LI So KHi,ЛИ Со Хи,O CHun Tek,О Чун Тэк,LI CHe Kvan,ЛИ Че Кван,LI CHe Von,ЛИ Че Вон,PE Soyal,ПЭ Соял,KHA Nina,ХА Нина,LI Sera,ЛИ Сера
申请号：
RU2013145418/04
公开号：
RU0002597266C2
申请日:
2012.04.12
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
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 Ra 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 derivati
