The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 6, 2011, Pages 1588-1592

  Watson, Nigel S ^a   Adams, Carl ^a   Belton, David ^a   Brown, David ^a   Burns Kurtis, Cynthia L ^b   Chaudry, Laiq ^a   Chan, Chuen ^a   Convery, Máire A ^a   Davies, David E ^a   Exall, Anne M ^a   Harling, John D ^a   Irvine, Stephanie ^a   Irving, Wendy R ^a   Kleanthous, Savvas ^a   McLay, Iain M ^a   Pateman, Anthony J ^a   Patikis, Angela N ^a   Roethke, Theresa J ^b   Senger, Stefan ^a   Stelman, Gary J ^b   Toomey, John R ^b   West, Robert I ^a   Whittaker, Caroline ^a   Zhou, Ping ^a   Young, Robert J ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Factor Xa; Oral inhibitors; P450 inhibition; Property based design; Structure based design

Indexed keywords

BENZAZEPINE DERIVATIVE; BLOOD CLOTTING FACTOR 10A INHIBITOR; SULFONAMIDOPYRROLIDIN 2 ONE DERIVATIVE; TETRAHYDROISOQUINOLINE; TISSUE PLASMINOGEN ACTIVATOR; UNCLASSIFIED DRUG;

ANTICOAGULATION; ARTICLE; CHEMICAL MODIFICATION; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG RESEARCH; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BENZAZEPINES; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; FACTOR XA; MOLECULAR STRUCTURE; RATS; SERINE PROTEINASE INHIBITORS; TETRAHYDROISOQUINOLINES;

EID: 79952362409     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.129     Document Type: Article

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