The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 02, 2023
Filed:
Sep. 09, 2020
Shanghaitech University, Shanghai, CN;
Xiaobao Yang, Shanghai, CN;
Biao Jiang, Shanghai, CN;
Qianqian Yin, Shanghai, CN;
Jinju Chen, Shanghai, CN;
Quanju Zhao, Shanghai, CN;
Chaowei Ren, Shanghai, CN;
Renhong Sun, Shanghai, CN;
Ning Sun, Shanghai, CN;
Xing Qiu, Shanghai, CN;
Ying Kong, Shanghai, CN;
Yan Li, Shanghai, CN;
Linyi Liu, Shanghai, CN;
ShanghaiTech University, Shanghai, CN;
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.