Small molecule activators of NRF2 pathway

US9737525B2 · kind B2 · utility

Assignees

• The General Hospital Corporation · US
• The Regents of the University of California · US

Inventors

• Aleksey G. Kazantsev · Chapel Hill, US
• Leslie Thompson · Irvine, US
• Ruben Abagyan · Village of La Jolla, US
• Malcolm Casale · Mission Viejo, US

Key dates

• Filing date: Jun 6, 2014
• Grant date: Aug 22, 2017
• Expiry date: Jun 6, 2034

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/4439
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer.