and if one of B¹ and B² is N, then R² or R⁵ is absent; R¹ and R² each independently represent H,-F,-OH,-NH₂, -C(=O)H,-CH₂OH,-OC₁-C-₆ alkyl, -SC₁-C-₆ alkyl, etc. R¹ and R² together with carbon atoms with which they are connected, can form a 5- or 6-member heterocyclic aromatic or non-aromatic cyclic compound having from 1 to 2 heteroatoms, independently selected from a group consisting of N and O, possibly substituted R⁸; R³ is -H, -F, -OH, -C-₁-C₆ alkyl or -OC₁-C-₆alkyl; R⁴ is -H, halogen, -CN, -NO₂, -C₁-C₆alkyl, -C₃-C₆cycloalkyl,-cikloprop-1-yl-R⁹, -cykloprop-1-yl-C(O)-NR⁷R⁸, -OR⁷, -CH₂OR⁷, -CH₂NR⁷R⁸, -SR⁷, -C(=O)R⁷, -CO₂R⁷, -CHR⁷CO₂R⁸, -C(=O)NR⁷R⁸ etc.; R⁵ is -H; R⁶ is -H or -C₁-C₆ alkyl; R^a is -CF₃; p is an integer ranging from 0 to 2; A¹ and A² each independently represent -O-, -(CR¹¹R¹²)- or -NR¹³; A³ is -(CH₂)_n-; X is S or O; m is an integer ranging from 0 to 3; n is an integer ranging from 0 to 2; q is an integer ranging from 1 to 3, the said -C₁-C₃alkyl,-C₃-C₆cycloalkyl or -C₁-C₆ alkyl are unsubstituted or substituted with one or more substitutes selected from a group, consisting of halogen, -OH, CN,-CO₂H,-C(=O)CH₃, -OC(= O)CH₃, -C₁-C₃alkyl and -Ph. Cycloalkenylarylic derivatives of formula 1 are intended for preparing a pharmaceutical composition for preventing or treating dyslipidemia and atherosclerosis associated with fyslipidemia, by increasing the level of high-density lipoprotein cholesterol (HDL-C) and reducing the level of low density lipoprotein cholesterol (LDL-C) by inhibiting CETR containing cycloalkenylarylic derivatives of formula 1 or isomers together with pharmaceutically acceptable carriers. Invention is also related to a method of producing cycloalkenylarylic derivatives of formula 1 (versions).

EFFECT: technical result is cycloalkenylarylic derivatives having inhibitory activity with respect to transport protein cholesterin esters (CETR).

7 cl, 47 tbl, 2 ex