Title: Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Journal: Journal of medicinal chemistry 20130711
Title: The mechanism of γ-Secretase dysfunction in familial Alzheimer disease.
Journal: The EMBO journal 20120516
Title: ACS chemical neuroscience molecule spotlight on Begacestat (GSI-953).
Journal: ACS chemical neuroscience 20120118
Title: Alzheimer's disease and the amyloid cascade hypothesis: a critical review.
Journal: International journal of Alzheimer's disease 20120101
Title: Remembering what's new in Alzheimer's management.
Journal: Journal of pharmacology & pharmacotherapeutics 20110101
Title: BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells.
Journal: Journal of biomedical science 20110101
Title: Drug development for Alzheimer's disease: recent progress.
Journal: Experimental neurobiology 20101201
Title: Clinical trials in CNS--SMi's eighth annual conference.
Journal: IDrugs : the investigational drugs journal 20100201
Title: Brain amyloid β protein and memory disruption in Alzheimer's disease.
Journal: Neuropsychiatric disease and treatment 20100101
Title: Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.
Journal: Alzheimer's research & therapy 20100101
Title: Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Journal: The Journal of pharmacology and experimental therapeutics 20091101
Title: [Alzheimer's disease treatment by inhibition/modulation of the gamma-secretase activity].
Journal: Rinsho shinkeigaku = Clinical neurology 20091101
Title: Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
Journal: Journal of medicinal chemistry 20091022
Title: Biological markers for early detection and pharmacological treatment of Alzheimer's disease.
Journal: Dialogues in clinical neuroscience 20090601
Title: Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Journal: Journal of medicinal chemistry 20081211
Title: Mayer SC, et al. Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. J Med Chem. 2008 Dec 11;51(23):7348-51.
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