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  • Title: Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
    Author: Mederski WW, Cezanne B, van Amsterdam C, Bühring KU, Dorsch D, Gleitz J, März J, Tsaklakidis C.
    Journal: Bioorg Med Chem Lett; 2004 Dec 06; 14(23):5817-22. PubMed ID: 15501047.
    Abstract:
    Neutral chlorothiophenecarboxamides bearing an amino acid and a substituted aniline were synthesized and investigated for their factor Xa inhibitory activity in vitro. From selected 2-methylphenyl morpholinones the solution properties were determined. The most soluble and active compounds were then investigated in different animal species to compare the pharmacokinetic parameters. This led to a potent, water soluble and orally bioavailable candidate for further development: EMD 495235.
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