Neal Green

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi request reprint Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1
    Neal J Green
    Department of Chemical Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem 11:2991-3013. 2003
  2. ncbi request reprint Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles
    Neal Green
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, USA
    J Med Chem 50:4728-45. 2007
  3. ncbi request reprint Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles
    Neelu Kaila
    Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem 15:6425-42. 2007
  4. doi request reprint Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood
    Junjun Wu
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 19:3485-8. 2009
  5. ncbi request reprint Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
    Yonghan Hu
    Department of Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 16:6067-72. 2006
  6. ncbi request reprint Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood
    J Perry Hall
    Department of Inflammation, Wyeth Research, Cambridge, Massachusetts 02140, USA
    J Biol Chem 282:33295-304. 2007
  7. ncbi request reprint Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships
    Lori Krim Gavrin
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 15:5288-92. 2005
  8. doi request reprint Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties
    Steven J Kirincich
    Chemical and Screening Sciences, Wyeth Research, MA 02140, USA
    Bioorg Med Chem 17:4383-405. 2009
  9. ncbi request reprint A rat pharmacokinetic/pharmacodynamic model for assessment of lipopolysaccharide-induced tumor necrosis factor-alpha production
    Qin Wang
    Department of Discovery Pharmacokinetics, Wyeth Research, 1 Burtt Road, Andover, MA 01810, USA
    J Pharmacol Toxicol Methods 56:67-71. 2007

Detail Information

Publications9

  1. ncbi request reprint Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1
    Neal J Green
    Department of Chemical Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem 11:2991-3013. 2003
    ..1 at equimolar stoichiometry. With this as a starting point, we report here the synthesis and initial in vitro structure-activity relationships of a series of these compounds...
  2. ncbi request reprint Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles
    Neal Green
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, USA
    J Med Chem 50:4728-45. 2007
    ....
  3. ncbi request reprint Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles
    Neelu Kaila
    Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem 15:6425-42. 2007
    ..Lead compound 4-cycloheptylamino-6-[(pyridin-3-ylmethyl)-amino]-[1,7]naphthyridine-3-carbonitrile (30) was efficacious in a rat model of LPS-induced TNF-alpha production...
  4. doi request reprint Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood
    Junjun Wu
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 19:3485-8. 2009
    ..In a LPS-stimulated rat inflammation model, compound 34 showed good efficacy in inhibiting TNF-alpha production...
  5. ncbi request reprint Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
    Yonghan Hu
    Department of Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 16:6067-72. 2006
    ..Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFalpha release when administered intraperitoneally in mice...
  6. ncbi request reprint Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood
    J Perry Hall
    Department of Inflammation, Wyeth Research, Cambridge, Massachusetts 02140, USA
    J Biol Chem 282:33295-304. 2007
    ....
  7. ncbi request reprint Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships
    Lori Krim Gavrin
    Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 15:5288-92. 2005
    ..The early exploratory work described here may lead to the discovery of compounds with significant therapeutic potential for treating rheumatoid arthritis and other inflammatory diseases...
  8. doi request reprint Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties
    Steven J Kirincich
    Chemical and Screening Sciences, Wyeth Research, MA 02140, USA
    Bioorg Med Chem 17:4383-405. 2009
    ..These compounds are active in whole blood assays, and cell-based assay results indicate that prevention of arachidonic acid release arises from selective cPLA(2)alpha inhibition...
  9. ncbi request reprint A rat pharmacokinetic/pharmacodynamic model for assessment of lipopolysaccharide-induced tumor necrosis factor-alpha production
    Qin Wang
    Department of Discovery Pharmacokinetics, Wyeth Research, 1 Burtt Road, Andover, MA 01810, USA
    J Pharmacol Toxicol Methods 56:67-71. 2007
    ..The purpose of this study was to validate a rat pharmacokinetic/pharmacodynamic (PK/PD) model for rapid assessment of drug candidates that intended to interrupt TNFalpha synthesis or release...