Publications by authors named "Christopher Helal"

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Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Martin Pettersson, Douglas S Johnson, John M Humphrey, Christopher W Am Ende, Todd W Butler, Christopher J Helal

J Med Chem· June 2024

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Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Martin K Himmelbauer, Bekim Bajrami, Rebecca Basile, Andrew Capacci, TeYu Chen, Christopher J Helal

J Med Chem· May 2024

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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Uthpala Seneviratne, Zhen Huang, Christopher W Am Ende, Todd W Butler, Leah Cleary, Christopher J Helal

Cell Chem Biol· February 2021

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Synthetic Approaches to New Drugs Approved during 2018.
Andrew C Flick, Carolyn A Leverett, Hong X Ding, Emma McInturff, Sarah J Fink, Christopher J Helal

J Med Chem· October 2020

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5-Aryltetrazoles from Direct C-H Arylation with Aryl Bromides.
Yuan Zhang, Jack Chang Hung Lee, Matthew R Reese, Brian P Boscoe, John M Humphrey, Christopher J Helal

J Org Chem· April 2020

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High-Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates.
Helen A Clement, Michele Boghi, Rory M McDonald, Louise Bernier, Jotham W Coe, Christopher J Helal

Angew Chem Int Ed Engl· December 2019

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Synthetic Approaches to the New Drugs Approved During 2017.
Andrew C Flick, Carolyn A Leverett, Hong X Ding, Emma McInturff, Sarah J Fink, Christopher J Helal

J Med Chem· August 2019

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Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis.
Christopher J Helal, Mark Bundesmann, Susan Hammond, Melissa Holmstrom, Jacquelyn Klug-McLeod

ACS Med Chem Lett· August 2019

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Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
Jennifer E Davoren, Deane Nason, Jotham Coe, Keith Dlugolenski, Christopher Helal

J Med Chem· December 2018

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Increased building block access through collaboration.
Christopher J Helal, Alessandra Bartolozzi, Steven D Goble, Neelakanda S Mani, Angel Guzman-Perez

Drug Discov Today· August 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, Christopher J Helal

J Med Chem· April 2018

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Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Christopher J Helal, Eric P Arnold, Tracey L Boyden, Cheng Chang, Thomas A Chappie

J Med Chem· April 2018

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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Christopher J Helal, Eric Arnold, Tracey Boyden, Cheng Chang, Thomas A Chappie

J Med Chem· February 2018

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Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides.
Hua Zhou, Paramita Mukherjee, Rongqiang Liu, Edelweiss Evrard, Dianpeng Wang, Christopher J Helal

Org Lett· February 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

ACS Med Chem Lett· February 2018

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A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow.
Damith Perera, Joseph W Tucker, Shalini Brahmbhatt, Christopher J Helal, Ashley Chong

Science· January 2018

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Ru/Ni Dual Catalytic Desulfinative Photoredox C-C Cross-Coupling of Alkyl Sulfinate Salts and Aryl Halides.
Thomas Knauber, Ramalakshmi Chandrasekaran, Joseph W Tucker, Jinshan Michael Chen, Matthew Reese, Christopher Helal

Org Lett· December 2017

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Parallel Synthesis of 1H-Pyrazolo[3,4-d]pyrimidines via Condensation of N-Pyrazolylamides and Nitriles.
Akshay A Shah, Lois K Chenard, Joseph W Tucker, Christopher J Helal

ACS Comb Sci· November 2017

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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.
Lei Zhang, Laigao Chen, Elizabeth M Beck, Thomas A Chappie, Richard V Coelho, Christopher J Helal

J Med Chem· October 2017

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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Christopher J Helal, Eric P Arnold, Tracey L Boyden, Cheng Chang, Thomas A Chappie

J Med Chem· July 2017

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Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.
Martin Pettersson, Douglas S Johnson, Danica A Rankic, Gregory W Kauffman, Christopher W Am Ende, Christopher J Helal

Medchemcomm· April 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, Christopher J Helal

J Med Chem· January 2017

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Preclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme.
Laigao Chen, Nabeel Nabulsi, Mika Naganawa, Kenneth Zasadny, Marc B Skaddan, Christopher J Helal

J Nucl Med· September 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, Christopher J Helal

J Med Chem· July 2016

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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, Christopher J Helal

J Med Chem· March 2015

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