Toll-like receptor 2 ligands and methods of making and using thereof

US10118942B2 · kind B2 · utility

Assignees

• H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE INC. · US
• Arizona Board of Regents on Behalf of the University of Arizona · US
• University of South Florida · US

Inventors

• David L. Morse · Tampa, US
• Josef Vagner · Tucson, US
• Mark McLaughlin · Tampa, US
• Robert J. Gillies · Tampa, US
• Amanda Huynh · Land O' Lakes, US
• Michael Doligalski · Lutz, US

Key dates

• Filing date: Mar 25, 2016
• Grant date: Nov 6, 2018
• Expiry date: Mar 25, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K51/0497
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.