Structural optimization affording 2-(R)-(1-(R)-3,5- bis(trifluoromethyl)phenylethoxy)-3'-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4- triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist

Journal of Medicinal Chemistry

Volumn 41, Issue 23, 1998, Pages 4607-4614

  Hale, Jeffrey J ^a   Mills, Sander G ^a   MacCoss, Malcolm ^a   Finke, Paul E ^a   Cascieri, Margaret A ^a   Sadowski, Sharon ^a   Ber, Elzbieta ^a   Chicchi, Gary G ^a   Kurtz, Marc ^a   Metzger, Joseph ^a   Eiermann, George ^a   Tsou, Nancy N ^a   Tattersall, F David ^b   Rupniak, Nadia M J ^b   Williams, Angela R ^b   Rycroft, Wayne ^b   Hargreaves, Richard ^b   MacIntyre, D Euan ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

[3,5 BIS(TRIFLUOROMETHYL)PHENYLETHOXY](4 FLUORO)PHENYL 4 (OXO 1,2,4 TRIAZOL 5 YL)METHYLMORPHOLINE; NEUROKININ 1 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANTIEMETIC ACTIVITY; ARTICLE; CONFORMATIONAL TRANSITION; DRUG CONFORMATION; DRUG EFFECT; DRUG FORMULATION; DRUG SYNTHESIS; MIGRAINE; STRUCTURE ACTIVITY RELATION; VOMITING;

ACETALS; ADMINISTRATION, ORAL; ANIMALS; BEHAVIOR, ANIMAL; BINDING, COMPETITIVE; CAPILLARY PERMEABILITY; CELL LINE; CHO CELLS; CRICETINAE; DITERPENES; ESOPHAGUS; FEMALE; FERRETS; GERBILLINAE; HINDLIMB; HUMANS; INFLAMMATION; MALE; MORPHOLINES; RECEPTORS, NEUROKININ-1; TRACHEA; URINARY BLADDER; VOMITING;

EID: 15144354434     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm980299k     Document Type: Article

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