Integrin-mediated drug targeting

Details Integrin-mediated drug targeting Integrin-mediated drug targeting

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61K 31/4745 (2006.01) A61K 38/00 (2006.01) A61P 35/00 (2006.01) C07D 491/22 (2006.01) C07K 5/06 (2006.01) C07K 5/083 (2006.01) C07K 5/117 (2006.01)

Patent

CA 2383981

The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to .alpha.v.beta.3 integrin antagonists via preferred linking units. The preferred linking units guarantee serum stability of the conjugate of cytostatic and .alpha.v.beta.3 integrin antagonist and at the same time the desired intracellular action in tumour cells as a result of their enzymatic or hydrolytic cleavability with release of the cytostatic.

La présente invention concerne des cytostatiques présentant une action spécifique aux tumeurs résultant de leur liaison à des antagonistes d'intégrine .alpha.¿v?.beta.¿3? par l'intermédiaire d'unités de liaison. Les unités de liaisons optimales décrites dans l'invention garantissent à la fois la stabilité du sérum du conjugué d'un cytostatique et d'un antagoniste d'intégrine .alpha.¿v?.beta.¿3? et l'action intracellulaire désirée dans les cellules tumorales résultant de leur aptitude au clivage hydrolytique et enzymatique avec la libération du cytostatique.

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