Search Results - "Tanaka, Pearl"
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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2013)“…Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson’s disease and this Letter describes the SAR of a series of dihydropteridinone based…”
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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2013)“…Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is…”
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Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch
Published in Journal of medicinal chemistry (11-07-2013)Get full text
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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce [alpha]-Synuclein Phosphorylation in Rat Brain
Published in ChemMedChem (01-08-2013)“…Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of [alpha]-synuclein in Lewy bodies, which are one of the…”
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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
Published in Journal of medicinal chemistry (11-07-2013)“…Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We…”
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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain
Published in ChemMedChem (01-08-2013)“…Polo‐like kinase‐2 (Plk‐2) has been implicated as the dominant kinase involved in the phosphorylation of α‐synuclein in Lewy bodies, which are one of the…”
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P1‐029: A comparison of conventional versus push‐pull microdialysis for the detection of amyloid β in the mouse brain
Published in Alzheimer's & dementia (01-07-2011)Get full text
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A comparison of conventional versus push-pull microdialysis for the detection of amyloid β in the mouse brain
Published in Alzheimer's & dementia (01-07-2011)Get full text
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Pharmacokinetic and pharmacodynamic investigation of ELND006, a novel APP-selective gamma-secretase inhibitor, on amyloid-β concentrations in the brain, CSF and plasma of multiple nonclinical species following oral administration
Published in Alzheimer's & dementia (01-07-2010)Get full text
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P3‐320: Pharmacokinetic and pharmacodynamic investigation of ELND006, a novel APP‐selective gamma‐secretase inhibitor, on amyloid‐β concentrations in the brain, CSF and plasma of multiple nonclinical species following oral administration
Published in Alzheimer's & dementia (01-07-2010)Get full text
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