论文信息 - Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.

Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.

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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