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.
Claims21
A medicament, which comprises, as an active compound, one or more compounds of the general formula I and/or II
- in which
- E is a group from
- B is —SO2— or —CO—,
- X is —NR1 or —CHR1,
- Z is —R4, —OR4 or —NH—R4,
- Y is —OR2or —NHR2,
- R1 is in each case independently —H, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, unsubstituted or substituted,
- R2 is —H, —OR1, —COR1, —CON(R1)2 or —COOR1,
- R3 is —H, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, unsubstituted or substituted, or —COR6 or —COOR6 or an oligo- or polyalkyleneoxy radical,
- R4 is —H, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, unsubstituted or substituted, or a cyclic radical,
- R5 is —OR6, —N(R6)2, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, unsubstituted or substituted, and
- R6 is —H, —C1-C6-alkyl, —C2-C6-alkenyl or —C2-C6-alkynyl, unsubstituted or substituted, or a cyclic radical,
- with each cyclic radical being able to carry one or more substituents 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,
- and it being possible for each alkyl, alkenyl or alkynyl to be straight-chained or branched and to carry one or more substituents selected from the group consisting of halogen, —OR6, —OCOR6, —N(R6)2, —NR6COR6, —NR6CON(R6)2, COOR6 or a cyclic radical,
- or salts of said compounds and optionally pharmaceutically customary carriers, diluents or/and adjuvants.
Dependencies are inferred from the claim text.