Inhibitors for urokinase receptor

US6528619B1 · kind B1 · utility

Assignee

• Roche Diagnostics GMBH · DE

Inventors

• Markus Bürgle · Hersbruck, DE
• Heinrich Graeff · Birkenfeld, DE
• Horst Kessler · Schwalbach, DE
• Viktor Magdolen · Tauberbischofsheim, DE
• Bernhard König · Bobingen, DE
• Marcus Koppitz · Berlin, DE
• Christoph Riemer · Hersbruck, DE
• Manfred Schmitt · Munich, DE
• Ulrich Weidle · Hersbruck, DE

Key dates

• Filing date: Jan 10, 2000
• Grant date: Mar 4, 2003
• Expiry date: Jan 10, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12Y304/21073
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides peptides as inhibitors of the binding of urokinase to the urokinase receptor. The peptides have the general structural formula (I):X1-[X2]n-X3-X4-K-Y-F-X5-X6-I-X7-W-[X8]m  (I)in whichX1, X2, X3, X4, X5, X6, X7 and X8 each denote an aminocarboxylic acid,n and m are each independently 0 or 1,K denotes an aminocarboxylic acid with a lysine side chain,Y denotes an aminocarboxylic acid with a tyrosine side chain,F denotes an aminocarboxylic acid with a phenyl-alanine side chain,I denotes an aminocarboxylic acid with an isoleucine side chain,W denotes an aminocarboxylic acid with a tryptophan side chain,and the monomeric building blocks are linked by —CONR1— or —NR1CO— bonds where R1 in each case independently denotes hydrogen, methyl or ethyl, and pharmaceutically compatible salts and derivatives thereof.