PROTEIN DEGRADATION TARGETING BCR-ABL COMPOUND AND ANTITUMOR APPLICATION THEREOF
Alternative Title蛋白降解靶向BCR-ABL化合物及其抗肿瘤应用
YANG Xiaobao; JIANG Biao; YIN Qianqian; CHEN Jinju; ZHAO Quanju; REN Chaowei; SUN Renhong; SUN Ning; QIU Xing; KONG Ying; LI Yan; LIU Linyi
2019-03-08
Date Available2019-09-12
StatusPCT-有效期内
Rights HolderSHANGHAITECH UNIVERSITY
Application NumberWOCN19077535
Open (Notice) NumberWO2019170150A1
Subtype发明专利
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.
Other 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。
IPC Classification NumberC07D417/14 ; A61K31/497 ; A61P35/02
CountryWO
Patent Agent上海胜康律师事务所 ; SYNCLAW ATTORNEYS
Agency上海胜康律师事务所 ; SYNCLAW ATTORNEYS
Document Type专利
Identifierhttp://kms.shanghaitech.edu.cn/handle/2MSLDSTB/104594
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
AffiliationSHANGHAITECH UNIVERSITY
Recommended Citation
GB/T 7714
YANG Xiaobao,JIANG Biao,YIN Qianqian,et al. PROTEIN DEGRADATION TARGETING BCR-ABL COMPOUND AND ANTITUMOR APPLICATION THEREOF[P]. 2019-03-08.
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