Donna M Barten

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. doi request reprint Therapeutic strategies for Alzheimer's disease
    Donna M Barten
    Bristol Myers Squibb, Neuroscience Drug Discovery, 5 Research Parkway, Wallingford, CT 06492, USA
    Mol Neurobiol 37:171-86. 2008
  2. doi request reprint Tau transgenic mice as models for cerebrospinal fluid tau biomarkers
    Donna M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, Wallingford, CT 06492, USA
    J Alzheimers Dis 24:127-41. 2011
  3. doi request reprint Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027
    Donna M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, Wallingford, Connecticut 06492, USA
    J Neurosci 32:7137-45. 2012
  4. ncbi request reprint Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor
    D M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, P O Box 5100, 3CD 405, 5 Research Pkwy, Wallingford, CT 06492, USA
    J Pharmacol Exp Ther 312:635-43. 2005
  5. ncbi request reprint Gamma-secretase inhibitors for Alzheimer's disease: balancing efficacy and toxicity
    Donna M Barten
    Bristol Myers Squibb, Pharmaceutical Research Institute, Neuroscience Drug Discovery, Wallingford, Connecticut 06492, USA
    Drugs R D 7:87-97. 2006
  6. doi request reprint Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase
    Carl P Bergstrom
    Department of Discovery Chemistry, Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:464-8. 2008
  7. doi request reprint 2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors
    Michael F Parker
    Molecular Sciences and Candidate Optimization and Neuroscience Discovery Biology, Bristol Myers Squibb R and D, 5 Research Parkway, Wallingford, CT 06492, United States
    Bioorg Med Chem Lett 22:6828-31. 2012
  8. ncbi request reprint Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase
    Carl P Bergstrom
    Department of Discovery Chemistry, Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:175-8. 2008
  9. doi request reprint P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice
    Jere E Meredith
    Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT, USA
    J Pharmacol Exp Ther 326:502-13. 2008
  10. ncbi request reprint Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheime
    C V C Prasad
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:4006-11. 2007

Collaborators

Detail Information

Publications22

  1. doi request reprint Therapeutic strategies for Alzheimer's disease
    Donna M Barten
    Bristol Myers Squibb, Neuroscience Drug Discovery, 5 Research Parkway, Wallingford, CT 06492, USA
    Mol Neurobiol 37:171-86. 2008
    ..In summary, plaques, tangles, neurodegeneration and dementia guide the development of multiple therapeutic approaches for AD and are the subject of this review...
  2. doi request reprint Tau transgenic mice as models for cerebrospinal fluid tau biomarkers
    Donna M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, Wallingford, CT 06492, USA
    J Alzheimers Dis 24:127-41. 2011
    ..Taken together, these assays and mouse models may be used to facilitate a deeper understanding of CSF tau in neurodegenerative disease...
  3. doi request reprint Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027
    Donna M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, Wallingford, Connecticut 06492, USA
    J Neurosci 32:7137-45. 2012
    ..Together, these data suggest that tau-mediated loss of MT stability may contribute to disease progression and that very low doses of BMS-241027 may be useful in the treatment of AD and other tauopathies...
  4. ncbi request reprint Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor
    D M Barten
    Neuroscience Drug Discovery, Bristol Myers Squibb, P O Box 5100, 3CD 405, 5 Research Pkwy, Wallingford, CT 06492, USA
    J Pharmacol Exp Ther 312:635-43. 2005
    ....
  5. ncbi request reprint Gamma-secretase inhibitors for Alzheimer's disease: balancing efficacy and toxicity
    Donna M Barten
    Bristol Myers Squibb, Pharmaceutical Research Institute, Neuroscience Drug Discovery, Wallingford, Connecticut 06492, USA
    Drugs R D 7:87-97. 2006
    ..Taken together, the results of studies to date suggest that gamma-secretase inhibitors have the potential to address a large unmet medical need if the technical challenges can be overcome...
  6. doi request reprint Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase
    Carl P Bergstrom
    Department of Discovery Chemistry, Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:464-8. 2008
    ..Carbamate 54 was found to significantly reduce brain Abeta in transgenic mice. 54 was also found to possess markedly improved brain levels in transgenic mice compared to previously disclosed 1 and 2...
  7. doi request reprint 2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors
    Michael F Parker
    Molecular Sciences and Candidate Optimization and Neuroscience Discovery Biology, Bristol Myers Squibb R and D, 5 Research Parkway, Wallingford, CT 06492, United States
    Bioorg Med Chem Lett 22:6828-31. 2012
    ..A series of (N-benzyl-N-phenylsulfonamido)alkyl amides were developed from classic and parallel synthesis strategies. Compounds with good in vitro and in vivo γ-secretase activity were identified and described...
  8. ncbi request reprint Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase
    Carl P Bergstrom
    Department of Discovery Chemistry, Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:175-8. 2008
    ..The synthesis and gamma-secretase inhibition data for a series of nitrogen-appended N-alkylsulfonamides (11-47) are described. Inhibition of brain Abeta in transgenic mice was demonstrated by two of these compounds (23 and 44)...
  9. doi request reprint P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice
    Jere E Meredith
    Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT, USA
    J Pharmacol Exp Ther 326:502-13. 2008
    ....
  10. ncbi request reprint Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheime
    C V C Prasad
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:4006-11. 2007
    ..Chronic dosing of BMS-433796 in Tg2576 mice suggested a narrow therapeutic window and Notch-mediated toxicity at higher doses...
  11. ncbi request reprint 2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase
    C V C Prasad
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 14:3535-8. 2004
    ..2,3-Benzodiazepin-1,4-diones were designed as peptidomimetics at the carboxy terminus of hydroxyamides. Inhibition of brain Abeta production was improved by one of the compounds containing constrained modification...
  12. doi request reprint Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)
    Kenneth M Boy
    Department of Neuroscience Discovery Chemistry, Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 21:6916-24. 2011
    ..The full in vivo profile of 1i in rats and 28n in Tg 2576 mice is presented...
  13. ncbi request reprint N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors
    Michael F Parker
    Department of Discovery Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:4432-6. 2007
    ..A series of N-alkylbenzenesulfonamides were developed from a high throughput screening hit. Classic and parallel synthesis strategies were employed to produce compounds with good in vitro and in vivo gamma-secretase activity...
  14. ncbi request reprint Soluble Abeta and cognitive function in aged F-344 rats and Tg2576 mice
    Mark D Lindner
    Neuroscience Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Behav Brain Res 173:62-75. 2006
    ....
  15. ncbi request reprint Amino-caprolactam derivatives as gamma-secretase inhibitors
    Michael F Parker
    Department of Discovery Chemistry, Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 17:5790-5. 2007
    ..A series of amino-caprolactam sulfonamides were developed from a screening hit. Compounds with good in vitro and in vivo gamma-secretase activity are reported...
  16. doi request reprint Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
    Lorin A Thompson
    Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 21:6909-15. 2011
    ..The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats...
  17. doi request reprint The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression
    Catherine R Burton
    Bristol Myers Squibb Research and Development, Wallingford, Connecticut 06492, USA
    J Biol Chem 283:22992-3003. 2008
    ..Hypothetical mechanisms for the Abeta rise, including the "incomplete processing" and endocytic models, are discussed...
  18. ncbi request reprint Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice
    Margi E Goldstein
    Research and Development, Neuroscience Drug Discovery, Bristol Myers Squibb Co, Wallingford, CT 06492, USA
    J Pharmacol Exp Ther 323:102-8. 2007
    ....
  19. ncbi request reprint An assessment of the effects of serotonin 6 (5-HT6) receptor antagonists in rodent models of learning
    Mark D Lindner
    Department of Neuroscience, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    J Pharmacol Exp Ther 307:682-91. 2003
    ..The results of our experiments are not consistent with previous reports that suggested that 5-HT6 antagonists might have therapeutic potential for cognitive disorders...
  20. doi request reprint Pharmacodynamics of selective inhibition of γ-secretase by avagacestat
    Charles F Albright
    Research and Development, Bristol Myers Squibb, Wallingford, Connecticut 06492, USA
    J Pharmacol Exp Ther 344:686-95. 2013
    ..Our results demonstrate the selectivity of avagacestat for APP over Notch cleavage, supporting further evaluation of avagacestat for AD therapy...
  21. doi request reprint Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1
    Lawrence R Marcin
    Bristol Myers Squibb, Research and Development, 5 Research Parkway, Wallingford, CT 06492 7660, USA
    Bioorg Med Chem Lett 21:537-41. 2011
    ..The same analog exhibited a high efflux ratio in a bidirectional Caco-2 assay and was likely a substrate of the efflux transporter P-glycoprotein. X-ray crystal structures are reported for two indole HEAs in complex with BACE-1...
  22. ncbi request reprint Hydroxytriamides as potent gamma-secretase inhibitors
    C V C Prasad
    Department of Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 14:1917-21. 2004
    ..An (S)-hydroxy group or 3,5-difluorophenylacetyl group at the amino terminus and N-methyltertiary amide moiety at the carboxy terminus provided potent gamma-secretase inhibitors with an IC(50) <10 nM...