Fluorinated piperidine acetic acids as γ-secretase modulators

The discovery and optimization of a novel class of difluoropiperidine acetic acid γ-secretase modulators is described. These compounds selectivity inhibit the formation of the more pathogenic Aβ42 without impacting Aβ40 production and, importantly, undesired Notch cleavage. We report herein a novel...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-01, Vol.20 (2), p.755-758
Hauptverfasser:	Stanton, Matthew G., Hubbs, Jed, Sloman, David, Hamblett, Christopher, Andrade, Paula, Angagaw, Minilik, Bi, Grace, Black, Regina M., Crispino, Jamie, Cruz, Jonathan C., Fan, Eric, Farris, Georgia, Hughes, Bethany L., Kenific, Candia M., Middleton, Richard E., Nikov, George, Sajonz, Peter, Shah, Sanjiv, Shomer, Nirah, Szewczak, Alexander A., Tanga, Flobert, Tudge, Matthew T., Shearman, Mark, Munoz, Benito
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetates - chemical synthesis Acetates - chemistry Acetates - pharmacokinetics Alzheimer’s disease Amyloid beta-Peptides - genetics Amyloid beta-Peptides - metabolism Amyloid Precursor Protein Secretases - metabolism Animals Biological and medical sciences Diazonium Compounds - chemistry Disease Models, Animal Fluorine - chemistry Medical sciences Mice Mice, Transgenic Neuropharmacology Peptide Fragments - genetics Peptide Fragments - metabolism Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacokinetics Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rats Receptors, Notch - metabolism γ-Secretase
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