HYDROXYAMIDINE AND HYDROXYGUANIDINE COMPOUNDS AS UROKINASE INHIBITORS
The invention relates to novel compounds for the inhibition of the urokinase plasminogen activator (uPA) with high bioavailability and which can also be administered orally, and to the use thereof as therapeutic active ingredients for the treatment of urokinase or/and urokinase receptor associated diseases, such as, for example, tumours and metastization. The invention especially relates to compounds (I) and (II) that contain hydroxyamidine or hydroxyguanidine groups, wherein E represents a group consisting of (a).
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(2008/06/13)
3-Amidinophenylalanine-based inhibitors of urokinase
Synthesis and anti-uPA activity of a series of Nα-triisopropyl-phenylsulfonyl-protected 3-amidino-phenylalanine amides are described. We have explored SAR around the C-terminal amide part for inhibition of uPA, plasmin and trypsin. Modification of the ami
Stuerzebecher, Joerg,Vieweg, Helmut,Steinmetzer, Torsten,Schweinitz, Andrea,Stubbs, Milton T.,Renatus, Martin,Wikstroem, Peter
p. 3147 - 3152
(2007/10/03)
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