Cytostatic conjugates with integrin ligands

US7304037B2 · kind B2 · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Hans-Georg Lerchen · Leverkusen, DE
• Jorg Baumgarten · Wuppertal, DE
• Andreas Schoop · Overath, DE
• Markus Albers · Leverkusen, DE

Key dates

• Filing date: Mar 8, 2002
• Grant date: Dec 4, 2007
• Expiry date: Oct 23, 2022

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especially be found in tumor tissue. The preferred linking units provide sufficient stability of the conjugate of cytostatic and αvβ3 integrin antagonist in biological fluids and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.