Thomas A Comery

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease
    Thomas A Comery
    Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Neurosci 25:8898-902. 2005
  2. doi Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia
    Steven M Grauer
    Wyeth Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Pharmacol Exp Ther 331:574-90. 2009
  3. doi 1-Sulfonylindazoles as potent and selective 5-HT6 ligands
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:2413-5. 2009
  4. doi Identification of a series of benzoxazoles as potent 5-HT6 ligands
    Kevin G Liu
    Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:1115-7. 2009
  5. doi 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists
    Kevin G Liu
    Wyeth Research, CN 8000, Princeton, New Jersey 08543, United States
    J Med Chem 53:7639-46. 2010
  6. doi Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:3214-6. 2009
  7. doi 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists
    Simon N Haydar
    Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 53:2521-7. 2010
  8. doi The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists
    Wayne E Childers
    Chemical Sciences, Pfizer Global Research and Development, Princeton, New Jersey 08543 8000, USA
    J Med Chem 53:4066-84. 2010
  9. doi Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem 19:650-62. 2011
  10. doi Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)
    John Dunlop
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    J Pharmacol Exp Ther 328:766-76. 2009

Detail Information

Publications25

  1. ncbi Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease
    Thomas A Comery
    Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Neurosci 25:8898-902. 2005
    ..Furthermore, they suggest that acute treatment with GSI may provide improved cognitive functioning as well as disease-modifying effects in Alzheimer's disease...
  2. doi Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia
    Steven M Grauer
    Wyeth Discovery Neuroscience, Wyeth Research, CN8000, Princeton, New Jersey 08543, USA
    J Pharmacol Exp Ther 331:574-90. 2009
    ..Together, our results suggest that PDE10A inhibitors alleviate both dopaminergic and glutamatergic dysfunction thought to underlie schizophrenia, which may contribute to the broad-spectrum efficacy...
  3. doi 1-Sulfonylindazoles as potent and selective 5-HT6 ligands
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:2413-5. 2009
    ..One compound exemplified in this series showed 24% oral bioavailability and in vivo efficacy in a NOR cognition model at 10mg/kg following an oral administration in rats...
  4. doi Identification of a series of benzoxazoles as potent 5-HT6 ligands
    Kevin G Liu
    Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:1115-7. 2009
    ..The synthesis and detailed SAR of this class of compounds are reported. The compounds have been shown to be full antagonists in a cyclic AMP functional assay...
  5. doi 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists
    Kevin G Liu
    Wyeth Research, CN 8000, Princeton, New Jersey 08543, United States
    J Med Chem 53:7639-46. 2010
    ..The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described...
  6. doi Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 19:3214-6. 2009
    ..Herein, we report the identification of a novel series of 3-piperidinyl-5-sulfonylindazole derivatives as potent 5-HT(6) antagonists. The synthesis and SAR of this class of compounds are reported...
  7. doi 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists
    Simon N Haydar
    Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
    J Med Chem 53:2521-7. 2010
    ..The synthesis and structure-activity relationship of this potent class are discussed...
  8. doi The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists
    Wayne E Childers
    Chemical Sciences, Pfizer Global Research and Development, Princeton, New Jersey 08543 8000, USA
    J Med Chem 53:4066-84. 2010
    ....
  9. doi Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists
    Kevin G Liu
    Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem 19:650-62. 2011
    ..Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT(6) antagonists. The synthesis and detailed SAR of this class of compounds are reported...
  10. doi Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)
    John Dunlop
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    J Pharmacol Exp Ther 328:766-76. 2009
    ..This latter observation provides further evidence in support of the potential therapeutic utility of alpha7 nAChR PAMs in schizophrenia...
  11. pmc Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade
    J Steven Jacobsen
    Departments of Discovery Neuroscience and Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 105:8754-9. 2008
    ....
  12. doi (S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor
    Derek C Cole
    Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 19:926-9. 2009
    ..5-fold) gamma-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol 7.b.2 (Abeta(40/42) EC(50)=28 nM), which is efficacious in reduction of Abeta production in vivo...
  13. pmc Early-onset behavioral and synaptic deficits in a mouse model of Alzheimer's disease
    J Steven Jacobsen
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Proc Natl Acad Sci U S A 103:5161-6. 2006
    ..Overall, these data show that the perforant path input from the entorhinal cortex to the DG is compromised both structurally and functionally, and this pathology is manifested in memory defects long before significant plaque deposition...
  14. ncbi The LXR agonist TO901317 selectively lowers hippocampal Abeta42 and improves memory in the Tg2576 mouse model of Alzheimer's disease
    David R Riddell
    Discovery Neuroscience, Wyeth Research, CN8000, Princeton, NJ 08543, USA
    Mol Cell Neurosci 34:621-8. 2007
    ..These data demonstrate that LXR agonists do not directly inhibit APP processing but rather facilitate the clearance of Abeta42 and may represent a novel therapeutic approach to Alzheimer's disease...
  15. doi Social odor recognition: a novel behavioral model for cognitive dysfunction in Parkinson's disease
    Michael M Monaghan
    Discovery Neuroscience, Pfizer Global Research and Development, CN8000, Princeton, NJ 08534, USA
    Neurodegener Dis 7:153-9. 2010
    ..However, cognitive impairments in PD patients are a common clinical feature that has gained increased attention...
  16. doi The supra-additive hyperactivity caused by an amphetamine-chlordiazepoxide mixture exhibits an inverted-U dose response: negative implications for the use of a model in screening for mood stabilizers
    Michele P Kelly
    Department of Neuroscience, Discovery Research, Wyeth, Princeton, NJ 08852, USA
    Pharmacol Biochem Behav 92:649-54. 2009
    ..We argue that these data, in addition to other practical and theoretical concerns surrounding the model, limit the utility of the AMPH-CDP mixture model in drug discovery...
  17. doi A cog in cognition: how the alpha 7 nicotinic acetylcholine receptor is geared towards improving cognitive deficits
    Steven C Leiser
    Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, United States
    Pharmacol Ther 122:302-11. 2009
    ..This review will focus on the recent work highlighting the role of alpha7 in cognition and cognitive processes...
  18. doi WAY-163909, a 5-HT2C agonist, enhances the preclinical potency of current antipsychotics
    Steven M Grauer
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Psychopharmacology (Berl) 204:37-48. 2009
    ....
  19. pmc Phosphodiesterase 11A in brain is enriched in ventral hippocampus and deletion causes psychiatric disease-related phenotypes
    Michele P Kelly
    Pfizer Research, Princeton, NJ 08852, USA
    Proc Natl Acad Sci U S A 107:8457-62. 2010
    ..Together, our data provide convincing evidence that PDE11A expression is restricted in the brain but plays a significant role in regulating brain function...
  20. doi Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists
    Derek C Cole
    Chemical Sciences, Wyeth Research, 401 N Middletown Rd Pearl River, NY 10965, United States
    Bioorg Med Chem Lett 20:1237-40. 2010
    ..Optimization of the physical properties of the series led to (S)-6n, with improved brain to plasma exposure and efficacy in both water intake and novel object recognition models...
  21. doi SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist
    Simon N Haydar
    Chemical Sciences and Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
    Bioorg Med Chem 17:5247-58. 2009
    ..The SAR and biological evaluation of this series of compounds are discussed...
  22. doi Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405)
    Warren D Hirst
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    J Pharmacol Exp Ther 325:134-45. 2008
    ..These results further support the rationale for use of this compound class in the treatment of cognitive dysfunction associated with psychiatric and neurological conditions...
  23. doi The 5-HT(2C) receptor agonist WAY-163909 decreases impulsivity in the 5-choice serial reaction time test
    Rachel Navarra
    Discovery Neuroscience, CN8000, Princeton, NJ 08543, USA
    Behav Brain Res 188:412-5. 2008
    ..WAY-163909 treatment selectively and dose-dependently decreased impulsivity suggesting that agonism of the 5-HT(2C) receptor may be useful for modulating impulsivity in disease states where impulsivity is a pathological feature...
  24. doi A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands
    Kevin G Liu
    Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
    Bioorg Med Chem Lett 18:3929-31. 2008
    ..A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands is reported...
  25. pmc ApoE promotes the proteolytic degradation of Abeta
    Qingguang Jiang
    Alzheimer Research Laboratory, Department of Neurosciences, Case Western Reserve University School of Medicine, Cleveland, OH 44106, USA
    Neuron 58:681-93. 2008
    ..GW3965 treatment also reversed contextual memory deficits. These data demonstrate a mechanism through which ApoE facilitates the clearance of Abeta from the brain and suggest that LXR agonists may represent a novel therapy for AD...