- Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds
-
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
- -
-
-
- Aminoisoquinolines: Design and synthesis of an orally active benzamidine isostere for the inhibition of factor Xa.
-
The design, synthesis and SAR of sulfonamidopyrrolidinone fXa inhibitors incorporating a new benzamidine isostere, namely aminoisoquinolines, is described. These inhibitors have higher Caco-2 cell permeability than comparable benzamidines and attain higher levels of exposure upon oral dosing. The most potent member 14b (fXa Ki=6 nM) is selective against other serine proteasesof interest (>600 fold).
- Choi-Sledeski,Becker,Green,Davis,Ewing,Mason,Ly,Spada,Liang,Cheney,Barton,Chu,Brown,Colussi,Bentley,Leadley,Dunwiddie,Pauls
-
p. 2539 - 2544
(2007/10/03)
-