Discovery of 1-(3′-aminobenzisoxazol-5′-yl)-3-trifluoromethyl- N-[2-fluoro-4-[(2′-dimethylaminomethyl)imidazol-1-yl]phenyl] -1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor

Journal of Medicinal Chemistry

Volumn 48, Issue 6, 2005, Pages 1729-1744

  Quan, Mimi L ^a   Lam, Patrick Y S ^a   Han, Qi ^a   Pinto, Donald J P ^a   He, Ming Y ^a   Li, Renhua ^a   Ellis, Christopher D ^a   Clark, Charles G ^a   Teleha, Christopher A ^a   Sun, Jung Hui ^a   Alexander, Richard S ^a   Bai, Steve ^a   Luettgen, Joseph M ^a   Knabb, Robert M ^a   Wong, Pancras C ^a   Wexler, Ruth R ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATED PROTEIN C; ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 9A; CHYMOTRYPSIN; KALLIKREIN; PYRAZOLE; RAZAXABAN; THROMBIN; TRYPSIN; UNCLASSIFIED DRUG; UROKINASE;

ANIMAL MODEL; ARTICLE; CHEMICAL MODIFICATION; CHEMICAL STRUCTURE; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; NONHUMAN; PLASMA; PROTEIN BINDING; SENSITIVITY AND SPECIFICITY; SUBSTITUTION REACTION; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BLOOD PROTEINS; CACO-2 CELLS; CRYSTALLOGRAPHY, X-RAY; DOGS; FACTOR XA; FIBRINOLYTIC AGENTS; HUMANS; IMIDAZOLES; ISOXAZOLES; MODELS, MOLECULAR; PERMEABILITY; PROTEIN BINDING; PYRAZOLES; RABBITS; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBOSIS;

EID: 20144374942     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0497949     Document Type: Article

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