Title of article :
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa
Author/Authors :
Werner W.K.R. Mederski، نويسنده , , Bertram Cezanne، نويسنده , , Christoph van Amsterdam، نويسنده , , Karl-Ulrich Bühring، نويسنده , , Dieter Dorsch، نويسنده , , Johannes Gleitz، نويسنده , , Joachim M?rz، نويسنده , , Christos Tsaklakidis، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
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.
Keywords :
ANTICOAGULANTS , Pharmacokinetics , Factor Xa inhibitors , bertram.cezanne@merck.de , EMD 495235.* Correspondingauthors. E-mail addresses: mederski@merck.de , Chlorothiophenecarboxamides
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
