Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents

US10981866B2 · 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
• Orit Jacobson Weiss · Silver Spring, US

Key dates

• Filing date: Oct 3, 2017
• Grant date: Apr 20, 2021
• Expiry date: Oct 3, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/05
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention is directed to a compound of Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula III wherein the definitions of R1-R12 and L1-L4 are provided in the disclosure, wherein R13 is a chelating group comprising 177Lu, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.