Anthony J Roecker

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi 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 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. ncbi 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
  4. ncbi 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
  5. ncbi 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
  6. ncbi 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
  7. ncbi 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
  8. ncbi 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

Detail Information

Publications8

  1. ncbi 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 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. ncbi 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
    ....
  4. ncbi 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...
  5. ncbi 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
    ....
  6. ncbi 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
    ....
  7. ncbi 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
    ....
  8. ncbi 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...