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US 5,621,002 AGranted
Prodrugs for enzyme mediated activation
AssigneesBehringwerke Aktiengesellschaft, Laboratoires Hoechst S/A
InventorsKlaus Bosslet, J org Czech, Dieter Hoffmann, Andrea Vasella, Roland Hoos, Fran.cedilla.ois Tillequin, Jean-Claude Florent, Michel Azoulay, Claude Monneret, Jean-Claude Jacquesy, Jean-Pierre Gesson, Michel Koch
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Abstract
Enzymatically clearable prodrugs with reduced Michaelis-Menten constant (Km) are described.
Claims9
A compound having the formula (I)
- S--Z--W (I)
- wherein
- S is an inhibitor of a human glycosidase and has the formula ##STR11## wherein each R is independently H, OH, F, NH.sub.2, COOH, CH.sub.2 --COOH, CH(OH)--COOH, PO.sub.3 H.sub.2, CH.sub.2 --PO.sub.3 H.sub.2 or CH(OH)--PO.sub.3 H.sub.2,
- X is NH, O or S, and
- m is 0 or 1;
- W is a pharmacologically active substance;
- and
- Z is a direct bond or a self-immolative spacer,
- provided that S is not .beta.-D-glucuronic add or 2-amino-.beta.-D-glucuronic acid when W is an anthracycline.
6 more elements
Dependencies are inferred from the claim text.