Author/Authors :
Marc Nazaré، نويسنده , , Melanie Essrich، نويسنده , , David W Will، نويسنده , , Hans Matter، نويسنده , , Kurt Ritter، نويسنده , , Matthias Urmann، نويسنده , , Armin Bauer، نويسنده , , Herman Schreuder، نويسنده , , Jorg Czech، نويسنده , , Martin Lorenz، نويسنده , , Volker Laux، نويسنده , , Volkmar Wehner، نويسنده ,
Abstract :
A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for P4 ligands in combination with a neutral biaryl P1 ligand were investigated with the 2-carboxyindole scaffold. A diverse set of P4 substituents was identified, which, in conjunction with a biaryl P1 ligand, gave highly potent factor Xa inhibitors, which were also selective versus other proteases and efficacious in various antithrombotic secondary assays.
Keywords :
fax: +49-69-331-399 , e-mail: marc.nazare@aventis.com , Factor Xa inhibitors.* Corresponding author. Tel.: +49-69-305-15150