Gobbi, Luca C.; Knust, Henner; Korner, Matthias; Honer, Michael; Czech, Christian; Belli, Sara; Muri, Dieter; Edelmann, Martin R.; Hartung, Thomas; Erbsmehl, Isabella; Grall-Ulsemer, Sandra; Koblet, Andreas; Rueher, Marianne; Steiner, Sandra; Ravert, Hayden T.; Mathews, William B.; Holt, Daniel P.; Kuwabara, Hiroto; Valentine, Heather; Dannals, Robert F.; Wong, Dean F.; Borroni, Edilio published the artcile< Identification of Three Novel Radiotracers for Imaging Aggregated Tau in Alzheimer's Disease with Positron Emission Tomography>, Application In Synthesis of 112-63-0, the main research area is PET radiotracer preparation tau protein aggregate imaging Alzheimer’s; tau neurofibrillary tangle amyloid PET imaging.
Aggregates of tau and beta amyloid (Aβ) plaques constitute the histopathol. hallmarks of Alzheimer’s disease and are prominent targets for novel therapeutics as well as for biomarkers for diagnostic in vivo imaging. In recent years much attention has been devoted to the discovery and development of new PET tracers to image tau aggregates in the living human brain. Access to a selective PET tracer to image and quantify tau aggregates represents a unique tool to support the development of any novel therapeutic agent targeting pathol. forms of tau. The objective of the study described herein was to identify such a novel radiotracer. As a result of this work, we discovered three novel PET tracers (2-(4-[11C]methoxyphenyl)imidazo[1,2-a]pyridin-7-amine 7 ([11C]RO6924963), N-[11C]methyl-2-(3-methylphenyl)imidazo[1,2-a]pyrimidin-7-amine 8 ([11C]RO6931643), and [18F]2-(6-fluoropyridin-3-yl)pyrrolo[2,3-b:4,5-c’]dipyridine 9 ([18F]RO6958948)) with high affinity for tau neurofibrillary tangles, excellent selectivity against Aβ plaques, and appropriate pharmacokinetic and metabolic properties in mice and non-human primates.
Journal of Medicinal Chemistry published new progress about Alzheimer disease. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.
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