Keith P Moore

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Keith P Moore
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5831-5. 2007
  2. ncbi request reprint Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Stacey R Lindsley
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:4057-61. 2007
  3. doi request reprint First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates
    Sethu Sankaranarayanan
    Department of Alzheimer s Research, WP 26A 2000, Merck Research Labs, 770 Sumneytown Pike, West Point, PA 19486, USA
    J Pharmacol Exp Ther 328:131-40. 2009
  4. doi request reprint Attenuation of scratch-induced reactive astrogliosis by novel EphA4 kinase inhibitors
    Sophie Parmentier-Batteur
    Merck and Co, Inc, West Point, Pennsylvania 19486 0004, USA
    J Neurochem 118:1016-31. 2011

Collaborators

Detail Information

Publications4

  1. ncbi request reprint Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Keith P Moore
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5831-5. 2007
    ..Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one case, potency was compromised in the process...
  2. ncbi request reprint Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
    Stacey R Lindsley
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:4057-61. 2007
    ..These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability...
  3. doi request reprint First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates
    Sethu Sankaranarayanan
    Department of Alzheimer s Research, WP 26A 2000, Merck Research Labs, 770 Sumneytown Pike, West Point, PA 19486, USA
    J Pharmacol Exp Ther 328:131-40. 2009
    ..These results demonstrate the first in vivo proof of concept of CSF A beta lowering after oral administration of a BACE1 inhibitor in a nonhuman primate...
  4. doi request reprint Attenuation of scratch-induced reactive astrogliosis by novel EphA4 kinase inhibitors
    Sophie Parmentier-Batteur
    Merck and Co, Inc, West Point, Pennsylvania 19486 0004, USA
    J Neurochem 118:1016-31. 2011
    ..Taken together, these results suggest that EphA4 kinase inhibitors might interfere with the astrogliosis reaction and thereby lead to improved neurological outcome after ischemic injury...