Imaging agents for imaging protease activity and uses thereof

US10646591B2 · kind B2 · utility

Assignee

• The United States of America, as represented by the Secretary, Department of Health and Human Services · US

Inventors

• Xiaoyuan Chen · Acton, US
• Seulki Lee · Elkridge, US
• Lei Zhu · Hefei, CN

Key dates

• Filing date: Oct 28, 2016
• Grant date: May 12, 2020
• Expiry date: Nov 10, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61N5/062
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are imaging agents having the following Formula I: wherein F is a near infrared fluorophore, S is an enzymatically cleavable oligopeptide, Q is a fluorescence quencher molecule, and M is a moiety selected from the group consisting of PEG or derivative thereof and a targeting ligand, and wherein F, Q and M are linked to separate amino acids of the enzymatically cleavable oligopeptide. Compositions comprising such compounds, as well as methods of use, methods of identifying a cell or a population of cells in vivo expressing a protease of interest, and methods of treating a disease through imaging are also disclosed.