Shaun R Stauffer

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1788-92. 2007
  2. ncbi request reprint Small molecule inhibition of the Bcl-X(L)-BH3 protein-protein interaction: proof-of-concept of an in vivo chemopotentiator ABT-737
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 3 P O Box 4, West Point, PA 19486, USA
    Curr Top Med Chem 7:961-5. 2007
  3. doi request reprint Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 51:6259-62. 2008
  4. ncbi request reprint Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites
    Georgia B McGaughey
    Department of Molecular Systems, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1117-21. 2007
  5. ncbi request reprint Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA
    J Med Chem 46:5294-7. 2003
  6. doi request reprint Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
    Melissa Egbertson
    Medicinal Chemistry Department, WP14 2 Merck and Co, West Point, PA 19486, USA Electronic address
    Bioorg Med Chem Lett 25:4812-9. 2015
  7. pmc T-type calcium channels regulate cortical plasticity in-vivo. [corrected]
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, Philadelphia, Pennsylvania, USA
    Neuroreport 20:257-62. 2009
  8. doi request reprint Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronates
    James Z Deng
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
    Org Lett 11:345-7. 2009
  9. ncbi request reprint Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid
    Matthew G Stanton
    J Med Chem 50:3431-3. 2007
  10. ncbi request reprint Fluorescence resonance energy transfer (FRET) as a high-throughput assay for coupling reactions. Arylation of amines as a case study
    Shaun R Stauffer
    Department of Chemistry, Yale University, P O Box 208107, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 125:6977-85. 2003

Collaborators

Detail Information

Publications10

  1. ncbi request reprint Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1788-92. 2007
    ....
  2. ncbi request reprint Small molecule inhibition of the Bcl-X(L)-BH3 protein-protein interaction: proof-of-concept of an in vivo chemopotentiator ABT-737
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 3 P O Box 4, West Point, PA 19486, USA
    Curr Top Med Chem 7:961-5. 2007
    ..This review will focus on the recent advances surrounding the non-peptidic Bcl-2/X(L) inhibitor ABT-737 developed by Abbot laboratories and highlight the key structural characteristics found within this unique BH3 alpha-helical mimetic...
  3. doi request reprint Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 51:6259-62. 2008
    ..Using the crystal structure as a guide, potent compounds with good brain penetration were designed...
  4. ncbi request reprint Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites
    Georgia B McGaughey
    Department of Molecular Systems, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1117-21. 2007
    ..These X-ray structures were used to correlate K(i) values, which span over five orders of magnitude, with the calculated interaction energy, using the Merck Molecular Force Field for a series of 19 tertiary carbinamine inhibitors...
  5. ncbi request reprint Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA
    J Med Chem 46:5294-7. 2003
    ..Further, 10j accelerated clot lysis in vitro and was shown to be efficacious in a primate model of thrombosis...
  6. doi request reprint Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
    Melissa Egbertson
    Medicinal Chemistry Department, WP14 2 Merck and Co, West Point, PA 19486, USA Electronic address
    Bioorg Med Chem Lett 25:4812-9. 2015
    ....
  7. pmc T-type calcium channels regulate cortical plasticity in-vivo. [corrected]
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, Philadelphia, Pennsylvania, USA
    Neuroreport 20:257-62. 2009
    ..These results show that the T-type calcium channel plays a central role in cortical plasticity...
  8. doi request reprint Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronates
    James Z Deng
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
    Org Lett 11:345-7. 2009
    ..Use of this methodology affords greatly enhanced yields of these notoriously difficult couplings. Furthermore, mechanistic investigations suggest a possible role of copper in the catalytic cycle...
  9. ncbi request reprint Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid
    Matthew G Stanton
    J Med Chem 50:3431-3. 2007
    ....
  10. ncbi request reprint Fluorescence resonance energy transfer (FRET) as a high-throughput assay for coupling reactions. Arylation of amines as a case study
    Shaun R Stauffer
    Department of Chemistry, Yale University, P O Box 208107, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 125:6977-85. 2003
    ..Reactions with K(3)PO(4) base in aqueous mixtures of polar and nonpolar organic solvents were shown to be appropriate for the amination chemistry...