697284-64-3Relevant articles and documents
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa
Mederski, Werner W.K.R.,Cezanne, Bertram,Amsterdam, Christoph Van,Bühring, Karl-Ulrich,Dorsch, Dieter,Gleitz, Johannes,M?rz, Joachim,Tsaklakidis, Christos
, p. 5817 - 5822 (2007/10/03)
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.