Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines

Journal of Medicinal Chemistry

Volumn 46, Issue 4, 2003, Pages 461-473

  Burgey, Christopher S ^a   Robinson, Kyle A ^a   Lyle, Terry A ^a   Sanderson, Philip E J ^a   Lewis, S Dale ^a   Lucas, Bobby J ^a   Krueger, Julie A ^a   Singh, Rominder ^a   Miller Stein, Cynthia ^a   White, Rebecca B ^a   Wong, Bradley ^a   Lyle, Elizabeth A ^a   Williams, Peter D ^a   Coburn, Craig A ^a   Dorsey, Bruce D ^a   Barrow, James C ^a   Stranieri, Maria T ^a   Holahan, Marie A ^a   Sitko, Gary R ^a   Cook, Jacquelynn J ^a   McMasters, Daniel R ^a   McDonough, Colleen M ^a   Sanders, William M ^a   Wallace, Audrey A ^a   Clayton, Franklin C ^a   Bohn, Dennis ^a   Leonard, Yvonne M ^a   Detwiler Jr , Theodore J ^a   Lynch Jr , Joseph J ^a   Yan, Youwei ^a   Chen, Zhongguo ^a   Kuo, Lawrence ^a   Gardell, Stephen J ^a   Shafer, Jules A ^a   Vacca, Joseph P ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 PHENETHYLAMINO) 6 METHYLPYRAZINONE ACETAMIDE; 3 AMINOPYRAZINONE ACETAMIDE; 3 FLUORO 2 PYRIDYLMETHYL 3 [2,2 DIFLUORO 2 (2 PYRIDYL)ETHYLAMINO] 6 CHLOROPYRAZIN 2 ONE 1 ACETAMIDE; 3 FLUORO 2 PYRIDYLMETHYL 3 [2,2 DIFLUORO 2 (2 PYRIDYL)ETHYLAMINO] 6 CYANOPYRAZIN 2 ONE 1 ACETAMIDE; 3 FLUORO 2 PYRIDYLMETHYL 3 [2,2 DIFLUORO 2 (2 PYRIDYL)ETHYLAMINO] 6 METHYLPYRAZIN 2 ONE 1 ACETAMIDE; HEPARIN; PYRIDINE DERIVATIVE; THROMBIN INHIBITOR; UNCLASSIFIED DRUG; WARFARIN;

ANIMAL EXPERIMENT; ANTICOAGULANT THERAPY; ARTICLE; CHEMICAL MODIFICATION; DOG; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; MONKEY; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ACETAMIDES; ADMINISTRATION, ORAL; ANIMALS; ANTICOAGULANTS; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; DOGS; MACACA MULATTA; MODELS, MOLECULAR; PROTEASE INHIBITORS; PYRAZINES; PYRIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBIN;

EID: 0037434510     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020311f     Document Type: Article

References (35)

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