abstract |
The present invention relates to new amidines and guanidines, their preparation and their use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and the complement proteases C1s and C1r. DOLLAR A The invention also relates to pharmaceutical compositions containing the compounds as active ingredients, as well as the use of the compounds as thrombin inhibitors, anticoagulants, complement inhibitors and as anti-inflammatory agents. The linking of a serine protease inhibitor with an amidine or guanidine function to an alkyl radical with two or more hydroxyl functions is characteristic of the new compounds, this alkyl radical being derived from sugar derivatives. Several sugar components or components derived from sugars can also be linked to one another. This principle of coupling with sugar derivatives leads to orally active compounds. |