Efforts toward oral bioavailability in factor VIIa inhibitors

Dange Vijaykumar; Roopa Rai; Michael Shaghafi; Tony Ton; Steve Torkelson; Ellen M Leahy; Jennifer R Riggs; Huiyong Hu; Paul A Sprengeler; William D Shrader; Colin O'Bryan; Ronnell Cabuslay; Ellen Sanford; Erik Gjerstadt; Liang Liu; Juthamas Sukbuntherng; Wendy B Young

doi:10.1016/j.bmcl.2006.04.018

Efforts toward oral bioavailability in factor VIIa inhibitors

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. doi: 10.1016/j.bmcl.2006.04.018. Epub 2006 May 2.

Authors

Dange Vijaykumar¹, Roopa Rai, Michael Shaghafi, Tony Ton, Steve Torkelson, Ellen M Leahy, Jennifer R Riggs, Huiyong Hu, Paul A Sprengeler, William D Shrader, Colin O'Bryan, Ronnell Cabuslay, Ellen Sanford, Erik Gjerstadt, Liang Liu, Juthamas Sukbuntherng, Wendy B Young

Affiliation

¹ Celera, 180 Kimball Way, South San Francisco, CA 94979, USA. dvijayku@hotmail.com

PMID: 16650987
DOI: 10.1016/j.bmcl.2006.04.018

Abstract

Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in improved physicochemical properties, leading to enhanced oral absorption in rat.

MeSH terms

Administration, Oral
Animals
Anticoagulants / chemical synthesis*
Anticoagulants / pharmacology*
Biological Availability
Factor VIIa / antagonists & inhibitors*
Rats
Structure-Activity Relationship
Thrombin / antagonists & inhibitors
Thrombosis / drug therapy*

Substances

Anticoagulants
Factor VIIa
Thrombin