Factor Xa (fXa) plays a critical role in the coagulation cascade, serving as the point of
convergence of the intrinsic and extrinsic pathways. Together with nonenzymatic cofactor Va and …

Modification of a series of pyrazole factor Xa inhibitors to incorporate an aminobenzisoxazole
as the P 1 ligand resulted in compounds with improved selectivity for factor Xa relative to …

The dose-limiting issue with available anticoagulant therapies is bleeding. Is there an approach
that could provide antithrombotic protection with reduced bleeding? One hypothesis is …

Intravascular clot formation is an important factor in a number of cardiovascular diseases.
Therefore, the prevention of blood coagulation has become a major target for new therapeutic …

A series of benzamidine isoxazoline derivatives was evaluated for their inhibitory potency
against purified human factor Xa (fXa) and in a rabbit model of arteriovenous shunt thrombosis …

Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to
demonstrate robust efficacy with a low bleeding risk profile. Herein, we describe a series of …

With the introduction of thrombin and factor Xa inhibitors to the oral anticoagulant market,
significant improvements in both efficacy and safety have been achieved. Early clinical and …

Factor XIa (FXIa) is a blood coagulation enzyme that is involved in the amplification of
thrombin generation. Mounting evidence suggests that direct inhibition of FXIa can block …

BMS-654457 ((+) 3′-(6-carbamimidoyl-4-methyl-4-phenyl-1,2,3,4-tetrahydro-quinolin-2-yl)-4-carbamoyl-5′-(3-methyl-butyrylamino)-biphenyl-2-carboxylic
acid) is a small-molecule …

A novel series of macrocyclic FXIa inhibitors was designed based on our lead acyclic phenyl
imidazole chemotype. Our initial macrocycles, which were double-digit nanomolar FXIa …