Zobrazeno 1 - 10
of 70
pro vyhledávání: '"Michael Aaron Brodney"'
Autor:
Laura A. McAllister, Michael Aaron Brodney, Jane M. Withka, Jiangli Yan, Thomas N. O'Connell, Laurence Philippe, Kevin Ogilvie, Lara C. Czabaniuk, Matthew Frank Brown, Guoyun Bai, Adam M. Gilbert, Daniel P. Uccello, Erik Alphie Lachapelle, Chao Li, Michael J. Shapiro, Christopher Ryan Butler, Romelia Salomon-Ferrer, Jeremy T. Starr
Publikováno v:
ACS Med Chem Lett
[Image: see text] The ring strain present in azetidines can lead to undesired stability issues. Herein, we described a series of N-substituted azetidines which undergo an acid-mediated intramolecular ring-opening decomposition via nucleophilic attack
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61495fbd8a53cc5202ef7fb9ae427eaa
https://europepmc.org/articles/PMC8521649/
https://europepmc.org/articles/PMC8521649/
Autor:
Ekaterina Tankisheva, Ping He, Michael Aaron Brodney, Robert Alexander, Richard Margolin, Claire Leurent, Jessica Mancuso, Ruolun Qiu, Danny Chen, Jae Eun Ahn
Publikováno v:
Journal of Alzheimer's Disease
PF-06751979 is a selective inhibitor of the beta-site amyloid precursor protein cleaving enzyme-1, which is a key aspartyl protease in the generation of amyloid-β (Aβ) peptides, thought to be critical for the cerebral degeneration observed in Alzhe
Autor:
Laigao Chen, Anabella Villalobos, Ryosuke Arakawa, Shawn D. Doran, Christer Halldin, Brian T. O’Neill, Akihiro Takano, Michael Aaron Brodney, Nahid Amini, Charles E. Nolan, Timothy J. McCarthy, Jason K. Dutra, Sangram Nag, Cheng Chang, Lei Zhang
Publikováno v:
Journal of Nuclear Medicine. 60:992-997
Beta-secretase 1 (BACE1) is a key enzyme in the generation of beta-amyloid, which is accumulated in the brain of Alzheimer’s disease (AD) patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain, and showed high
Autor:
Kelly R. Bales, Anabella Villalobos, David Riddell, Shawn D. Doran, Christopher Ryan Butler, Bruce N. Rogers, Lorraine F. Lanyon, Karamjeet Pandher, Claude Ambroise, Ashley Robshaw, Gabriela Barreiro, Christopher Houle, Kevin Ogilvie, Brian T. O’Neill, Erik Alphie Lachapelle, Germaine Boucher, Xinjun Hou, Katherine Hales, David Karanian, Michael Aaron Brodney, Leanne M. Buzon, Kimberly Lapham, Lei Zhang, Luis Martinez-Alsina, Charles E. Nolan, Claire M. Steppan, Cathleen Gonzales, John C. Murray, Cheng Chang, Jason K. Dutra, Elizabeth Mary Beck
Publikováno v:
Journal of Medicinal Chemistry. 61:4476-4504
A major challenge in the development of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease is the alignment of potency, drug-like properties, and selectivity over related aspartyl proteases
Autor:
Anthony R. Harris, Susan M. Lotarski, Michael Aaron Brodney, Michael Popiolek, Catherine A. Thorn, Stephen Jenkinson, Che Wah Lee, Jennifer E. Davoren, Stefanus J. Steyn, Lei Zhang, Terrence Peter Kenakin, Betty Pettersen, Sarah Grimwood, Damien Webb, Michelle R. Garnsey, Simeon Ramsey, John T. Lazzaro, Steven Victor O'neil, Lisa Nottebaum, Jean-Philippe Fortin, Jeremy R. Edgerton
Publikováno v:
Journal of Medicinal Chemistry. 60:6649-6663
Recent data demonstrated that activation of the muscarinic M1 receptor by a subtype-selective positive allosteric modulator (PAM) contributes to the gastrointestinal (GI) and cardiovascular (CV) cholinergic adverse events (AEs) previously attributed
Autor:
Felix Vajdos, Eric Benvenuti, Leanne M. Buzon, Brian T. O’Neill, Gabriela Barreiro, David Riddell, Kevin Atchison, Charles E. Nolan, Ashley Robshaw, Eric F. Johnson, Kevin D. Parris, Shawn D. Doran, Michael Aaron Brodney, Xinjun Hou, Luis Martinez-Alsina, Kimberly Lapham, Mei-Hui Hsu, Elizabeth Mary Beck, Christopher Ryan Butler, Kevin Ogilvie, Cathleen Gonzales, Lorraine F. Lanyon, Christopher John Helal
Publikováno v:
Journal of Medicinal Chemistry
A growing subset of β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) utilizes an anilide chemotype that engages a key residue (Gly230) in the BACE1 binding site. Although the anilide moiety affords excellent potency, it s
Publikováno v:
Organic letters. 21(7)
Palladium catalyzed hydrodefluorination was developed for fine-tuning the properties of fluoro-(hetero)aromatic compounds. The robust reaction can be set up in air, requires only commercially available components, and tolerates a variety of heterocyc
Autor:
Karen J. Coffman, Michael Aaron Brodney, John C. Murray, Daniel W. Widlicka, Chunguang Xiao, Brian Samas, Rainville Joseph Philip
Publikováno v:
Organic Process Research & Development. 20:233-241
A potent 5-HT4 partial agonist, 1 (PF-04995274), targeted for the treatment of Alzheimer’s disease and cognitive impairment, has been prepared on a multi-kilogram scale. The initial synthetic route, that proceeded through a 4-substituted 3-hydroxyb
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(11)
A facile method for late stage diversification of lead molecules for the M1 PAM program using biosynthesis is described. Liver microsomes from several species are screened to identify a high turnover system. Subsequent incubations using less than 1 m
Autor:
Timothy L. Foley, Justin I. Montgomery, Daniel P. Uccello, Anthony R. Harris, Steven Victor O'neil, Bruce N. Rogers, Douglas S. Johnson, Justin R. Piro, Tarek A. Samad, Christopher Ryan Butler, Stephen Noell, Rafael G. Silva, Deane M. Nason, Christopher John Helal, Adam M. Gilbert, Julie Cianfrogna, Laura A. McAllister, Scot Richard Mente, Christopher L. Shaffer, Kari R. Fonseca, Damien Webb, Jayvardhan Pandit, Michael Aaron Brodney
Publikováno v:
Journal of medicinal chemistry. 61(7)
Monoacylglycerol lipase (MAGL) inhibition provides a potential treatment approach to neuroinflammation through modulation of both the endocannabinoid pathway and arachidonoyl signaling in the central nervous system (CNS). Herein we report the discove