Douglas S Johnson

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. pmc Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
    Douglas S Johnson
    Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 19:2865-9. 2009
  2. pmc Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
    Douglas S Johnson
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Future Med Chem 2:949-64. 2010
  3. doi request reprint Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, 700 Main Street, Cambridge, MA, 02139, USA
    Expert Opin Ther Pat 23:1349-66. 2013
  4. doi request reprint Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder
    Douglas S Johnson
    Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:2621-5. 2011
  5. pmc Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain
    Kay Ahn
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Chem Biol 16:411-20. 2009
  6. doi request reprint Design, Synthesis, and Pharmacological Evaluation of a Novel Series of Pyridopyrazine-1,6-dione γ-Secretase Modulators
    Martin Pettersson
    Pfizer Worldwide Research and Development, 610 Main Street, Cambridge, Massachusetts 02139, United States
    J Med Chem 57:1046-62. 2014
  7. pmc Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain
    Kay Ahn
    Pfizer Worldwide Research and Development, Groton, Connecticut, USA
    J Pharmacol Exp Ther 338:114-24. 2011
  8. pmc γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin
    Nikolay Pozdnyakov
    Pfizer Worldwide Research and Development, Cambridge, Massachusetts 02139, USA
    J Biol Chem 288:9710-20. 2013
  9. doi request reprint Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, USA
    Bioorg Med Chem Lett 22:2906-11. 2012
  10. doi request reprint Novel γ-secretase modulators: a review of patents from 2008 to 2010
    Martin Pettersson
    Pfizer Worldwide Research and Development, Neuroscience Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA
    Expert Opin Ther Pat 21:205-26. 2011

Collaborators

Detail Information

Publications14

  1. pmc Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
    Douglas S Johnson
    Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 19:2865-9. 2009
    ..Several compounds showed in vivo activity in a rat complete Freund's adjuvant (CFA) model of inflammatory pain...
  2. pmc Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
    Douglas S Johnson
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Future Med Chem 2:949-64. 2010
    ..Emerging proteomic technologies offer a means to systematically discriminate safe (selective) versus deleterious (nonselective) covalent inhibitors and thus should inspire their future design and development...
  3. doi request reprint Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, 700 Main Street, Cambridge, MA, 02139, USA
    Expert Opin Ther Pat 23:1349-66. 2013
    ..Therefore, GSMs have emerged as an important therapeutic strategy for the treatment of AD...
  4. doi request reprint Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder
    Douglas S Johnson
    Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:2621-5. 2011
    ..This strategy led to identification of PF-00217830 (2) with robust inhibition of sLMA (MED=0.3mg/kg) and DOI-induced head twitches in rats (31% and 78% at 0.3 and 1mg/kg) with no catalepsy observed at the highest dose tested (10 mg/kg)...
  5. pmc Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain
    Kay Ahn
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Chem Biol 16:411-20. 2009
    ..These data thus designate PF-3845 as a valuable pharmacological tool for in vivo characterization of the endocannabinoid system...
  6. doi request reprint Design, Synthesis, and Pharmacological Evaluation of a Novel Series of Pyridopyrazine-1,6-dione γ-Secretase Modulators
    Martin Pettersson
    Pfizer Worldwide Research and Development, 610 Main Street, Cambridge, Massachusetts 02139, United States
    J Med Chem 57:1046-62. 2014
    ....
  7. pmc Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain
    Kay Ahn
    Pfizer Worldwide Research and Development, Groton, Connecticut, USA
    J Pharmacol Exp Ther 338:114-24. 2011
    ..Based on its exceptional selectivity and in vivo efficacy, combined with long duration of action and optimal pharmacokinetic properties, PF-04457845 is a clinical candidate for the treatment of pain and other nervous system disorders...
  8. pmc γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin
    Nikolay Pozdnyakov
    Pfizer Worldwide Research and Development, Cambridge, Massachusetts 02139, USA
    J Biol Chem 288:9710-20. 2013
    ..Furthermore, the enhancement of PS1-NTF labeling by E2012-BPyne in the presence of L458 suggests a degree of cooperativity between the active site of γ-secretase and the modulatory binding site of certain GSMs...
  9. doi request reprint Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, USA
    Bioorg Med Chem Lett 22:2906-11. 2012
    ..Lead compounds such as 35 and 43 have moderate to good in vitro potency and excellent selectivity against Notch. Good oral bioavailability was achieved as well as robust brain Aβ42 lowering activity at 100 mg/kg po dose...
  10. doi request reprint Novel γ-secretase modulators: a review of patents from 2008 to 2010
    Martin Pettersson
    Pfizer Worldwide Research and Development, Neuroscience Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA
    Expert Opin Ther Pat 21:205-26. 2011
    ..This has become an important therapeutic strategy aimed at modulating Aβ production...
  11. pmc The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH)
    Marc B Skaddan
    Pfizer Worldwide Research and Development, Pfizer Inc, Eastern Point Road, Mail Stop 8274 1342, Groton, CT 06340, USA
    Nucl Med Biol 39:1058-67. 2012
    ..We report here the synthesis and in vivo evaluation of [(18)F]PF-9811, a novel PET ligand for non-invasive imaging of FAAH in the brain...
  12. ncbi request reprint Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity
    Kyunghye Ahn
    Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Biochemistry 46:13019-30. 2007
    ....
  13. doi request reprint Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses
    Yasong Lu
    MS 220 4546, Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    J Pharmacol Exp Ther 342:366-75. 2012
    ..We further discuss the implications of our findings to drug discovery and development with regard to preclinical PK/PD characterization and clinical prediction of Aβ lowering in the brain...
  14. doi request reprint Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist
    Snahel D Patel
    Pfizer Global Research and Development, Cambridge Laboratories, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:5689-93. 2008
    ..Structure-activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other alpha(2)-AR subtypes...