Title of article
Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity
Author/Authors
Kevin R. Guertin، نويسنده , , Charles J. Gardner، نويسنده , , Scott I. Klein، نويسنده , , Allison L. Zulli، نويسنده , , Mark Czekaj، نويسنده , , Yong Gong، نويسنده , , Alfred P. Spada، نويسنده , , Daniel L. Cheney، نويسنده , , Sebastian Maignan، نويسنده , , Jean-Pierre Guilloteau، نويسنده , , Karen D. Brown، نويسنده , , Dennis J. Colussi، نويسنده , , Valeria Chu، نويسنده , , Christopher L. Heran، نويسنده , , Suzanne R. Morgan، نويسنده , , Ross G. Bentley، نويسنده , , Christopher T. Dunwiddie، نويسنده , , Robert J. Leadley، نويسنده , , Henry W. Pauls، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
1671
To page
1674
Abstract
Further optimization of the β-aminoester class of factor Xa (fXa) inhibitors is described culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with excellent in vivo anticoagulant activity. An X-ray structure of FXV673 bound to human fXa is also presented. Based on its selectivity, potent in vivo activity and favorable pre-clinical safety profile, FXV673 was selected for further development and is currently undergoing clinical trials.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792285
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