上海科技大学知识管理系统

The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), intermediates of formula (IV), and uses of the intermediates. The compound of formula (I) has a degrading effect on a specific target protein, which is mainly composed of three parts. The first part is a small molecule compound (SMBP, Small Molecules Binding Protein) that can bind to a protein, the second part LIN is a linker, and the three-part ULM is a ubiquitin ligand (ULM, Ubiquitin Ligase Binding Moiety), wherein SMBP is covalently bound to LIN, and LIN is covalently bound to ULM. A series of compounds designed and synthesized in the present disclosure have a wide range of pharmacological activities, including the functions of degrading specific proteins and//or inhibiting activities of specific proteins, and thus can be used in related tumor treatments.

本公开涉及式(I)化合物及其抗肿瘤用途，以及式(III)化合物的中间体，式(IV)化合物的中间体和中间体的用途。 式(I)化合物对一种特定的靶蛋白具有降解作用，该靶蛋白主要由三部分组成。 第一部分是小分子化合物(SMBP， 可与蛋白质结合的小分子结合蛋白)，第二部分LIN是接头，三部分ULM是泛素配体(ULM，泛素连接酶结合部分)，其中SMBP与LIN共价结合，LIN与ULM共价结合。 本发明设计并合成的一系列化合物具有广泛的药理活性，包括降解特定蛋白和//或抑制特定蛋白活性的功能，因此可用于相关的肿瘤治疗。