Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Wesley F. Austin"'
Autor:
Barbara Tate, Timothy D. McKee, Robyn M. B. Loureiro, Jo Ann Dumin, Weiming Xia, Kevin Pojasek, Wesley F. Austin, Nathan O. Fuller, Jed L. Hubbs, Ruichao Shen, Jeff Jonker, Jeff Ives, Brian S. Bronk
Publikováno v:
International Journal of Alzheimer's Disease, Vol 2012 (2012)
The Amyloid Hypothesis states that the cascade of events associated with Alzheimer's disease (AD)—formation of amyloid plaques, neurofibrillary tangles, synaptic loss, neurodegeneration, and cognitive decline—are triggered by Aβ peptide dysregul
Externí odkaz:
https://doaj.org/article/ab1e212d58e445b0a7989a30b7207773
Autor:
J. L. Ives, Bronk Brian Scott, Gerd Osswald, Wesley F. Austin, Nathan O. Fuller, Jed L. Hubbs, Ruichao Shen
Publikováno v:
Organic Process Research & Development. 18:683-692
This work describes the demonstration of a kilogram-scale synthesis of a γ-secretase modulator from a plant-sterol-derived starting material. Key to developing a synthetic route capable of delivering a kilogram of the target compound was the develop
Autor:
Dieter Haag, Mark A. Findeis, Wesley F. Austin, Nathan O. Fuller, Janos Kovacs, Ruichao Shen, Steffen Phillip Creaser, Gerd Osswald, Jed L. Hubbs, J. L. Ives, Bronk Brian Scott
Publikováno v:
Organic Process Research & Development. 18:676-682
The process development and production of two cycloartenol triterpenoid glycosides on a multikilogram scale are described. The two compounds were used as key intermediates for the synthesis of a γ-secretase modulator and a novel potential therapeuti
Autor:
Ahmed F. Abdel-Magid, Jaan A. Pesti, Rajappa Vaidyanathan, Debra J. Wallace, Ian Mangion, Paul Coleman, Seb Caille, John G. Allen, Xianglin Shi, William F. Kiesman, Donald G. Walker, Hidenori Takahashi, Alessandra Bartolozzi, Thomas Simpson, Keith Fandrick, Jason Mulder, Jean-Nicolas Desrosiers, Nitin Patel, Xingzhong Zeng, Daniel Fandrick, Carl A. Busacca, Jinhua J. Song, Chris H. Senanayake, Timothy P. Heffron, Andrew McClory, Andreas Stumpf, Jason D. Burch, Benjamin D. Sherry, Donald R. Gauthier, Louis-Charles Campeau, Jessica E. Reed, Jeff B. Smaill, Shu Yu, Olivier Dirat, Jed L. Hubbs, Nathan O. Fuller, Wesley F. Austin, Ruichao Shen, Brian S. Bronk, Gerald J. Tanoury, Stephen Eastham, Cristian L. Harrison, Benjamin J. Littler, Piero L. Ruggiero, Zhifeng Ye, Anne-Laure Grillo
Publikováno v:
Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development Volume 1 ISBN: 9780841231894
Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development Volume 1
Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development Volume 1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::418479f7aad724755498862a4275ca3b
https://doi.org/10.1021/bk-2016-1239.ch010
https://doi.org/10.1021/bk-2016-1239.ch010
Autor:
Robyn M. B. Loureiro, Barbara Tate, Weiming Xia, Timothy D. McKee, J. L. Ives, Bronk Brian Scott, Ruichao Shen, Nathan O. Fuller, Wesley F. Austin, Steffen Phillip Creaser, Jed Hubbs
Publikováno v:
Journal of Medicinal Chemistry. 55:9270-9282
A series of triterpene-based γ-secretase modulators is optimized. An acetate present at the C24 position of the natural product was replaced with either carbamates or ethers to provide compounds with better metabolic stability. With one of those pha
Publikováno v:
Tetrahedron. 64:915-925
(Trialkylsilyl)vinylketenes react with lithium ynolates to generate 3-(oxido)dienylketenes, which undergo rapid 6π-electrocyclization. The ultimate products of this benzannulation are highly substituted resorcinol monosilyl ethers, which are formed
Autor:
Jianguo Ma, Nathan O. Fuller, Bronk Brian Scott, Jian Li, Wesley F. Austin, Ruichao Shen, Timothy D. McKee, Jo Ann Dumin, Jed L. Hubbs, Zhen Gong, Robyn M. B. Loureiro, Barbara Tate, J. L. Ives
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(7)
Early lead compounds in this gamma secretase modulator series were found to potently inhibit CYP3A4 and other human CYP isoforms increasing their risk of causing drug–drug-interactions (DDIs). Using structure–activity relationships and CYP3A4 str
Autor:
Jo Ann Dumin, Jed L. Hubbs, Wesley F. Austin, Nathan O. Fuller, Timothy D. McKee, Jeff Jonker, Jeff Ives, Ruichao Shen, Bronk Brian Scott, Robyn M. B. Loureiro, Barbara Tate
Publikováno v:
Alzheimer's Research & Therapy
Introduction Modulation of the gamma-secretase enzyme, which reduces the production of the amyloidogenic Aβ42 peptide while sparing the production of other Aβ species, is a promising therapeutic approach for the treatment of Alzheimer's disease. Sa
Autor:
Weiming Xia, Timothy D. McKee, Wesley F. Austin, J. L. Ives, Robyn M. B. Loureiro, Barbara Tate, Nathan O. Fuller, Mark A. Findeis, Steffen Phillip Creaser, Jed L. Hubbs, Bronk Brian Scott
The discovery of a new series of γ-secretase modulators is disclosed. Starting from a triterpene glycoside γ-secretase modulator that gave a very low brain-to-plasma ratio, initial SAR and optimization involved replacement of a pendant sugar with a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32d225a43eb41a4dab52e94aea5ea53a
https://europepmc.org/articles/PMC4025870/
https://europepmc.org/articles/PMC4025870/