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  • The Discovery of (2R,4R)-N-...
    The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor
    Kohrt, Jeffrey T.; Bigge, Christopher F.; Bryant, John W.; Casimiro-Garcia, Agustin; Chi, Liguo; Cody, Wayne L.; Dahring, Tawny; Dudley, Danette A.; Filipski, Kevin J.; Haarer, Staci; Heemstra, Ron; Janiczek, Nancy; Narasimhan, Lakshmi; McClanahan, Thomas; Peterson, J. Thomas; Sahasrabudhe, Vaisheli; Schaum, Robert; Van Huis, Chad A.; Welch, Kathleen M.; Zhang, Erli; Leadley, Robert J.; Edmunds, Jeremy J.

    Chemical biology & drug design, 08/2007, Letnik: 70, Številka: 2
    Journal Article

    Herein, we report the discovery of novel, proline‐based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional incorporation of 1‐(4‐amino‐3‐fluoro‐phenyl)‐1H‐pyridin‐2‐one 22, as a P4 pharmacophore, we discovered compound 7 (PD 0348292). This compound is a selective, orally bioavailable, efficacious FXa inhibitor that is currently in phase II clinical trials for the treatment and prevention of thrombotic disorders.

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