O-malonyltryrosyl compounds, O-malonyltryrosyl compound-containing peptides, and use thereof

US5688992A · kind A · utility

Assignee

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

Inventors

• Terrence R. Burke, Jr. · Kirkwood, US
• Bin Ye · Moraga, US
• Miki Akamatsu · Rockville, US
• Hemanta K. Kole · Baltimore, US
• Xinjian Yan · 恩江镇, CN
• Peter R. Roller · Rockville, US

Key dates

• Filing date: Mar 31, 1995
• Grant date: Nov 18, 1997
• Expiry date: Mar 31, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/18
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to non-phosphorus containing O-malonyltryrosyl compounds, derivatives thereof, uses of the O-malonyltryrosyl compounds in the synthesis of peptides, and O-malonyltryrosyl compound-containing peptides. The O-malonyltyrosyl malonyltyrosyl compounds and O-malonyltryrosyl compound-containing peptides of the present invention are uniquely stable to phosphotases, capable of crossing cell membranes, suitable for application to peptide synthesis of O-malonyltryrosyl compound-containing peptides, and amenable to prodrag defivatization for delivery into cells. The present invention also provides for O-malonyltryrosyl compound-containing peptides which exhibit inhibitory potency against binding interactions of receptor domains with phosphotyrosyl-containing peptide ligands.