Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.

Costanzo, Michael J; Yabut, Stephen C; Zhang, Han-Cheng; White, Kimberley B; de Garavilla, Lawrence; Wang, Yuanping; Minor, Lisa K; Tounge, Brett A; Barnakov, Alexander N; Lewandowski, Frank; Milligan, Cynthia; Spurlino, John C; Abraham, William M; Boswell-Smith, Victoria; Page, Clive P; Maryanoff, Bruce E

Costanzo, Michael J; Yabut, Stephen C; Zhang, Han-Cheng; White, Kimberley B; de Garavilla, Lawrence; Wang, Yuanping; Minor, Lisa K; Tounge, Brett A; Barnakov, Alexander N; Lewandowski, Frank; Milligan, Cynthia; Spurlino, John C; Abraham, William M; Boswell-Smith, Victoria; Page, Clive P; Maryanoff, Bruce E.

Affiliation

Costanzo MJ; Research and Early Development, Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, Spring House, PA 19477-0776, USA. mcostanz@prdus.jnj.com

Bioorg Med Chem Lett ; 18(6): 2114-21, 2008 Mar 15.

Article in En | MEDLINE | ID: mdl-18272363

Subject(s)

Asthma/drug therapy; Respiratory Hypersensitivity/drug therapy; Serine Proteinase Inhibitors/pharmacology; Spiro Compounds/chemical synthesis; Spiro Compounds/pharmacology; Tryptases/antagonists & inhibitors; Administration, Oral; Animals; Biological Availability; Chromatography, High Pressure Liquid; Crystallography, X-Ray; Cytochrome P-450 Enzyme Inhibitors; Disease Models, Animal; Dogs; Guinea Pigs; Humans; Microsomes, Liver/drug effects; Microsomes, Liver/enzymology; Molecular Structure; Rats; Serine Proteinase Inhibitors/chemical synthesis; Serine Proteinase Inhibitors/pharmacokinetics; Sheep; Spectrometry, Mass, Electrospray Ionization; Spiro Compounds/pharmacokinetics; Trypsin/metabolism; Tryptases/metabolism

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Respiratory Hypersensitivity / Asthma / Spiro Compounds / Serine Proteinase Inhibitors / Tryptases Type of study: Evaluation_studies Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Type: Article Affiliation country: United States

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