Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.

Bell, I M; Erb, J M; Freidinger, R M; Gallicchio, S N; Guare, J P; Guidotti, M T; Halpin, R A; Hobbs, D W; Homnick, C F; Kuo, M S; Lis, E V; Mathre, D J; Michelson, S R; Pawluczyk, J M; Pettibone, D J; Reiss, D R; Vickers, S; Williams, P D; Woyden, C J

Bell, I M; Erb, J M; Freidinger, R M; Gallicchio, S N; Guare, J P; Guidotti, M T; Halpin, R A; Hobbs, D W; Homnick, C F; Kuo, M S; Lis, E V; Mathre, D J; Michelson, S R; Pawluczyk, J M; Pettibone, D J; Reiss, D R; Vickers, S; Williams, P D; Woyden, C J.

Affiliation

Bell IM; Department of Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania 19486, USA.

J Med Chem ; 41(12): 2146-63, 1998 Jun 04.

Article in En | MEDLINE | ID: mdl-9622556

Subject(s)

Oxazines; Pyridines; Receptors, Oxytocin/antagonists & inhibitors; Administration, Oral; Animals; Biological Availability; Cell Line; Chromatography, High Pressure Liquid; Dogs; Female; Humans; Kidney/cytology; Kidney/embryology; Kidney/metabolism; Liver/metabolism; Male; Mass Spectrometry; Oxazines/chemical synthesis; Oxazines/metabolism; Oxazines/pharmacokinetics; Oxazines/pharmacology; Pregnancy; Pyridines/chemical synthesis; Pyridines/metabolism; Pyridines/pharmacokinetics; Pyridines/pharmacology; Rats; Receptors, Oxytocin/metabolism; Recombinant Proteins/antagonists & inhibitors; Recombinant Proteins/metabolism; Spectrophotometry, Ultraviolet; Uterine Contraction/drug effects; Uterus/drug effects; Uterus/physiology

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Collection: 01-internacional Database: MEDLINE Main subject: Oxazines / Pyridines / Receptors, Oxytocin Language: En Journal: J Med Chem Year: 1998 Document type: Article

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XML

PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Oxazines / Pyridines / Receptors, Oxytocin Language: En Journal: J Med Chem Year: 1998 Document type: Article