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Patenting perspective on Keap1 inhibitors (2019-2024)
Yongfu Luo1, Ziyu Yang1, Yuan Zhang1
1Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University Medical College, Suzhou, China.
Expert Opinion on Therapeutic Patents
|February 5, 2025
Summary
Kelch-like ECH-associated protein 1 (Keap1) inhibitors are promising for oxidative stress and inflammation. Recent patents reveal advancements in structural optimization and novel strategies like PROTACs for enhanced therapeutic potential.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Pharmacology
Background:
- Kelch-like ECH-associated protein 1 (Keap1) negatively regulates nuclear factor erythroid 2-related factor 2 (Nrf2).
- Oxidative stress and inflammation are implicated in various diseases.
- Keap1 is a validated drug target for these conditions.
Purpose of the Study:
- To review patents on Keap1 inhibitors from 2019 to 2024.
- To analyze structural characteristics and optimization strategies.
- To assess pharmacological properties and clinical progress of Keap1 inhibitors.
Main Methods:
- Patent literature search (2019-2024).
- Analysis of chemical structures and reported properties.
- Review of preclinical and clinical development data.
Main Results:
- Significant advancements in Keap1 inhibitor design.
- Emerging strategies include ROS-cleavable prodrugs, bivalent inhibitors, and PROTACs.
- Expanding range of drug types and therapeutic applications.
Conclusions:
- Keap1 inhibitors show enhanced potency and drug-like properties.
- These inhibitors represent a promising therapeutic option for oxidative stress and inflammation-related diseases.
- Continued innovation in inhibitor design is expanding their clinical utility.
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