380237-42-3Relevant articles and documents
Base-substituted benzylamine analogs for use as coagulation factor xa inhibitors, the production and use thereof
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Page/Page column 8, (2008/06/13)
The invention relates to the novel base-substituted benzylamine analogs of general formula (I), wherein A represents P2-P1 with P1=(A) and P2=(B), for use as coagulation factor Xa inhibitors. The invention also relates to the production and use of said analogs in the therapy and prophylaxis of cardiovascular diseases and thromboembolic events.
4-Amidinobenzylamine-Based Inhibitors of Urokinase
Kuenzel, Sebastian,Schweinitz, andrea,Reissmann, Siegmund,Stuerzebecher, Joerg,Steinmetzer, Torsten
, p. 644 - 648 (2007/10/03)
A series of 4-amidinobenzylamine-based peptidomimetic inhibitors of urokinase was synthesized. The most potent one, benzylsulfonyl-D-Ser-Ala-4-amidinobenzylamide 16, inhibits uPA with a Ki of 7.7 nM but is less selective than 10 with a Gly as P2 residue. Hydroxyamidine and carbonate prodrugs were prepared, which are rapidly converted into the active inhibitors in rats after subcutaneous application.