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 …

…, SI Klein, AL Zulli, M Czekaj, Y Gong, AP Spada…

Index: Guertin, Kevin R; Gardner, Charles J; Klein, Scott I; Zulli, Allison L; Czekaj, Mark; Gong, Yong; Spada, Alfred P; Cheney, Daniel L; Maignan, Sebastian; Guilloteau, Jean-Pierre; Brown, Karen D; Colussi, Dennis J; Chu, Valeria; Heran, Christopher L; Morgan, Suzanne R; Bentley, Ross G; Dunwiddie, Christopher T; Leadley, Robert J; Pauls, Henry W Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 12 p. 1671 - 1674

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Citation Number: 48

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 ...