The race to an orally active Factor Xa inhibitor: recent advances.
ML Quan, JM Smallheer - Current Opinion in Drug Discovery & …, 2004 - europepmc.org
Factor Xa (fXa) is a key enzyme in the coagulation cascade and an essential component of
the prothrombinase complex, which activates prothrombin to thrombin, leading to fibrin clot …
the prothrombinase complex, which activates prothrombin to thrombin, leading to fibrin clot …
Synthesis and biological activity of novel 1, 2-disubstituted benzene derivatives as factor Xa inhibitors
H Koshio, F Hirayama, T Ishihara, R Shiraki… - Bioorganic & medicinal …, 2005 - Elsevier
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 …
throughput screening of the Yamanouchi compound library yielded lead compound 1 with …
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1
ML Quan, AY Liauw, CD Ellis, JR Pruitt… - Journal of medicinal …, 1999 - ACS Publications
Thrombosis is a major cause of mortality in the industrialized world. Therefore, the
prevention of blood coagulation has become a major target for new therapeutic agents. One …
prevention of blood coagulation has become a major target for new therapeutic agents. One …
Antithrombotic potential of GW813893: a novel, orally active, active-site directed factor Xa inhibitor
MA Abboud, SJ Needle, CL Burns-Kurtis… - Journal of …, 2008 - journals.lww.com
Background: Factor Xa (FXa) has been a target of considerable interest for drug
development efforts aimed at suppressing thrombosis. In this report, a new orally active …
development efforts aimed at suppressing thrombosis. In this report, a new orally active …
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants
PYS Lam, CG Clark, R Li, DJP Pinto… - Journal of medicinal …, 2003 - ACS Publications
As part of an ongoing effort to prepare orally active factor Xa inhibitors using structure-based
drug design techniques and molecular recognition principles, a systematic study has been …
drug design techniques and molecular recognition principles, a systematic study has been …
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors
ML Quan, CD Ellis, MY He, AY Liauw… - Bioorganic & medicinal …, 2003 - Elsevier
Factor Xa (fXa) is an important serine protease that holds the central position linking the
intrinsic and extrinsic activation mechanisms in the blood coagulation cascade. Therefore …
intrinsic and extrinsic activation mechanisms in the blood coagulation cascade. Therefore …
Discovery of a Tetrahydropyrimidin-2(1H)-one Derivative (TAK-442) as a Potent, Selective, and Orally Active Factor Xa Inhibitor
T Fujimoto, Y Imaeda, N Konishi, K Hiroe… - Journal of medicinal …, 2010 - ACS Publications
Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of
new anticoagulant agents. We previously reported the imidazo [1, 5-c] imidazol-3-one …
new anticoagulant agents. We previously reported the imidazo [1, 5-c] imidazol-3-one …
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2
ML Quan, CD Ellis, AY Liauw… - Journal of medicinal …, 1999 - ACS Publications
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 …
Therefore, the prevention of blood coagulation has become a major target for new …
Synthesis, Characterization, and Structure− Activity Relationships of Amidine-Substituted (Bis) benzylidene-Cycloketone Olefin Isomers as Potent and Selective Factor …
WJ Guilford, KJ Shaw, JL Dallas… - Journal of medicinal …, 1999 - ACS Publications
Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in blood coagulation
linking the intrinsic and extrinsic pathways to the final common pathway of the coagulation …
linking the intrinsic and extrinsic pathways to the final common pathway of the coagulation …
Design and synthesis of highly constrained factor Xa inhibitors: amidine-Substituted bis (benzoyl)-,-diazepan-2-ones and bis (benzylidene)-bis (gem-dimethyl) …
Two conformationally constrained templates have been designed to provide selective
inhibitors of the coagulation cascade serine protease, Factor Xa (FXa). The most active …
inhibitors of the coagulation cascade serine protease, Factor Xa (FXa). The most active …