Optimization of the β-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent in vivo anticoagulant activity

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 12, 2002, Pages 1671-1674

  Guertin, Kevin R ^a,b   Gardner, Charles J ^a   Klein, Scott I ^a   Zulli, Allison L ^a   Czekaj, Mark ^a   Gong, Yong ^a   Spada, Alfred P ^a   Cheney, Daniel L ^a   Maignan, Sebastian ^a   Guilloteau, Jean Pierre ^a   Brown, Karen D ^a   Colussi, Dennis J ^a   Chu, Valeria ^a   Heran, Christopher L ^a   Morgan, Suzanne R ^a   Bentley, Ross G ^a   Dunwiddie, Christopher T ^a   Leadley, Robert J ^a   Pauls, Henry W ^a  

^a SANOFI   (France)

^b HOFFMANN LA ROCHE INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (3 CARBAMIMIDOYLBENZYL) 3 (4 (1 OXYPYRIDIN 4 YL)BENZOYLAMINO)BUTYRIC ACID METHYL ESTER; 2-(3-CARBAMIMIDOYLBENZYL)-3-(4-(1-OXYPYRIDIN-4-YL)BENZOYLAMINO)BUTYRIC ACID METHYL ESTER; AMINE OXIDE; ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; ESTER; PYRIDINE DERIVATIVE; SERINE PROTEINASE INHIBITOR; BETA AMINOESTER; BLOOD CLOTTING FACTOR 10A INHIBITOR; ESTER DERIVATIVE; FXV 673; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; HUMAN; X RAY CRYSTALLOGRAPHY; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; IN VIVO STUDY; NONHUMAN; RAT; X RAY ANALYSIS;

ANTICOAGULANTS; CRYSTALLOGRAPHY, X-RAY; CYCLIC N-OXIDES; ESTERS; FACTOR XA; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRIDINES; SERINE PROTEINASE INHIBITORS; HUMAN;

EID: 0037124202     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)00213-5     Document Type: Article

References (23)