Hydroxyamidine and hydroxyguanidine compounds as urokinase inhibitors
AssigneeWilex AG
InventorsStefan Sperl, Markus Buergle, Wolfgang Schmalix, Katja Wosikowski, Bernd Clement
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Abstract
The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates in particular to compounds containing hydroxyamidine or hydroxyguanidine groups.
Claims6
A pharmaceutical composition, which comprises, as an active compound, one or more compounds of the formula
- in which E is a group
- R3 is —H,
- R5 is —OR6, —N(R6)2, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, said alkyl, alkenyl and alkynyl moieties being straight-chained or branched and being unsubstituted or substituted by at least one substituent selected from the group consisting of halogen, —OR6, —OCOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2, COOR6, and a radical selected from the group consisting of a cycloalkyl-, aryl-, and bicyclic-radical which is unsubstituted or substituted by at least one substituent selected from the group consisting of —C1-C3-alkyl, —C1-C3-alkoxy, halogen, —OR6, ═O, —NO2, —CN, —COOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2 and —OCOR6,
- R6 is —H, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, or a radical selected from the group consisting of a cycloalkyl-, aryl-, and bicyclic-radical which is unsubstituted or substituted by at least one substituent selected from the group consisting of —C1-C3-alkyl, —C1-C3-alkoxy, halogen, —OR6, ═O, —NO2, —CN, —COOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2 and —OCOR6,
- said alkyl, alkenyl and alkynyl moieties being straight-chained or branched and being unsubstituted or substituted by at least one substituent selected from the group consisting of halogen, —OR6, —OCOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2, COOR6 , and a radical selected from the group consisting of a cycloalkyl-, aryl-, and bicyclic-radical which is unsubstituted or substituted by at least one substituent selected from the group consisting of —C1-C3-alkyl, —C1-C3-alkoxy, halogen, —OR6, ═O, —NO2, —CN, —COOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2 and —OCOR6,
- or a salt of said compound
- and a pharmaceutically customary carrier, diluent or/and adjuvant.
A salt of a compound of the formula I,
- in which E is
- and R5 is ethoxy and wherein the salt is in the form of a hydrogen sulfate or sulfate.
Dependencies are inferred from the claim text.