首页> 外国专利> 2 2 Target protein degradation inducing compound preparation method thereof and pharmaceutical composition for preventing or treating EED EZH2 or PRC2 related diseases containing the same as an active ingredient

2 2 Target protein degradation inducing compound preparation method thereof and pharmaceutical composition for preventing or treating EED EZH2 or PRC2 related diseases containing the same as an active ingredient

机译:2 2诱导目标蛋白质降解的化合物的制备方法以及用于预防或治疗与EED EZH2或PRC2有关的疾病的药物组合物

摘要

The present invention relates to a target proteolytic induction degrader, a method for producing the same, and a pharmaceutical composition for preventing or treating EED, EZH2, or PRC2 related diseases containing the same as an active ingredient. The novel compounds represented by Formula 1 according to the present invention include cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, MDM2 (Mouse double minute 2 homolog) E3 ubiquitin ligase, As a degraducer compound that induces the degradation of a target protein, that is, EED (embryonic ectoderm development) or PRC2 (polycomb repressive complex 2) using cIAP (Cellular Inhibitor of Apoptosis Protein 1) E3 ubiquitin ligase, There is an aspect of remarkably achieving target protein degradation inducing activity through UPS (Ubiquitin Proteasome System), and a pharmaceutical composition for the prevention or treatment of target protein-related diseases or conditions containing it as an active ingredient, and health for prevention or improvement There is a useful effect that can provide a nutraceutical composition.
机译:靶蛋白水解诱导降解物,其制备方法以及用于预防或治疗与靶蛋白水解诱导降解物有关的与EDE,EZH2或PRC2有关的疾病的药物组合物。根据本发明,由式1表示的新化合物包括脑神经E3泛素连接酶,冯·Hippel-Lindau肿瘤抑制物(VHL)E3泛素连接酶,MDM2(小鼠双分钟2同系物)E3泛素连接酶,作为诱导神经元E3泛素连接的退行化合物。使用cIAP(细胞凋亡蛋白1的细胞抑制剂)E3泛素连接酶降解EED(胚胎外胚层发育)或PRC2(多梳抑制复合物2)的目标蛋白。通过显着地实现目标蛋白降解诱导活性的一个方面是UPS(泛素蛋白酶体系统),以及用于预防或治疗与目标蛋白质相关的疾病或病症的药物组合物,其包含其作为有效成分,以及对健康的预防或改善。可以提供营养保健组合物。

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