Publications by authors named "Michael Brodney"

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Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M Muscarinic Acetylcholine Receptor.
Christopher R Butler, Michael Popiolek, Laura A McAllister, Erik A LaChapelle, Melissa Kramer, Michael A Brodney

J Med Chem· July 2024

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Intramolecular Ring-Opening Decomposition of Aryl Azetidines.
Guoyun Bai, Thomas N O'Connell, Michael A Brodney, Christopher R Butler, Lara C Czabaniuk

ACS Med Chem Lett· October 2021

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Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects.
Ruolun Qiu, Jae Eun Ahn, Robert Alexander, Michael A Brodney, Ping He

J Alzheimers Dis· November 2020

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Quantitative Analysis of F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain.
Akihiro Takano, Laigao Chen, Sangram Nag, Michael A Brodney, Ryosuke Arakawa

J Nucl Med· July 2019

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Palladium Catalyzed Hydrodefluorination of Fluoro-(hetero)arenes.
Joseph J Gair, Ronald L Grey, Simon Giroux, Michael A Brodney

Org Lett· April 2019

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Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program.
Michael A Brodney, Raman Sharma, John T Lazzaro, Gregory S Walker, R Scott Obach

Bioorg Med Chem Lett· June 2018

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Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
Brian T O'Neill, Elizabeth M Beck, Christopher R Butler, Charles E Nolan, Cathleen Gonzales, Michael A Brodney

J Med Chem· May 2018

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Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain.
Lei Zhang, Laigao Chen, Jason K Dutra, Elizabeth M Beck, Sangram Nag, Michael A Brodney

J Med Chem· April 2018

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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
Laura A McAllister, Christopher R Butler, Scot Mente, Steven V O'Neil, Kari R Fonseca, Michael A Brodney

J Med Chem· April 2018

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Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Antonia F Stepan, Tuan P Tran, Christopher J Helal, Maria S Brown, Cheng Chang, Michael A Brodney

ACS Med Chem Lett· February 2018

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Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Christopher R Butler, Elizabeth M Beck, Anthony Harris, Zhen Huang, Laura A McAllister, Michael A Brodney

J Med Chem· December 2017

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Design and Synthesis of γ- and δ-Lactam M Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M-Selective PAM with Weak Agonist Activity.
Jennifer E Davoren, Michelle Garnsey, Betty Pettersen, Michael A Brodney, Jeremy R Edgerton

J Med Chem· August 2017

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Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
Christopher R Butler, Kevin Ogilvie, Luis Martinez-Alsina, Gabriela Barreiro, Elizabeth M Beck, Michael A Brodney

J Med Chem· January 2017

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Strategies toward optimization of the metabolism of a series of serotonin-4 partial agonists: investigation of azetidines as piperidine isosteres.
Ronald Scott Obach, Erik A LaChapelle, Michael A Brodney, Michelle Vanase-Frawley, Gregory W Kauffman

Xenobiotica· December 2016

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Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors.
Andrea M Zuhl, Charles E Nolan, Michael A Brodney, Sherry Niessen, Kevin Atchison

Nat Commun· October 2016

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Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.
Jennifer E Davoren, Che-Wah Lee, Michelle Garnsey, Michael A Brodney, Jason Cordes

J Med Chem· July 2016

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Biosynthesis of Fluorinated Analogs of Drugs Using Human Cytochrome P450 Enzymes Followed by Deoxyfluorination and Quantitative Nuclear Magnetic Resonance Spectroscopy to Improve Metabolic Stability.
R Scott Obach, Gregory S Walker, Michael A Brodney

Drug Metab Dispos· May 2016

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Design and optimization of selective azaindole amide M1 positive allosteric modulators.
Jennifer E Davoren, Steven V O'Neil, Dennis P Anderson, Michael A Brodney, Lois Chenard

Bioorg Med Chem Lett· January 2016

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Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.
Michael A Brodney, Elizabeth M Beck, Christopher R Butler, Gabriela Barreiro, Eric F Johnson

J Med Chem· April 2015

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Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.
Christopher R Butler, Michael A Brodney, Elizabeth M Beck, Gabriela Barreiro, Charles E Nolan

J Med Chem· March 2015

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Design, synthesis and evaluation of [(3)H]PF-7191, a highly specific nociceptin opioid peptide (NOP) receptor radiotracer for in vivo receptor occupancy (RO) studies.
Lei Zhang, Elena Drummond, Michael A Brodney, Julie Cianfrogna, Susan E Drozda

Bioorg Med Chem Lett· November 2014

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Metabolism of a serotonin-4 receptor partial agonist 4-{4-[4-tetrahydrofuran-3-yloxy)-benzo[d]isoxazol-3-yloxymethyl]-piperidin-1-ylmethyl}-tetrahydropyran-4-ol (TBPT): identification of an unusual pharmacologically active cyclized oxazolidine metabolite in human.
Aarti Sawant-Basak, Karen J Coffman, Gregory S Walker, Tim F Ryder, Elaine Tseng, Michael A Brodney

J Pharm Sci· September 2013

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Stereoselective synthesis of spiropiperidines as BACE-1 aspartyl protease inhibitors via late stage N-arylation of a 1,8-diazaspiro[4.5]dec-3-en-2-one pharmacophore.
Che-Wah Lee, Ricardo Lira, Jason Dutra, Kevin Ogilvie, Brian T O'Neill, Michael Brodney

J Org Chem· March 2013

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Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
Michael A Brodney, David E Johnson, Aarti Sawant-Basak, Karen J Coffman, Elena M Drummond

J Med Chem· November 2012

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Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.
Michael A Brodney, Gabriela Barreiro, Kevin Ogilvie, Eva Hajos-Korcsok, John Murray

J Med Chem· November 2012

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