Substituted 2-oxo-azepane derivatives are potent, orally active γ-secretase inhibitors - Kitas, Eric A.; Galley, Guido; Jakob-Roetne, Roland; Flohr, Alexander; Wostl, Wolfgang; Mauser, Harald; Alker, André M.; Czech, Christian; Ozmen, Laurence; David-Pierson, Pascale; Reinhardt, Dieter; Jacobsen, Helmut (Bioorganic & medicinal chemistry, 2008)
Keywords: Alzheimer’s disease; Amyloid Aβ lowering; Amyloid Precursor Protein Secretases - antagonists & inhibitors; Animals; Azepines - chemical synthesis; Azepines - chemistry; Azepines - pharmacology; Biological and medical sciences; Humans; Hydroxamic Acids - chemistry; In vivo; Medical sciences; Metabolism; Mice; Mice, Transgenic; Models, Molecular; Neuropharmacology; Pharmacology. Drug treatments; Protease Inhibitors - chemical synthesis; Protease Inhibitors - chemistry; Protease Inhibitors - pharmacology; Proteolytic activity; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease); Psychology. Psychoanalysis. Psychiatry; Psychopharmacology; Structure-Activity Relationship; γ-Secretase; Proteolytic activity; In vivo; Alzheimer’s disease; Metabolism; γ-Secretase; Amyloid Aβ lowering; Alzheimer disease; Lactam; Pyridine derivatives; Thiophene derivatives; Structure activity relation; Proteolysis; Chlorine Organic compounds; Degenerative disease; Aspartic endopeptidases; Alzheimer's disease; Nervous system diseases; Sulfonamide; Absorption Distribution Metabolisme Excretion; Enzyme; Rodentia; Oral administration; Antialzheimer agent; In vitro; Amyloid precursor protein; Cerebral disorder; Peptidases; Vertebrata; Mammalia; Mouse; β Amyloid protein; Animal; Central nervous system disease; Hydrolases; Fluorine Organic compounds; Pharmacokinetics