Urokinase inhibitors
AssigneeWilex AG
InventorsPeter Wikström, Helmut Vieweg, Jörg Stürzebecher
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Abstract
New urokinase inhibitors having a triisopropylphenylsulfonyl residue as an Nα-substituent for 3-amidinophenylalanine are provided. The introduction of the triisopropylphenylsulfonyl residue greatly increases the affinity of the compounds to urokinase and, thereby, increases their inhibitory activity against urokinase. These urokinase inhibitors are useful in determining the role of urokinase and urokinase receptor in various diseases, particularly in tumor propagation and metastasis. Methods of treating tumors and a pharmaceutical composition are also provided.
Claims6
Purified urokinase inhibitors of general formula
- which are present as compounds in L-form, and wherein R1 represents
- (a) a group of formula
- wherein either p=1 and r=2 and R2 is benzyloxycarbonyl, benzylaminocarbonyl or 2-thienylhydrazinocarbonyl, or p=2 and r=1 and R2 is ethoxycarbonyl, 2-propyloxycarbonyl, 2-propylaminocarbonyl, methylaminocarbonyl or methyl;
- or
- (b) a group of formula
- wherein R3 is selected from the group consisting of methoxycarbonyl, ethoxycarbonyl, and benzyloxycarbonyl, and
- wherein the compounds occur in the form of their free bases or as salts with inorganic acids, or as salts with organic acids.
Dependencies are inferred from the claim text.