Shanghaitech University

Xiaoling Song

Biao Jiang

Ning Sun

Xiaobao Yang

Jinju Chen

Chaowei Ren

Ying Kong

Yan Li

Xing Qiu

Yuedong Zhou

Renhong Sun

Quanju Zhao

Qianqian Yin

Haifan Lin

Jianshui Zhang

A compound of general formula (I), a compound of general formula (III) and anti-tumor applications thereof. A series of compounds designed and synthesized have a wide range of pharmacological activities, have the function of degrading specific proteins and/or inhibiting activity, and can be used in related tumor and cancer treatments.

ALK protein regulator and anti-tumor application thereof

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.

Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates

A compound of formula (I) and its antitumor application are disclosed. The compounds of formula (I) have degradation and inhibitory effects on ALK target proteins. They are mainly composed of four parts: the first part, ALK-TKI, being compounds with ALK tyrosine kinase inhibitory activity; the second part, LIN, being different kinds of linker (Linker); the third part, the ULM, being a small molecule ligand (ULM, ubiquitin ligase binding moiety) with ubiquitination of VHL, CRBN or other proteases; and the fourth part, the group A, being a carbonyl group or absent, which covalently bond ALK-TKI to LIN, wherein LIN and ULM are covalently bonded. A series of compounds designed and synthesized by the present disclosure have wide pharmacological activities, have functions of degrading ALK protein and inhibiting ALK activity, and can be used for related tumor treatment.

ALK protein degradation agent and anti-tumor application thereof

Growing community of inventors

Shanghai, China

Xiaoling Song