Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: Discovery of N-(3R,6S)-6-(2,3- difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl-4-(2-oxo-2, 3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide (MK-0974)

Journal of Medicinal Chemistry

Volumn 50, Issue 23, 2007, Pages 5564-5567

  Paone, Daniel V ^a   Shaw, Anthony W ^a   Nguyen, Diem N ^a   Burgey, Christopher S ^a   Deng, James Z ^a   Kane, Stefanie A ^a   Koblan, Kenneth S ^a   Salvatore, Christopher A ^a   Mosser, Scott D ^a   Johnston, Victor K ^a   Wong, Bradley K ^a   Miller Stein, Cynthia M ^a   Hershey, James C ^a   Graham, Samuel L ^a   Vacca, Joseph P ^a   Williams, Theresa M ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCITONIN GENE RELATED PEPTIDE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; CAPROLACTAM DERIVATIVE; CAPSAICIN; MK 0974; N [6 (2,3 DIFLUOROPHENYL) 2 OXO 1 (2,2,2 TRIFLUOROETHYL)AZEPAN 3 YL] 4 (2 OXO 2,3 DIHYDRO 1H IMIDAZO[4,5 B]PYRIDIN 1 YL)PIPERIDINE 1 CARBOXAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DOG; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; MIGRAINE; NONHUMAN; RAT; RHESUS MONKEY; SKIN BLOOD FLOW; TREATMENT OUTCOME;

ADMINISTRATION, ORAL; ANIMALS; AZEPINES; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; DOGS; HUMANS; IMIDAZOLES; MACACA MULATTA; MIGRAINE DISORDERS; RATS; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE; REGIONAL BLOOD FLOW; SKIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 36148978527     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm070668p     Document Type: Article

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