L. Anselm, D. Banner, J. Benz
Sep 1, 2010
Citations
0
Influential Citations
35
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
A series of (3R,4R)-pyrrolidine-3,4-dicarboxylic acid amides was investigated with respect to their factor Xa inhibitory activity, selectivity, pharmacokinetic properties, and ex vivo antithrombotic activity. The clinical candidate from this series, R1663, exhibits excellent selectivity against a panel of serine proteases and good pharmacokinetic properties in rats and monkeys. A Phase I clinical study with R1663 has been finalized.