Thomas S Reger

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi Positive allosteric interaction of structurally diverse T-type calcium channel antagonists
    Victor N Uebele
    Department of Depression and Circadian Disorders, Merck Research Laboratories, West Point, PA 19486, USA
    Cell Biochem Biophys 55:81-93. 2009
  2. ncbi Pyridyl amides as potent inhibitors of T-type calcium channels
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 21:1692-6. 2011
  3. ncbi Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:1173-6. 2010
  4. ncbi In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice
    Richard L Kraus
    Department of Neuroscience, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA
    J Pharmacol Exp Ther 335:409-17. 2010
  5. ncbi Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists
    Kelly Ann S Schlegel
    Department of Medicinal Chemistry, Merck and Co, Inc, West Point, PA 19486, USA
    Bioorg Med Chem Lett 20:5147-52. 2010
  6. ncbi Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
    Nicholas D Smith
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:3197-200. 2005
  7. ncbi Characterization of alpha(4)beta(1) (CD49d/CD29) on equine leukocytes: potential utility of a potent alpha(4)beta(1) (CD49d/CD29) receptor antagonist in the treatment of equine heaves (recurrent airway obstruction)
    Kelly M Treonze
    Department of Immunology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Vet Immunol Immunopathol 130:79-87. 2009
  8. ncbi 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
    Dehua Huang
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5473-6. 2004
  9. ncbi Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, West Point, Pennsylvania 19486 0004, USA
    J Clin Invest 119:1659-67. 2009
  10. ncbi Glucuronidation of carboxylic acid containing compounds by UDP-glucuronosyltransferase isoforms
    Kayo Sakaguchi
    Merck Research Laboratories, San Diego, 3535 General Atomics Court, San Diego, CA 92121, USA
    Arch Biochem Biophys 424:219-25. 2004

Collaborators

Detail Information

Publications10

  1. ncbi Positive allosteric interaction of structurally diverse T-type calcium channel antagonists
    Victor N Uebele
    Department of Depression and Circadian Disorders, Merck Research Laboratories, West Point, PA 19486, USA
    Cell Biochem Biophys 55:81-93. 2009
    ....
  2. ncbi Pyridyl amides as potent inhibitors of T-type calcium channels
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 21:1692-6. 2011
    ..Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep...
  3. ncbi Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists
    Thomas S Reger
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:1173-6. 2010
    ..A tight-binding inhibitor 5j with a long off-rate provided sustained receptor occupancy despite poor oral pharmacokinetics...
  4. ncbi In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice
    Richard L Kraus
    Department of Neuroscience, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA
    J Pharmacol Exp Ther 335:409-17. 2010
    ....
  5. ncbi Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists
    Kelly Ann S Schlegel
    Department of Medicinal Chemistry, Merck and Co, Inc, West Point, PA 19486, USA
    Bioorg Med Chem Lett 20:5147-52. 2010
    ..In vivo, 45 suppressed seizure frequency in a rat model of absence epilepsy and showed significant alterations of sleep architecture after oral dosing to rats as measured by EEG...
  6. ncbi Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
    Nicholas D Smith
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:3197-200. 2005
    ..Constant infusion studies using 17 demonstrate that extrapolated brain levels of 16 may be maintained for over 24h in rats...
  7. ncbi Characterization of alpha(4)beta(1) (CD49d/CD29) on equine leukocytes: potential utility of a potent alpha(4)beta(1) (CD49d/CD29) receptor antagonist in the treatment of equine heaves (recurrent airway obstruction)
    Kelly M Treonze
    Department of Immunology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Vet Immunol Immunopathol 130:79-87. 2009
    ..3 mg/kg, receptor blockade of >80% was observed out to 24 h with a concomitant leukocytosis. We believe that Compound B possesses suitable intrinsic and pharmacological properties to be evaluated clinically in horses affected by RAO...
  8. ncbi 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
    Dehua Huang
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5473-6. 2004
    ....
  9. ncbi Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, West Point, Pennsylvania 19486 0004, USA
    J Clin Invest 119:1659-67. 2009
    ..Together, these studies reveal what we believe to be a previously unknown role for T-type calcium channels in the regulation of sleep and weight maintenance and suggest the potential for a novel therapeutic approach to treating obesity...
  10. ncbi Glucuronidation of carboxylic acid containing compounds by UDP-glucuronosyltransferase isoforms
    Kayo Sakaguchi
    Merck Research Laboratories, San Diego, 3535 General Atomics Court, San Diego, CA 92121, USA
    Arch Biochem Biophys 424:219-25. 2004
    ..These data indicate that UGT2B7 could be the major isoform involved in the glucuronidation of carboxylic acid compounds in humans...