Anthony J Roecker

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5677-82. 2007
  2. ncbi request reprint Orexin receptor antagonists: medicinal chemistry and therapeutic potential
    Anthony J Roecker
    Department of Medicinal Chemistry Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Curr Top Med Chem 8:977-87. 2008
  3. doi request reprint Discovery of 5''-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, PA 19486 USA
    ChemMedChem 9:311-22. 2014
  4. doi request reprint Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia
    Christopher D Cox
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA
    J Med Chem 53:5320-32. 2010
  5. doi request reprint Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States
    Bioorg Med Chem Lett 20:4201-5. 2010
  6. doi request reprint Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs)
    Swati P Mercer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA Electronic address
    Bioorg Med Chem Lett 23:6620-4. 2013
  7. doi request reprint Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure
    Christopher J Winrow
    Depression and Circadian Disorders Department, Merck Research Laboratories, West Point, PA, USA
    Neuropharmacology 58:185-94. 2010
  8. doi request reprint Orexin receptors as therapeutic drug targets
    Anthony L Gotter
    Department of Neuroscience, Merck Research Laboratories, West Point, Pennsylvania, USA
    Prog Brain Res 198:163-88. 2012
  9. doi request reprint Proline bis-amides as potent dual orexin receptor antagonists
    Jeffrey M Bergman
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 18:1425-30. 2008
  10. ncbi request reprint Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Curr Top Med Chem 11:696-725. 2011

Collaborators

Detail Information

Publications10

  1. ncbi request reprint Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5677-82. 2007
    ..Crystallographic evidence of binding mode and in vivo potency data is also highlighted...
  2. ncbi request reprint Orexin receptor antagonists: medicinal chemistry and therapeutic potential
    Anthony J Roecker
    Department of Medicinal Chemistry Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Curr Top Med Chem 8:977-87. 2008
    ..Receptor subtype selectivity will also be described to highlight the tools currently available to delineate receptor-specific pharmacology...
  3. doi request reprint Discovery of 5''-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, PA 19486 USA
    ChemMedChem 9:311-22. 2014
    ....
  4. doi request reprint Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia
    Christopher D Cox
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA
    J Med Chem 53:5320-32. 2010
    ....
  5. doi request reprint Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States
    Bioorg Med Chem Lett 20:4201-5. 2010
    ..In this Letter, we describe the synthesis of constrained diazepanes having a 3,9 diazabicyclo[4.2.1]nonane bicyclic core with good oral bioavailability and sleep-promoting activity in a rat EEG model...
  6. doi request reprint Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs)
    Swati P Mercer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA Electronic address
    Bioorg Med Chem Lett 23:6620-4. 2013
    ..A compound from this series demonstrated potent sleep promotion when dosed orally to EEG telemetrized rats. ..
  7. doi request reprint Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure
    Christopher J Winrow
    Depression and Circadian Disorders Department, Merck Research Laboratories, West Point, PA, USA
    Neuropharmacology 58:185-94. 2010
    ....
  8. doi request reprint Orexin receptors as therapeutic drug targets
    Anthony L Gotter
    Department of Neuroscience, Merck Research Laboratories, West Point, Pennsylvania, USA
    Prog Brain Res 198:163-88. 2012
    ....
  9. doi request reprint Proline bis-amides as potent dual orexin receptor antagonists
    Jeffrey M Bergman
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 18:1425-30. 2008
    ..A compound from this series has demonstrated in vivo central activity when dosed peripherally in a pharmacodynamic model of orexin activity...
  10. ncbi request reprint Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Curr Top Med Chem 11:696-725. 2011
    ....