CIS imidazolines as inhibitors of the interaction of the Protein is similar to p53 and MDM2 polypeptides

摘要

Imidazoline Derivative of a compound of formula I, where X1 is lower and Lower alkoxy substituted by Fluorine, trifluoromethyl or alkoxy; x2 is less than h, halogen, alkyl, etc.; X3 is H, Lower alkoxy, halogen, among others; x4 and X5 are inferior and can be United and rent Mong to form a cycloalkyl; X6 is Ciano, - CH2 - Oh, among others; y1 and Y2 are h,Lower alkyl; R is replaced by a heterocycle piperidinilo 5 or 6 links, among others.Preferred compounds are: hydrochloride [(4S, 5R) - 2 - (4 - tert - butyl - phenyl - 2 - ethoxy) - 4.5 - bis - (4 - Fluorine phenyl) - 4,5-dihydro - imidazol-1-yl] - [4 - (2 - ethyl - metanosulfonil) piperazin-1-yl] - methanone hydrochloride of 4 - [(4S, 5R) - 2 - (4 - tert - butyl - phenyl - 2 - ethoxy) - 4.5 - bis - (4 - Fluorine phenyl) - 4,5-dihydro - imidazole - 1 - car Bo - Nil] - piperazin - 2 - ona, among others.It also relates to a Pharmaceutical Composition and a preparation method. These compounds inhibit the interaction of Protein with similar to the p53 MDM2 polypeptides and are useful in the treatment of proliferative diseases such as cancer