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  • Title: Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
    Author: Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.
    Journal: Bioorg Med Chem Lett; 2014 Aug 01; 24(15):3341-5. PubMed ID: 24951330.
    Abstract:
    In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant activity (PT EC2x), cell permeability, and oral bioavailability.
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