The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based
factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are …

Inappropriate thrombus formation within blood vessels is the leading cause of mortality in
the industrialized world. Factor Xa (FXa) is a trypsin-like serine protease that plays a key role …

New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized
and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and …

Thienopyridine sulfonamide pyrrolidinones were found to be potent and selective inhibitors
of the coagulation cascade enzyme factor Xa. SAR studies led to several compounds that …

A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to
the prime site of factor Xa (FXa) were designed and synthesized. Compounds with …

The blood coagulation enzyme factor Xa (FXa) is a particularly promising target for
anticoagulant therapy, and identification of oral small-molecule inhibitors of FXa remains a …

Using N, N-dialkylated benzamidines as the novel P4 motifs, we have designed and
synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and …

This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by
modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent …

Anthranilamide-based benzamidine compound 4 and its N-substituted analogs were
designed and examined as factor Xa inhibitors using substituted benzamidines as …

Factor Xa (fXa) is a serine protease that plays a pivotal role in the coagulation cascade. High-
throughput screening of the Yamanouchi compound library yielded lead compound 1 with …