Research Topics
| Anthony KreftSummaryAffiliation: Wyeth Research Country: USA Publications
| Collaborators
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Detail Information
Publications
Brain and plasma exposure profiling in early drug discovery using cassette administration and fast liquid chromatography-tandem mass spectrometryMei Yi Zhang
Chemical and Screening Sciences, Wyeth Research, CN8000, Princeton, NJ 08543 8000, USA
J Pharm Biomed Anal 34:359-68. 2004..The method described here has been used for providing early brain penetration information in several CNS exploratory and discovery programs...
Discovery of a novel series of Notch-sparing gamma-secretase inhibitorsAnthony Kreft
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Bioorg Med Chem Lett 18:4232-6. 2008..Lead optimization studies led to the discovery of analog 8e with improved gamma-secretase inhibitory potency and Notch-sparing selectivity...
Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's diseaseRobert L Martone
Wyeth Research, Departments of Discovery Neuroscience, Princeton, New Jersey 08543, USA
J Pharmacol Exp Ther 331:598-608. 2009..In healthy human volunteers, oral administration of a single dose of GSI-953 produces dose-dependent changes in plasma Abeta levels, confirming pharmacodynamic activity of GSI-953 in humans...
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitorsEric Gundersen
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Bioorg Med Chem Lett 15:1891-4. 2005..Described below is a series of gamma-secretase inhibitors designed from a scaffold identified by a ROCS [J. Comput. Chem.1996, 17, 1653] search of the corporate database...
