Discovery of covalent EGFR inhibitors by cysteine 775
CN119365454APending Publication Date: 2025-01-24DANA FARBER CANCER INSTITUTE INC +1
0 Cites 0 Cited by
Patent Information
- Application Number
- CN202380041900.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2022-04-05
- Filing Date
- 2023-04-05
- Publication Date
- 2025-01-24
AI Technical Summary
Technical Problem
Existing EGFR tyrosine kinase inhibitors are highly resistant to tumors carrying T790M mutations, and patients develop resistance to AZD9291 treatment after obtaining the C797S mutation, resulting in a reduced therapeutic effect.
Method used
Provides a new compound (formula A-I), which targets the CYS775 on EGFR, has an alternative mechanism, can effectively suppress the activity of EGFR, and is suitable for treating EGFR-related tumors with different mutations.
Benefits of technology
This compound can effectively inhibit the activity of EGFR, potentially overcoming the dependence of existing treatments on drug-resistant mutations, and providing a new therapeutic strategy to deal with drug resistance problems related to EGFR mutations.
✦ Generated by Eureka AI based on patent content.
Abstract
The present disclosure relates to compounds that are epidermal growth factor receptor (EGFR) inhibitors; pharmaceutical compositions comprising such compounds; and methods of treating or preventing kinase-mediated conditions, including cancer and other proliferative diseases.
Need to check novelty before this filing date? Find Prior Art