Invention Grant
- Patent Title: Compounds targeting and degrading BCR-ABL protein and its antitumor application
-
Application No.: US17015319Application Date: 2020-09-09
-
Publication No.: US11639343B2Publication Date: 2023-05-02
- Inventor: Xiaobao Yang , Biao Jiang , Qianqian Yin , Jinju Chen , Quanju Zhao , Chaowei Ren , Renhong Sun , Ning Sun , Xing Qiu , Ying Kong , Yan Li , Linyi Liu
- Applicant: ShanghaiTech University
- Applicant Address: CN Shanghai
- Assignee: ShanghaiTech University
- Current Assignee: ShanghaiTech University
- Current Assignee Address: CN Shanghai
- Agency: Osha Bergman Watanabe & Burton LLP
- Main IPC: C07D401/14
- IPC: C07D401/14 ; C07D417/14 ; A61P35/02 ; A61K45/06

Abstract:
The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.
Information query