Cytostatic-glycoconjugates having specifically cleavable linking units
OwnerHans-Georg Lerchen, Joerg Baumgarten +1inventors
InventorsHans-Georg Lerchen, Joerg Baumgarten, Oswald Lockhoff
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Abstract
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to specific carbohydrate moeities via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), elastase or cathepsines, i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee sufficient serum stability of the conjugate of cytostatic and carbohydrate moeity 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.
Claims10
Conjugate, characterized by the formula (I)
- CT-LI-Sp1-Sp2-K (I)
- in which
- CT denotes a cytotoxic radical or a radical of a cytostatic or of a cytostatic derivative, which can additionally carry a hydroxyl, carboxyl or amino group,
- LI is a linker group comprising 5 to 8 amino acid residues in the D or L configuration, which can each optionally carry protective groups,
- Sp1 is absent or a carbonyl or a thiocarbonyl radical,
- Sp2 is an optionally substituted arylene or alkylene radical,
- K is an unsubstituted or regioselectively modified carbohydrate radical;
- and their physiologically acceptable salts, hydrates and stereoisomers.
Dependencies are inferred from the claim text.