申请人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V
公开号:WO2017211818A1
公开(公告)日:2017-12-14
The present invention relates to a compound of formula (I), wherein X is C=0, C=S or B-OH; Y is an electrophile and Z is a leaving group, or Y══Z is an electrophile; R1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, said first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits β1 and β2 of a proteasome; R2 and R3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethinyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen.
本发明涉及一种化合物,其化学式为(I),其中X为C=0,C=S或B-OH;Y为亲电试剂,Z为脱离基团,或Y══Z为亲电试剂;R1包括或由(a)(i)结合到蛋白酶体的蛋白酶位点的第一基团,所述第一基团与X结合;以及(ii)可选地增强传递的第二基团;或(b)结合到蛋白酶体的亚基β1和β2之间的基团;R2和R3独立地选自H,甲基,甲氧基,乙基,乙烯基,乙炔基和氰基,其中甲基和乙基可以被OH或卤素取代。