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Chuck E. Kreiman
Researcher at Amgen
Publications - 1
Citations - 50
Chuck E. Kreiman is an academic researcher from Amgen. The author has contributed to research in topics: Structure–activity relationship & Xanthene. The author has an hindex of 1, co-authored 1 publications receiving 46 citations.
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Inhibitors of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1): Identification of (S)-7-(2-Fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′H-spiro[chromeno[2,3-b]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)
Thomas Dineen,Kui Chen,Alan C. Cheng,Katayoun Derakhchan,Oleg Epstein,Joel Esmay,Dean Hickman,Chuck E. Kreiman,Isaac E. Marx,Robert C. Wahl,Paul H. Wen,Matthew Weiss,Douglas A. Whittington,Stephen J. Wood,Robert T. Fremeau,Ryan White,Vinod F. Patel +16 more
TL;DR: 4-aza substitution on the xanthene core is described as a means to increase BACE1 potency while reducing hERG binding affinity and this compound produced robust and sustained reductions of CSF and brain Aβ levels in a rat pharmacodynamic model and exhibited significantly reduced potential for QTc elongation in a cardiovascular safety model.