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Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
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.
Affiliation
  • Guertin KR; Drug Innovation and Approval, Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. kevin.guertin@roche.com
Bioorg Med Chem Lett ; 12(12): 1671-4, 2002 Jun 17.
Article in En | MEDLINE | ID: mdl-12039587
ABSTRACT
Further optimization of the beta-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.
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Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Serine Proteinase Inhibitors / Cyclic N-Oxides / Factor Xa Inhibitors / Anticoagulants Type of study: Diagnostic_studies / Prognostic_studies Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country:
Search on Google
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PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Serine Proteinase Inhibitors / Cyclic N-Oxides / Factor Xa Inhibitors / Anticoagulants Type of study: Diagnostic_studies / Prognostic_studies Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country: