Hydrogen peroxide-responsive KEAP1-NRF2 ppi inhibitor prodrug, and preparation method therefor
US12383535B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Nov 16, 2020 |
| Grant date | Aug 12, 2025 |
| Priority date | — |
| Expiry date | May 2, 2043 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D277/14
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a H2O2-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The H2O2 activated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a H2O2-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.