John A McCauley

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Orally efficacious NR2B-selective NMDA receptor antagonists
    Christopher F Claiborne
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 13:697-700. 2003
  2. ncbi request reprint NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles
    John A McCauley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    J Med Chem 47:2089-96. 2004
  3. doi request reprint Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor
    John A McCauley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 53:2443-63. 2010
  4. doi request reprint Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
    Michael T Rudd
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:7207-13. 2012
  5. doi request reprint Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease
    Michael T Rudd
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:7201-6. 2012
  6. ncbi request reprint In vitro characterization of novel NR2B selective NMDA receptor antagonists
    Laszlo Kiss
    Neuroscience Drug Discovery, Merck Research Laboratories, West Point, PA 19486, USA
    Neurochem Int 46:453-64. 2005
  7. pmc MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease
    Nigel J Liverton
    Merck Research Laboratories, Department of Medicinal Chemistry, WP42A 40, West Point, PA 19486, USA
    Antimicrob Agents Chemother 54:305-11. 2010
  8. ncbi request reprint Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists
    Kevin T Nguyen
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:3997-4000. 2007
  9. ncbi request reprint Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist
    Nigel J Liverton
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 50:807-19. 2007
  10. doi request reprint Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists
    Charles J McIntyre
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 19:5132-5. 2009

Collaborators

Detail Information

Publications13

  1. ncbi request reprint Orally efficacious NR2B-selective NMDA receptor antagonists
    Christopher F Claiborne
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 13:697-700. 2003
    ..Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects...
  2. ncbi request reprint NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles
    John A McCauley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    J Med Chem 47:2089-96. 2004
    ..Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs...
  3. doi request reprint Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor
    John A McCauley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 53:2443-63. 2010
    ....
  4. doi request reprint Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
    Michael T Rudd
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:7207-13. 2012
    ..The effect of the constraint is most dramatic against gt 1b A156 mutants where ~20-fold improvements in potency are achieved by introduction of a variety of ring systems into the P2-P4 linker...
  5. doi request reprint Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease
    Michael T Rudd
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:7201-6. 2012
    ..Cyclization of the 2-substituted quinoline substituent led to a series of tricyclic P2 compounds which also display superb gt3a potency...
  6. ncbi request reprint In vitro characterization of novel NR2B selective NMDA receptor antagonists
    Laszlo Kiss
    Neuroscience Drug Discovery, Merck Research Laboratories, West Point, PA 19486, USA
    Neurochem Int 46:453-64. 2005
    ..These results provide the first detailed functional analysis of the kinetic mechanism of MERCK 1, MERCK 2, and MERCK 3 inhibition of NMDA receptors...
  7. pmc MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease
    Nigel J Liverton
    Merck Research Laboratories, Department of Medicinal Chemistry, WP42A 40, West Point, PA 19486, USA
    Antimicrob Agents Chemother 54:305-11. 2010
    ..On the basis of this favorable profile, MK-7009 was selected for clinical development and is currently being evaluated in controlled clinical trials with both healthy volunteers and HCV-infected patients...
  8. ncbi request reprint Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists
    Kevin T Nguyen
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:3997-4000. 2007
    ..A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 29 is orally active in a carrageenan-induced rat hyperalgesia model of pain...
  9. ncbi request reprint Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist
    Nigel J Liverton
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 50:807-19. 2007
    ..Compound 20j demonstrated efficacy in in vivo rodent models of antinociception, allodynia, and Parkinson's disease...
  10. doi request reprint Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists
    Charles J McIntyre
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 19:5132-5. 2009
    ..Preferred compounds were subsequently evaluated for selectivity in an alpha(1)-adrenergic receptor binding counter-screen and a cell-based assay of NR2B activity...
  11. doi request reprint Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease
    Nigel J Liverton
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Am Chem Soc 130:4607-9. 2008
    ..The in vitro activity and selectivity as well as the rat pharmacokinetic profile of 25a compare favorably with the data for other NS3/4A protease inhibitors currently in clinical development for the treatment of HCV...
  12. ncbi request reprint Kinetic characterization of novel NR2B antagonists using fluorescence detection of calcium flux
    Bohumil Bednar
    Department of Neurology, Merck Research Laboratories, WP26A 2000 Sumneytown Pike, West Point, PA 19454, USA
    J Neurosci Methods 137:247-55. 2004
    ..All kinetic constants, obtained using our fluorescence method, correlate well with data measured by voltage clamp...
  13. ncbi request reprint Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2)
    Michael T Rudd
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 3, Merck and Co, Inc, PO Box 4, West Point, PA 19486 USA
    Curr Top Med Chem 5:869-84. 2005
    ..Structure-activity relationships as well as pharmacokinetic properties and in vivo activity are reviewed...