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. ncbi request reprint Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States Electronic address
    Bioorg Med Chem Lett 24:2079-85. 2014
  4. 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
  5. ncbi 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
  6. 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
  7. 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
  8. 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
  9. ncbi request reprint Selective orexin 2 receptor antagonism blocks cue-induced reinstatement, but not nicotine self-administration or nicotine-induced reinstatement
    Jason M Uslaner
    Departments of Pharmacology, Merck and Co, Inc, West Point, PA 19486, USA Electronic address
    Behav Brain Res 269:61-5. 2014
  10. 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

Collaborators

Detail Information

Publications12

  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. ncbi request reprint Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States Electronic address
    Bioorg Med Chem Lett 24:2079-85. 2014
    ..These heterocycles were utilized to synthesize analogs in short order with high levels of potency on orexin 1 and orexin 2 receptors as well as in vivo sleep efficacy in the rat...
  4. 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
    ....
  5. ncbi 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
    ....
  6. 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...
  7. 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. ..
  8. 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
    ....
  9. ncbi request reprint Selective orexin 2 receptor antagonism blocks cue-induced reinstatement, but not nicotine self-administration or nicotine-induced reinstatement
    Jason M Uslaner
    Departments of Pharmacology, Merck and Co, Inc, West Point, PA 19486, USA Electronic address
    Behav Brain Res 269:61-5. 2014
    ..These findings indicate that orexin 2 receptor antagonism might have utility for attenuating relapse, particularly for patients sensitive to environmental stimuli associated with drug taking...
  10. 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
    ....
  11. 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...
  12. 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
    ....