Patent RU-2319696-C2 (RU)
Title: Cis-2,4,5-triarylimidazolines
Inventor: KHEJLI GREGORI DZHEJ
IPC: C07D401/12
Filed: 2004-06-08
Granted: 2008-03-20
Abstract: FIELD: organic chemistry, pharmacy. 
     SUBSTANCE: invention relates to novel compounds of the formula:   wherein X 1  and X 2  represent halogen atom; X 3  represents lower alkoxy group; R is chosen from group consisting of the following substances:         and   wherein R 1  is chosen from group consisting of N-lower alkyl, unsubstituted heterocycle and heterocycle substituted with one or some substitutes chosen from group consisting of -NH 2 , -NH-C(O)-lower alkyl, -C(O)-lower alkyl, -C(O)-lower alkoxy group, oxo group, heterocycle and lower alkyl substituted with hydroxy group; R 2  is chosen from hydrogen atom, methyl and lower alkoxy group; R 3  is chosen from group consisting of heteroaryl, heterocycle, lower alkyl substituted with R 7 , aryl, lower alkoxy group and lower alkyl; R 4  is chosen from group consisting of -C(O)-lower alkoxy group, lower alkoxy group, CH 2 -heterocycle, CH 2 -heterocycle substituted with oxo group, aryl, -NH-C(S)-N-lower alkyl, -NH-C(S)-N-aryl, -NH-C(O)-R 8 , N-alkyl substituted with -C(O)-R 16  and trifluoromethyl; R 5  is chosen from group consisting of oxo group, heteroaryl, aryl substituted with a substitute chosen from lower alkoxy group and fluorine atom, -C(S)-N-lower alkyl, -C(S)-N-aryl, -C(O)-R 13 , -SO 2 -R 14  and lower alkyl substituted with a substitute chosen from R 15  and -C(O)-R 16 ; R 6  is chosen from group consisting of lower alkyl substituted with N-lower alkyl, lower alkyl substituted with heterocycle, lower alkyl substituted with heterocycle substituted with one or two substitutes chosen from lower alkyl, lower alkyl substituted with hydroxyl and oxo group; R 7  is chosen from group consisting of cyano, hydroxy group, heteroaryl, heterocycle substituted with oxo group and aryl substituted with a substitute chosen from group consisting of -SO 2 NH, lower alkoxy and hydroxy group; R is chosen from group consisting of N-lower alkyl, heterocycle, heterocycle substituted with a substitute chosen from group consisting of oxo group, -C(O)-NH 2  and -C(O)-NH-lower alkyl, CH 2 -R 9  and CH 2 -R 10 ; R 9  is chosen group consisting of -NH 2 , N-lower alkyl, N-lower alkyl substituted with a substitute chosen from hydroxy and lower alkoxy group; R 10  is chosen from heterocycle and heterocycle substituted with one or some groups chosen from group consisting of -C(O)-NH 2 , lower alkyl substituted with hydroxy group, hydroxy group; R 13  is chosen from group consisting of heteroaryl, heteroaryl substituted with one or some substitutes chosen from group consisting of lower alkyl, aryl and halogen atom, heterocycle, heterocycle substituted with one or some substitutes chosen from group consisting of lower alkyl, aryl and halogen atom, -C(O)-lower alkyl, -C(O)-NH 2 , -C(O)-N-lower alkyl and lower alkyl substituted with -O-C(O)-CH 2 ; R 14  is chosen from group consisting of trifluoromethyl, lower alkyl, aryl substituted with lower alkyl, -NH 2 , N-lower alkyl, N-lower alkyl substituted with a substitute chosen from lower alkoxy, cyano, amino group and trifluoromethyl, heteroaryl, heteroaryl substituted with a substitute chosen from group consisting of amino group, halogen atom, -C(O)-lower alkoxy group, lower alkyl and lower alkyl substituted with hydroxyl, heterocycle and heterocycle substituted with a substitute chosen from group consisting of hydroxy, oxo group; R 15  is chosen from group consisting of lower alkoxy, cyano group, trifluoromethyl, N-lower alkyl, -SO 2 -lower alkyl, -C(O)-lower alkyl,  heteroaryl and heterocycle; R 16  is chosen from group consisting of lower alkoxy group, -NH 2 , N-lower alkyl, N-lower alkoxy group, N-lower alkenyl, N-benzyloxy group, N-lower alkyl, substituted R 18 , heterocycle and heterocycle substituted with one or two substitutes chosen from group consisting of hydroxy, alkoxy group, trifluoromethyl, -C(O)-lower alkyl, -C(O)-NH 2 , -C(O)-N-lower alkyl, lower alkyl substituted with hydroxy and oxo group; R 18  is chosen from group consisting of lower alkoxy, cyano group, trifluoromethyl, heterocycle and hydroxyl. Also, invention relates to a pharmaceutical composition possessing anti-proliferative activity based on these compounds. Invention provides synthesis of novel compounds possessing valuable biological properties. 
     EFFECT: valuable properties of compounds and pharmaceutical composition. 
     28 cl, 243 ex