Elastase inhibitor prodrug and use thereof

US12365699B2 · kind B2 · utility

Assignee

• SUZHOU ARK BIOPHARMACEUTICAL CO., LTD. · CN

Inventors

• Cheng PENG · Suzhou, CN
• Yang Zhou · Suzhou, CN
• Yanfei Wang · Lo Wu, CN
• Mengfei QIAN · Suzhou, CN
• Zhaoxiong Cai · Suzhou, CN
• Gang ZOU · Suzhou, CN
• Haiqing Yuan · Irvine, US
• Zhen Jim WU · Suzhou, CN

Key dates

• Filing date: Mar 8, 2021
• Grant date: Jul 22, 2025
• Expiry date: Oct 16, 2042

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F5/022
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present disclosure provides an elastase inhibitor prodrug and use thereof, being a compound of formula I or a pharmaceutically acceptable salt, ester, isomer or solvate thereof, prodrugs or isotopically labeled compound. Compared with the compound 52 (control example) in WO 2018/175173 A1, the compound disclosed herein has the advantages of high pulmonary exposure and long half-life. The prodrugs of the present disclosure significantly increase the concentration and residence time of the active compound (control example) in the lungs with significant improvements in pharmacokinetics in vivo compared to the control example.