Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors

Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1<i>H</i>-pyrazolo[3,4-<i>c</i>]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Donald Pinto, Michael J. Orwat, Stephanie C. Koch et al. · Journal of Medicinal Chemistry · 2007 · 397 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +14

Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl-<i>N</i>-[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1<i>H</i>-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor

Mimi L. Quan, Patrick Y. S. Lam, Qi Han et al. · Journal of Medicinal Chemistry · 2004 · 189 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +12

Discovery of 1-[3-(Aminomethyl)phenyl]-<i>N</i>-[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1<i>H</i>-pyrazole-5-carboxamide (DPC423), a Highly Potent, Selective, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Donald Pinto, Michael J. Orwat, Shuaige Wang et al. · Journal of Medicinal Chemistry · 2001 · 172 citations · Full text

Medicine, Pharmacology, Drug Discovery +11

Activation of human prothrombin by highly purified human factors V and X-a in presence of human antithrombin.

J.S. Rosenberg, David Beeler, R D Rosenberg · Journal of Biological Chemistry · 1975 · 111 citations · Full text

Life Sciences, Biochemistry, Molecular Biology +13

Structure-Based Design of Novel Guanidine/Benzamidine Mimics:  Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants

Patrick Y. S. Lam, Charles G. Clark, Renhua Li et al. · Journal of Medicinal Chemistry · 2003 · 96 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +15