未登录 Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease 临床候选PF-06648671的发现: 一种有效的 γ-分泌酶调节剂，用于治疗阿尔茨海默氏病 Pettersson, Martin; Johnson, Douglas S.; Humphrey, John M.; Am Ende, Christopher W.; Butler, Todd W.; Dorff, Peter H.; Efremov, Ivan V.; Evrard, Edelweiss; Green, Michael E.; Helal, Christopher J.; Kauffman, Gregory W.; Mullins, Patrick B.; Navaratnam, Thayalan; O'Donnell, Christopher J.; O'Sullivan, Theresa J.; Patel, Nandini C.; Stepan, Antonia F.; Stiff, Cory M.; Subramanyam, Chakrapani; Trapa, Patrick; Tran, Tuan P.; Vetelino, Beth Cooper; Yang, Eddie; Xie, Longfei; Pustilnik, Leslie R.; Steyn, Stefanus J.; Wood, Kathleen M.; Bales, Kelly R.; Hajos-Korcsok, Eva; Verhoest, Patrick R. 分享 收藏
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis Himmelbauer, Martin K.; Bajrami, Bekim; Basile, Rebecca; Capacci, Andrew; Chen, Teyu; Choi, Colin K.; Gilfillan, Rab; de Turiso, Felix Gonzalez-Lopez; Gu, Chungang; Hoemberger, Marc; Johnson, Douglas S.; Jones, J. Howard; Kadakia, Ekta; Kirkland, Melissa; Lin, Edward Y.; Liu, Ying; Ma, Bin; Magee, Tom; Mantena, Srinivasa; Marx, Isaac E.; Metrick, Claire M.; Mingueneau, Michael; Murugan, Paramasivam; Muste, Cathy A.; Nadella, Prasad; Nevalainen, Marta; Parker Harp, Chelsea R.; Pattaropong, Vatee; Pietrasiewicz, Alicia; Prince, Robin J.; Purgett, Thomas J.; Santoro, Joseph C.; Schulz, Jurgen; Sciabola, Simone; Tang, Hao; Vandeveer, H. George; Wang, Ti; Yousaf, Zain; Helal, Christopher J.; Hopkins, Brian T. 分享 收藏
Catalytic Enantioselective Synthesis of a cis-β-Boronyl Cyclobutylcarboxyester Scaffold and Its Highly Diastereoselective Nickel/Photoredox Dual-Catalyzed Csp3-Csp2 Cross-Coupling to Access Elusive trans-β-Aryl/Heteroaryl Cyclobutylcarboxyesters (vol 11, pg 404, 2021) Nguyen, Kevin; Clement, Helen A.; Bernier, Louise; Coe, Jotham W.; Farrell, William; Helal, Christopher J.; Reese, Matthew R.; Sach, Neal W.; Lee, Jack C.; Hall, Dennis G. 分享 收藏
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE Seneviratne, Uthpala; Huang, Zhen; Ende, Christopher W. am; Butler, Todd W.; Cleary, Leah; Dresselhaus, Erica; Evrard, Edelweiss; Fisher, Ethan L.; Green, Michael E.; Helal, Christopher J.; Humphrey, John M.; Lanyon, Lorraine F.; Marconi, Michael; Mukherjee, Paramita; Sciabola, Simone; Steppan, Claire M.; Sylvain, Emily K.; Tuttle, Jamison B.; Verhoest, Patrick R.; Wager, Travis T.; Xie, Longfei; Ramaswamy, Gayathri; Johnson, Douglas S.; Pettersson, Martin 分享 收藏
Catalytic Enantioselective Synthesis of a cis-β-Boronyl Cyclobutylcarboxyester Scaffold and Its Highly Diastereoselective Nickel/Photoredox Dual-Catalyzed Csp3-Csp2 Cross-Coupling to Access Elusive trans-β-Aryl/Heteroaryl Cyclobutylcarboxyesters Nguyen, Kevin; Clement, Helen A.; Bernier, Louise; Coe, Jotham W.; Farrell, William; Helal, Christopher J.; Reese, Matthew R.; Sach, Neal W.; Lee, Jack C.; Hall, Dennis G. 分享 收藏
Synthetic Approaches to New Drugs Approved during 2018 2018年批准的新药的合成方法 Flick, Andrew C.; Leverett, Carolyn A.; Ding, Hong X.; McInturff, Emma; Fink, Sarah J.; Helal, Christopher J.; DeForest, Jacob C.; Morse, Peter D.; Mahapatra, Subham; O'Donnell, Christopher J. 分享 收藏
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High-Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates Clement, Helen A.; Boghi, Michele; McDonald, Rory M.; Bernier, Louise; Coe, Jotham W.; Farrell, William; Helal, Christopher J.; Reese, Matthew R.; Sach, Neal W.; Lee, Jack C.; Hall, Dennis G. 分享 收藏
Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis Helal, Christopher J.; Bundesmann, Mark; Hammond, Susan; Holmstrom, Melissa; Klug-McLeod, Jacquelyn; Lefker, Bruce A.; McLeod, Dale; Subramanyam, Chakrapani; Zakaryants, Oleg; Sakata, Sylvie 分享 收藏
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Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization Davoren, Jennifer E.; Nason, Deane; Coe, Jotham; Dlugolenski, Keith; Helal, Christopher; Harris, Anthony R.; LaChapelle, Erik; Liang, Sidney; Liu, Yue; O'Connor, Rebecca; Orozco, Christine C.; Rai, Brajesh K.; Salafia, Michelle; Samas, Brian; Xu, Wenjian; Kozak, Rouba; Gray, David 分享 收藏
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor (vol 60, pg 5673, 2017) Helal, Christopher J.; Arnold, Eric P.; Boyden, Tracey L.; Chang, Cheng; Chappie, Thomas A.; Fennell, Kimberly F.; Forman, Michael D.; Hajos, Mihaly; Harms, John F.; Hoffman, William E.; Humphrey, John M.; Kang, Zhijun; Kleiman, Robin J.; Kormos, Bethany L.; LaChapelle, Erik A.; Lee, Che-Wah; Lu, Jiemin; Maklad, Noha; McDowell, Laura; Mente, Scot; O'Connor, Rebecca E.; Pandit, Jayvardhan; Piotrowski, Mary; Schmidt, Anne W.; Schmidt, Christopher J.; Ueno, Hirokazu; Verhoest, Patrick R.; Yang, Edward X. 分享 收藏
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation McAllister, Laura A.; Butler, Christopher R.; Mente, Scot; O'neil, Steven, V; Fonseca, Kari R.; Piro, Justin R.; Cianfrogna, Julie A.; Foley, Timothy L.; Gilbert, Adam M.; Harris, Anthony R.; Helal, Christopher J.; Johnson, Douglas S.; Montgomery, Justin, I; Nason, Deane M.; Noell, Stephen; Pandit, Jayvardhan; Rogers, Bruce N.; Samad, Tarek A.; Shaffer, Christopher L.; da Silva, Rafael G.; Uccello, Daniel P.; Webb, Damien; Brodney, Michael A. 分享 收藏
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189 晚期微粒体氧化减少药物-药物相互作用并鉴定磷酸二酯酶2A抑制剂PF-06815189 Stepan, Antonia F.; Tran, Tuan P.; Helal, Christopher J.; Brown, Maria S.; Chang, Cheng; O'Connor, Rebecca E.; De Vivo, Michael; Doran, Shawn D.; Fisher, Ethan L.; Jenkinson, Stephen; Karanian, David; Kormos, Bethany L.; Sharma, Raman; Walker, Gregory S.; Wright, Ann S.; Yang, Edward X.; Brodney, Michael A.; Wager, Travis T.; Verhoest, Patrick R.; Obach, R. Scott 分享 收藏
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate Helal, Christopher J.; Arnold, Eric; Boyden, Tracey; Chang, Cheng; Chappie, Thomas A.; Fisher, Ethan; Hajos, Mihaly; Harms, John F.; Hoffman, William E.; Humphrey, John M.; Pandit, Jayvardhan; Kang, Zhijun; Kleiman, Robin J.; Kormos, Bethany L.; Lee, Che-Wah; Lun, Jiemin; Maldad, Noha; McDowell, Laura; McGinnis, Dina; O'Connor, Rebecca E.; O'Donnell, Christopher J.; Ogden, Adam; Piotrowski, Mary; Schmidt, Christopher J.; Seymour, Patricia A.; Ueno, Hirokazu; Vansell, Nichole; Verhoest, Patrick R.; Yang, Edward X. 分享 收藏
Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides 引入用于合成硫 (VI) 氟化物的结晶，货架稳定的试剂 Zhou, Hua; Mukherjee, Paramita; Liu, Rongqiang; Evrard, Edelweiss; Wang, Dianpeng; Humphrey, John M.; Butler, Todd W.; Hoth, Lise R.; Sperry, Jeffrey B.; Sakata, Sylvie K.; Helal, Christopher J.; Ende, Christopher W. Am 分享 收藏
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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging Zhang, Lei; Chen, Laigao; Beck, Elizabeth M.; Chappie, Thomas A.; Coelho, Richard V.; Doran, Shawn D.; Fan, Kuo-Hsien; Helal, Christopher J.; Humphrey, John M.; Hughes, Zoe; Kuszpit, Kyle; Lachapelle, Erik A.; Lazzaro, John T.; Lee, Chewah; Mather, Robert J.; Patel, Nandini C.; Skaddan, Marc B.; Sciabola, Simone; Verhoest, Patrick R.; Young, Joseph M.; Zasadny, Kenneth; Villalobos, Anabella 分享 收藏
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Helal, Christopher J.; Arnold, Eric P.; Boyden, Tracey L.; Chang, Cheng; Chappie, Thomas A.; Fennell, Kimberly F.; Forman, Michael D.; Hajos, Mihaly; Harms, John F.; Hoffman, William E.; Humphrey, John M.; Kang, Zhijun; Kleiman, Robin J.; Kormos, Bethany L.; Lee, Che-Wah; Lu, Jiemin; Maklad, Noha; McDowell, Laura; Mente, Scot; O'Connor, Rebecca E.; Pandit, Jayvardhan; Piotrowski, Mary; Schmidt, Anne W.; Schmidt, Christopher J.; Ueno, Hirokazu; Verhoest, Patrick R.; Yang, Edward X. 分享 收藏
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