蛋白降解靶向BCR-ABL化合物及其抗肿瘤应用
Alternative TitleThe degradation of the protein targeting BCR - ABL compound and its anti-tumor application
杨小宝; 姜标; 阴倩倩; 陈金聚; 赵全菊; 任超伟; 孙仁红; 孙宁; 仇星; 孔莹; 李岩; 刘林义
2019-03-08
Date Available2019-09-17
Status申请中
Rights Holder上海科技大学
Application NumberCN201910175266.2
Open (Notice) NumberCN110240629A
Subtype发明专利
Abstract本公开提供式(I)的蛋白降解靶向BCR‑ABL化合物及其抗肿瘤应用。式(I)化合物对BCR‑ABL靶蛋白具有降解和抑制作用,其主要由四部分组成,第一部分BCR‑ABL‑TKIs是具有BCR‑ABL酪氨酸激酶抑制活性的化合物;第二部分LIN是链接单元;第三部分ULM是具有泛素化功能的VHL或者CRBN蛋白酶的小分子配体;以及第四部分基团A为羰基,其将BCR‑ABL‑TKIs和LIN共价结合,且LIN与ULM共价结合。本公开设计合成的一系列化合物具有广泛的药理活性,有降解BCR‑ABL蛋白和抑制BCR‑ABL活性的功能,可用于相关的肿瘤治疗。
Other AbstractThe present invention provides a protein degradation targeting BCR-ABL compound represented by formula (I) and an antitumor application thereof. The compound represented by formula (I) has the effects of degrading and inhibiting BCR-ABL target proteins, and mainly consists of four parts; the first part, BCR-ABL-TKIs, is a compound having BCR-ABL tyrosine kinase inhibitory activity; the second part, LIN, is a link unit; the third part, ULM, is a small molecular ligand of VHL or CRBN proteases having a ubiquitination function; and the fourth part, group A, is a carbonyl group, which covalently binds BCR-ABL-TKIs and LIN, and covalently binds LIN and ULM. A series of compounds designed and synthesized in the present invention have extensive pharmacological activities, have the functions of degrading BCR-ABL proteins and inhibiting BCR-ABL activity, and can thus be used in related tumor treatment.
IPC Classification NumberC07K5/062 ; A61K38/05 ; C07D417/14 ; C07D401/14 ; A61K31/506 ; A61K31/496 ; A61P35/00 ; A61P35/02
CPC Classification NumberA61K31/497 ; A61K38/05 ; A61P35/00 ; A61P35/02 ; A61K31/506 ; C07D401/14 ; C07D417/14 ; A61K31/496
Country中国
Patent Agent李献忠 ; 邱晓敏
Agency上海胜康律师事务所 31263
Document Type专利
Identifierhttp://kms.shanghaitech.edu.cn/handle/2MSLDSTB/104592
Collection免疫化学研究所_特聘教授组_抗体化学实验室
科技发展处
生命科学与技术学院_硕士生
Affiliation上海科技大学
Recommended Citation
GB/T 7714
杨小宝,姜标,阴倩倩,等. 蛋白降解靶向BCR-ABL化合物及其抗肿瘤应用[P]. 2019-03-08.
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