TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT
申请人:Korea Research Institute of Chemical Technology
公开号:EP3922632A1
公开(公告)日:2021-12-15
The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.
本发明涉及一种靶蛋白降解诱导剂Degraducer,其制备方法以及包含其作为活性成分的用于预防或治疗与EED、EZH2或PRC2相关疾病的药物组合物。根据本发明,由式1表示的一种新化合物是一种Degraducer化合物,通过利用cereblon E3泛素连接酶、von Hippel-Lindau肿瘤抑制因子(VHL)E3泛素连接酶、鼠双分钟2同源物(MDM2)E3泛素连接酶和细胞凋亡抑制蛋白1(cIAP)E3泛素连接酶诱导靶蛋白,即胚胎外胚层发育(EED)或多能复合体抑制2(PRC2)的降解,其中该化合物通过泛素蛋白酶体系统(UPS)显著实现靶蛋白降解诱导活性的方面,因此可以提供一种用于预防或治疗与靶蛋白相关疾病或症状的药物组合物,以及包含所述化合物作为活性成分的功能性保健食品组合物,具有有益效果。