Nicholas Stock

Summary

Publications

  1. ncbi The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent
    Nicholas Stock
    Department of Chemistry, Merck Research Laboratories, 3535 General Atomics Ct, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:2219-23. 2006
  2. doi 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administ
    Nicholas Stock
    Amira Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:4598-601. 2010
  3. doi 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:213-7. 2010
  4. doi 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103)
    John H Hutchinson
    Departments of Chemistry, Amira Pharmaceuticals, San Diego, California 92121, USA
    J Med Chem 52:5803-15. 2009
  5. doi Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:1173-6. 2010
  6. ncbi Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
    Nicholas D Smith
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:3197-200. 2005
  7. doi Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:1036-40. 2011
  8. pmc Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor
    Gretchen Bain
    Bristol Myers Squibb, San Diego, CA 92121, USA
    Br J Clin Pharmacol 75:779-90. 2013
  9. ncbi Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor
    Steve F Poon
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:2259-63. 2005
  10. ncbi Identification of the first potent, selective and bioavailable PPARĪ± antagonist
    Yalda Bravo
    Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA Electronic address
    Bioorg Med Chem Lett 24:2267-72. 2014

Collaborators

Detail Information

Publications13

  1. ncbi The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent
    Nicholas Stock
    Department of Chemistry, Merck Research Laboratories, 3535 General Atomics Ct, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:2219-23. 2006
    ....
  2. doi 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administ
    Nicholas Stock
    Amira Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:4598-601. 2010
    ..Dermal application of 6 using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling...
  3. doi 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:213-7. 2010
    ..Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model...
  4. doi 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103)
    John H Hutchinson
    Departments of Chemistry, Amira Pharmaceuticals, San Diego, California 92121, USA
    J Med Chem 52:5803-15. 2009
    ..Compound 11j was selected for clinical development and has successfully completed phase 1 trials in healthy volunteers...
  5. doi Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:1173-6. 2010
    ..A tight-binding inhibitor 5j with a long off-rate provided sustained receptor occupancy despite poor oral pharmacokinetics...
  6. ncbi Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
    Nicholas D Smith
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:3197-200. 2005
    ..Constant infusion studies using 17 demonstrate that extrapolated brain levels of 16 may be maintained for over 24h in rats...
  7. doi Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:1036-40. 2011
    ....
  8. pmc Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor
    Gretchen Bain
    Bristol Myers Squibb, San Diego, CA 92121, USA
    Br J Clin Pharmacol 75:779-90. 2013
    ....
  9. ncbi Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor
    Steve F Poon
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:2259-63. 2005
    ..Transforming the lactone moiety of the furanone to an imidate or an ortho-ester with a hydrophilic, endogenous appendage resulted in water soluble pro-drugs that converted to the parent drug in vivo...
  10. ncbi Identification of the first potent, selective and bioavailable PPARĪ± antagonist
    Yalda Bravo
    Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA Electronic address
    Bioorg Med Chem Lett 24:2267-72. 2014
    ..Compound 33 demonstrated excellent potency, selectivity against other nuclear hormone receptors, and good pharmacokinetics in mouse. ..
  11. doi Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist
    Shankar Venkatraman
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 19:5803-6. 2009
    ..The ethyl ester prodrug of 13 demonstrated excellent receptor occupancy after oral dosing in rats...
  12. ncbi N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels
    Jongwon Lim
    Department of Chemistry, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:1913-6. 2004
    ..Partial saturation of the acridine ring was also pursued and provided a compound with higher binding affinity than 1...
  13. ncbi Glucuronidation of carboxylic acid containing compounds by UDP-glucuronosyltransferase isoforms
    Kayo Sakaguchi
    Merck Research Laboratories, San Diego, 3535 General Atomics Court, San Diego, CA 92121, USA
    Arch Biochem Biophys 424:219-25. 2004
    ..These data indicate that UGT2B7 could be the major isoform involved in the glucuronidation of carboxylic acid compounds in humans...