نتائج البحث - "Michael Aaron Brodney"

1

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

المؤلفون: Ekaterina Tankisheva, Ping He, Michael Aaron Brodney, Robert Alexander, Richard Margolin, Claire Leurent, Jessica Mancuso, Ruolun Qiu, Danny Chen, Jae Eun Ahn

المصدر: Journal of Alzheimer's Disease

مصطلحات موضوعية: Male, 0301 basic medicine, Thiazines, Administration, Oral, Pharmacology, amyloid-β peptides, 0302 clinical medicine, Aspartic Acid Endopeptidases, Aged, 80 and over, Cross-Over Studies, General Neuroscience, Cerebral degeneration, General Medicine, Middle Aged, Healthy Volunteers, Psychiatry and Mental health, Clinical Psychology, Tolerability, Female, Alzheimer’s disease, pharmacokinetics, Research Article, medicine.drug, Adult, safety, Adolescent, Young Adult, 03 medical and health sciences, Phase I, Double-Blind Method, Pharmacokinetics, pharmacodynamics, medicine, Humans, Protease Inhibitors, Dosing, tolerability, Adverse effect, Aged, Pyrans, Amyloid beta-Peptides, business.industry, Drug interaction, Thiazoles, BACE1 protein-human, 030104 developmental biology, Pharmacodynamics, Midazolam, Amyloid Precursor Protein Secretases, Geriatrics and Gerontology, business, 030217 neurology & neurosurgery

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec86be9ff67e9a596041cc3d5a1abc14
https://doi.org/10.3233/jad-190228

2

Intramolecular Ring-Opening Decomposition of Aryl Azetidines

المؤلفون: 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

المصدر: ACS Med Chem Lett

مصطلحات موضوعية: chemistry.chemical_compound, chemistry, Nucleophile, Amide, Intramolecular force, Aryl, Organic Chemistry, Drug Discovery, Ring (chemistry), Biochemistry, Decomposition, Combinatorial chemistry, Ring strain

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61495fbd8a53cc5202ef7fb9ae427eaa
https://europepmc.org/articles/PMC8521649/

3

Quantitative Analysis of 18F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain

المؤلفون: 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

المصدر: Journal of Nuclear Medicine. 60:992-997

مصطلحات موضوعية: 0303 health sciences, Chemistry, Pharmacology, medicine.disease, Effective dose (pharmacology), 03 medical and health sciences, 0302 clinical medicine, In vivo, Oral administration, Radioligand, medicine, Distribution (pharmacology), Radiology, Nuclear Medicine and imaging, Alzheimer's disease, Quantitative analysis (chemistry), 030217 neurology & neurosurgery, 030304 developmental biology, Distribution Volume

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::dc017d72ab0f8c8c2e3e286dc6ce3d29
https://doi.org/10.2967/jnumed.118.217372

4

Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation

المصدر: Journal of Medicinal Chemistry. 61:4476-4504

مصطلحات موضوعية: Male, Models, Molecular, 0301 basic medicine, Protein Conformation, Thiazines, Cathepsin D, Skin Pigmentation, Amyloid beta-Protein Precursor, Mice, 03 medical and health sciences, Dogs, 0302 clinical medicine, Protein structure, In vivo, Drug Discovery, Amyloid precursor protein, Animals, Aspartic Acid Endopeptidases, Humans, Protease Inhibitors, Cells, Cultured, Pyrans, Melanosome, Hypopigmentation, chemistry.chemical_classification, Molecular Structure, biology, Brain, Phenotype, Mice, Inbred C57BL, Thiazoles, 030104 developmental biology, Enzyme, chemistry, Biochemistry, Drug Design, biology.protein, Melanocytes, Molecular Medicine, Amyloid Precursor Protein Secretases, Amyloid precursor protein secretase, 030217 neurology & neurosurgery

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f16220e824d55c04d1dd3342582ab393
https://doi.org/10.1021/acs.jmedchem.8b00246

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5

Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity

المصدر: Journal of Medicinal Chemistry. 60:6649-6663

مصطلحات موضوعية: 0301 basic medicine, Agonist, Allosteric modulator, medicine.drug_class, Chemistry, Allosteric regulation, Muscarinic acetylcholine receptor M1, Pharmacology, 03 medical and health sciences, 030104 developmental biology, Drug Discovery, Convulsion, medicine, Molecular Medicine, Cholinergic, Structure–activity relationship, medicine.symptom, Receptor

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::e16d6e6b4f8608876f69c7501545a8c8
https://doi.org/10.1021/acs.jmedchem.7b00597

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6

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality

المصدر: Journal of Medicinal Chemistry

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ded625eb28a2c9b897d6055a57557a14
https://doi.org/10.1021/acs.jmedchem.6b01451

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7

Palladium Catalyzed Hydrodefluorination of Fluoro-(hetero)arenes

المؤلفون: Simon Giroux, Michael Aaron Brodney, Joseph J. Gair, Ronald Grey

المصدر: Organic letters. 21(7)

مصطلحات موضوعية: Hydrodefluorination, chemistry, 010405 organic chemistry, Organic Chemistry, chemistry.chemical_element, Physical and Theoretical Chemistry, 010402 general chemistry, 01 natural sciences, Biochemistry, Combinatorial chemistry, 0104 chemical sciences, Catalysis, Palladium

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b767adfe8a374c757996e16a5fd02693
https://pubmed.ncbi.nlm.nih.gov/30912952

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8

Two Routes to 4-Fluorobenzisoxazol-3-one in the Synthesis of a 5-HT4 Partial Agonist

المؤلفون: Karen J. Coffman, Michael Aaron Brodney, John C. Murray, Daniel W. Widlicka, Chunguang Xiao, Brian Samas, Rainville Joseph Philip

المصدر: Organic Process Research & Development. 20:233-241

مصطلحات موضوعية: 010405 organic chemistry, Chemistry, Process development, Organic Chemistry, Physical and Theoretical Chemistry, 010402 general chemistry, Cognitive impairment, 01 natural sciences, Partial agonist, Combinatorial chemistry, 0104 chemical sciences

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::771536d070947fb6d876f8c7e768e4d4
https://doi.org/10.1021/acs.oprd.5b00389

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9

Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program

المؤلفون: Raman Sharma, Michael Aaron Brodney, Gregory S. Walker, R. Scott Obach, John T. Lazzaro

المصدر: Bioorganicmedicinal chemistry letters. 28(11)

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::550afcdd1c14b23dcb7abc8cddbdcadf
https://pubmed.ncbi.nlm.nih.gov/29716781

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10

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation

المصدر: Journal of medicinal chemistry. 61(7)

مصطلحات موضوعية: 0301 basic medicine, Models, Molecular, Arachidonic Acids, Pharmacology, 01 natural sciences, Amidohydrolases, Glycerides, 03 medical and health sciences, chemistry.chemical_compound, Structure-Activity Relationship, Dogs, Neuritis, Drug Discovery, Structure–activity relationship, Animals, Humans, Enzyme Inhibitors, Rats, Wistar, Neuroinflammation, Brain Chemistry, Trifluoromethyl, 010405 organic chemistry, Drug discovery, Anti-Inflammatory Agents, Non-Steroidal, Leaving group, Serine hydrolase, Endocannabinoid system, Macaca mulatta, Monoacylglycerol Lipases, 0104 chemical sciences, Rats, Monoacylglycerol lipase, 030104 developmental biology, chemistry, Drug Design, Molecular Medicine, Carbamates, Biomarkers, Endocannabinoids

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67ba4448563e7b467bb25a055a46ddd6
https://pubmed.ncbi.nlm.nih.gov/29498843

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