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Your search keyword '"Wuyts, Stijn"' showing total 11 results
Start Over Author "Wuyts, Stijn" Publisher american chemical society
11 results on '"Wuyts, Stijn"'

2. Discovery of N‑(4‑[18F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer.

Author

Rombouts, Frederik J. R., Declercq, Lieven, Andrés, José-Ignacio, Bottelbergs, Astrid, Chen, Lu, Iturrino, Laura, Leenaerts, Joseph E., Mariën, Jonas, Song, Fengbin, Wintmolders, Cindy, Wuyts, Stijn, Xia, Chunfang A., te Riele, Paula, Bormans, Guy, Vandenberghe, Rik, Kolb, Hartmuth, and Moechars, Diederik

Published
2019
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6. Green Chemistry Articles of Interest to the Pharmaceutical Industry.

Author

Bandichhor, Rakeshwar, Bhattacharya, Apurba, Cosbie, Andrew, Diorazio, Louis, Dunn, Peter, Fraunhoffer, Kenneth, Gallou, Fabrice, Hayler, John, Hickey, Matthew, Hinkley, Bill, Humphreys, Luke, Kaptein, Bernard, Oh, Lynette, Richardson, Paul, Roberts, Scott, White, Timothy, Wuyts, Stijn, and Jingjun Yin

Published
2015
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8. The GreenChemistry Articles of Interest.

Author

Bandichhor, Rakeshwar, Bhattacharya, Apurba, Diorazio, Louis, Dunn, Peter, Fraunhoffer, Kenneth, Gallou, Fabrice, Hayler, John, Hickey, Matthew, Hinkley, Bill, Hughes, David, Humphreys, Luke, Kaptein, Bernard, Mathew, Suju, Oh, Lynnette, Richardson, Paul, White, Timothy, and Wuyts, Stijn

Published
2014
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11. Discovery of N-(4-[ 18 F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer.

Author

Rombouts FJR, Declercq L, Andrés JI, Bottelbergs A, Chen L, Iturrino L, Leenaerts JE, Mariën J, Song F, Wintmolders C, Wuyts S, Xia CA, Te Riele P, Bormans G, Vandenberghe R, Kolb H, and Moechars D

Subjects
Alzheimer Disease diagnostic imaging, Alzheimer Disease metabolism, Animals, Cells, Cultured, Female, Fluorine Radioisotopes chemistry, Fluorine Radioisotopes pharmacokinetics, Hepatocytes metabolism, Humans, Isoquinolines chemistry, Macaca mulatta, Male, Pyridines chemistry, Rats, Rats, Wistar, Structure-Activity Relationship, Drug Discovery, Fluorine Radioisotopes metabolism, Isoquinolines pharmacokinetics, Positron-Emission Tomography, Pyridines pharmacokinetics, tau Proteins metabolism
Abstract

In Alzheimer's disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of aggregated tau a compelling biomarker. A structure-activity relationship exploration around an isoquinoline hit, followed by an exploration of tolerated fluorination positions, allowed us to identify 9 (JNJ-64326067), a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [ 18 F]9.

Published
2019
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