The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Aug. 12, 2025
Filed:
Nov. 16, 2020
China Pharmaceutical University, Suzhou, CN;
Qidong You, Suzhou, CN;
Zhengyu Jiang, Suzhou, CN;
Mengchen Lu, Suzhou, CN;
Xian Zhang, Suzhou, CN;
Jing Zhao, Suzhou, CN;
Xiaoke Guo, Suzhou, CN;
Xiaoli Xu, Suzhou, CN;
Lei Wang, Suzhou, CN;
CHINA PHARMACEUTICAL UNIVERSITY, Jiangsu, CN;
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 HO-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The HOactivated 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 HO-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.