Chemotactic peptide antagonists for imaging sites of inflammation

US6872536B1 · kind B1 · utility

Assignee

• BRACCO IMAGING S.P.A. · IT

Inventors

• David Roe · Portland, US
• Christine Maria Ribic · Hamilton, CA
• Betty Lawrence · Bolton, CA
• Catherine M. Pollock · Toronto, CA
• Alfred Pollack · Hannover, DE

Key dates

• Filing date: Nov 10, 1999
• Grant date: Mar 29, 2005
• Expiry date: Nov 10, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K7/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Radiopharmaceuticals comprising molecules that target to N-formyl-methionyl-leucy-phenylalanine (fMLF) receptor on leukocytes in order to target sites of inflammation for diagnostic imaging are described. The targeting molecules are attached to capping groups that make the entire molecule either antagonists or weak agonists of fMLF receptor and therefore do not elicit a chemotactic response resulting in neutropenia. The preferred targeting molecule is ReO-Gly-lys(Dimethylgly-t-Butylgly-cys-gly)glu-trp-phe-leu-nle-NHCOcyclopropyl (wherein the peptide sequence NLeu-Leu-Phe-Trp-Glu-Lys-Gly is SEQ. ID No. 1.) The invention also relates to the use of combinatorial chemistry to obtain preferred molecules that target sites of inflammation for diagnostic imaging.