An EGFR inhibitor and methods of making and using the same
By developing EGFR inhibitors, the problem of drug resistance caused by C797S mutations has been solved, providing highly effective and low-toxicity inhibitors for various mutant cell lines, and achieving significant inhibitory effects on EGFR mutations.
CN118103371BActive Publication Date: 2026-05-26SHANDONG NEW TIME PHARMA CO LTD
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SHANDONG NEW TIME PHARMA CO LTD
- Filing Date
- 2022-09-16
- Publication Date
- 2026-05-26
AI Technical Summary
Technical Problem
Existing EGFR inhibitors struggle to overcome resistance to C797S mutations, and the lack of highly effective and low-toxicity fourth-generation inhibitors limits their clinical use.
Method used
A class of EGFR inhibitors has been developed, which have significant inhibitory activity against EGFR D770-N771 ins NPG and EGFR D770-N771 ins NPG/T790M/C797S kinases, and have strong inhibitory activity against single-mutant and double-mutant cells. The preparation method is easy to control and the post-processing is simple.
Benefits of technology
It achieves effective inhibition of the C797S mutation, providing a highly efficient and low-toxicity fourth-generation EGFR inhibitor suitable for various mutant cell lines, overcoming the drug resistance problem of existing inhibitors.
✦ Generated by Eureka AI based on patent content.
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Figure CN118103371B_ABST
Abstract
A compound of formula I or a pharmaceutically acceptable salt thereof, and its use in the preparation of a compound that modulates EGFR tyrosine kinase activity or in the prevention and treatment of EGFR-related diseases. The EGFR inhibitor of formula I exhibits inhibitory activity against EGFR D770-N771 in NPG and NPG / T790M kinases, and inhibits cell proliferation of EGFR-Del19 / T790M / C797S kinase, KC-0122:Ba / F3EGFR-L858R / T790M / C797S triple mutant cell lines, and KC-0116:Ba / F3EGFR-Del19 / T790M / C797S triple mutant cell lines.
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