Direct inhibitors of Keap1-Nrf2 interaction as antioxidant inflammation modulators

US10106502B2 · kind B2 · utility

Assignees

• Rutgers, the State University of New Jersey · US
• The Broad Institute, Inc. · US

Inventors

• Longqin Hu · Piscataway, US
• Sadagopan Magesh · Highland Park, US
• Lin Chen · Hangzhou City, CN
• Timothy A. Lewis · Marlborough, US
• Ben Munoz · Newton, US
• Lili Wang · Beijing, CN

Key dates

• Filing date: Sep 28, 2017
• Grant date: Oct 23, 2018
• Expiry date: Sep 28, 2037

Classification

• Technology area (CPC G): Physics
• CPC primary: G01N33/5023
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.