| 摘要 |
FIELD: chemistry.SUBSTANCE: invention is related to cycloalkenylarylic derivatives of formula 1 or their isomers, in which Band Beach independently are N or C, Note here that both Band Bcannot be N, and if one of Band Bis N, then Ror Ris absent; Rand Reach independently represent H,-F,-OH,-NH, -C(=O)H,-CHOH,-OC-C-alkyl, -SC-C-alkyl, etc. Rand Rtogether 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 R; Ris -H, -F, -OH, -C--Calkyl or -OC-C-alkyl; Ris -H, halogen, -CN, -NO, -C-Calkyl, -C-Ccycloalkyl,-cikloprop-1-yl-R, -cykloprop-1-yl-C(O)-NRR, -OR, -CHOR, -CHNRR, -SR, -C(=O)R, -COR, -CHRCOR, -C(=O)NRRetc.; Ris -H; Ris -H or -C-Calkyl; Ris -CF; p is an integer ranging from 0 to 2; Aand Aeach independently represent -O-, -(CRR)- or -NR; Ais -(CH)-; 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 -C-Calkyl,-C-Ccycloalkyl or -C-Calkyl are unsubstituted or substituted with one or more substitutes selected from a group, consisting of halogen, -OH, CN,-COH,-C(=O)CH, -OC(= O)CH, -C-Calkyl 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 |
