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 …

Abstract The coagulation factor Xa (FXa) plays a central role in the blood coagulation
cascade. Recent studies have shown that FXa is a particularly attractive target for the …

Previously, we identified cyclohexane diamine derivative 1 as orally bioavailable factor Xa
inhibitor. We have investigated two racemic cis-piperidine diamine derivatives 2 and 3 …

We previously reported on a series of cyclohexanediamine derivatives as highly potent
factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an …

Factor Xa (FXa) is well known to play a pivotal role in blood coagulation, so FXa inhibitor is a
promising drug candidate for prophylaxis and treatment of thromboembolic diseases. In the …

Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis,
inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our …

To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa)
inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and …

DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITIES OF ORALLY ACTIVE COAGULATION
FACTOR Xa INHIBITORS Page 1 DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITIES OF …

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 …

A series of glycolic and mandelic acid derivatives was synthesized and investigated for their
factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors …