Title: Nonclinical Safety Assessment of the γ-Secretase Inhibitor Avagacestat.
Journal: Toxicological sciences : an official journal of the Society of Toxicology 20180601
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: Safety and tolerability of the γ-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease.
Journal: Archives of neurology 20121101
Title: Degradation kinetics and mechanism of an oxadiazole derivative, design of a stable drug product for BMS-708163, a γ-secretase inhibitor drug candidate.
Journal: Journal of pharmaceutical sciences 20120901
Title: Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.
Journal: Journal of medicinal chemistry 20120412
Title: Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.
Journal: The Journal of pharmacology and experimental therapeutics 20111201
Title: Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.
Journal: Journal of medicinal chemistry 20111124
Title: Development and validation of sensitive and selective LC-MS/MS methods for the determination of BMS-708163, a gamma-secretase inhibitor, in plasma and cerebrospinal fluid using deprotonated or formate adduct ions as precursor ions.
Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20100901
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
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