Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1795-8. doi: 10.1016/j.bmcl.2006.01.010. Epub 2006 Jan 24.

Abstract

We have previously reported on a series of aminobenzisoxazoles as potent, selective, and orally bioavailable factor Xa inhibitors, which culminated in the discovery of razaxaban. Herein, we describe another approach to improve factor Xa inhibitory potency and pharmacokinetic profile by incorporating basic and water soluble functionalities on the terminal ring of the P4 biaryl group found in our earlier Xa inhibitors. This approach resulted in a series of potent, selective, and orally bioavailable factor Xa inhibitors.

MeSH terms

  • Administration, Oral
  • Benzoxazoles / administration & dosage
  • Benzoxazoles / chemistry
  • Benzoxazoles / pharmacokinetics
  • Benzoxazoles / pharmacology*
  • Biological Availability
  • Factor Xa Inhibitors*
  • Serine Proteinase Inhibitors / administration & dosage
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacokinetics
  • Serine Proteinase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Benzoxazoles
  • Factor Xa Inhibitors
  • Serine Proteinase Inhibitors