Search Results - "Arnold, Eric P"

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor by 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

“…Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclinical models of cognition. To more fully explore the…”
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases by Vazquez, Michael L, Kaila, Neelu, Strohbach, Joseph W, Trzupek, John D, Brown, Matthew F, Flanagan, Mark E, Mitton-Fry, Mark J, Johnson, Timothy A, TenBrink, Ruth E, Arnold, Eric P, Basak, Arindrajit, Heasley, Steven E, Kwon, Soojin, Langille, Jonathan, Parikh, Mihir D, Griffin, Sarah H, Casavant, Jeffrey M, Duclos, Brian A, Fenwick, Ashley E, Harris, Thomas M, Han, Seungil, Caspers, Nicole, Dowty, Martin E, Yang, Xin, Banker, Mary Ellen, Hegen, Martin, Symanowicz, Peter T, Li, Li, Wang, Lu, Lin, Tsung H, Jussif, Jason, Clark, James D, Telliez, Jean-Baptiste, Robinson, Ralph P, Unwalla, Ray

“…Janus kinases (JAKs) are intracellular tyrosine kinases that mediate the signaling of numerous cytokines and growth factors involved in the regulation of…”
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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases by Gerstenberger, Brian S, Ambler, Catherine, Arnold, Eric P, Banker, Mary-Ellen, Brown, Matthew F, Clark, James D, Dermenci, Alpay, Dowty, Martin E, Fensome, Andrew, Fish, Susan, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, David W, Lin, Tsung H, Owen, Dafydd R, Saiah, Eddine, Sharma, Raman, Vajdos, Felix F, Xing, Li, Yang, Xiaojing, Yang, Xin, Wright, Stephen W

“…Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type…”
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Diastereoselective Synthesis of 2,3,6-Trisubstituted Piperidines by Humphrey, John M, Arnold, Eric P, Chappie, Thomas A, Feltenberger, John B, Nagel, Arthur, Simon, Wendy, Suarez-Contreras, Melani, Tom, Norma J, O’Neill, Brian T

“…We report the diastereoselective and chromatography-free syntheses of four 2-phenyl-6-alkyl-3-aminopiperidines. Ring construction was accomplished through a…”
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Oxidative Cyclization Approach to Benzimidazole Libraries by Arnold, Eric P, Mondal, Prolay K, Schmitt, Daniel C

“…An efficient approach to the parallel synthesis of benzimidazoles from anilines is described. Library approaches to vary the N1 and C2 vectors of…”
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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 by 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

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In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine by Coe, Jotham W., Vetelino, Michael G., Bashore, Crystal G., Wirtz, Michael C., Brooks, Paige R., Arnold, Eric P., Lebel, Lorraine A., Fox, Carol B., Sands, Steven B., Davis, Thomas I., Schulz, David W., Rollema, Hans, Tingley, F. David, O’Neill, Brian T.

“…[Display omitted] The preparation and biological activity of analogs of (−)-cytisine, an α4β2 nicotinic receptor partial agonist, are discussed…”
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3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation by Coe, Jotham W., Brooks, Paige R., Wirtz, Michael C., Bashore, Crystal G., Bianco, Krista E., Vetelino, Michael G., Arnold, Eric P., Lebel, Lorraine A., Fox, Carol B., Tingley, F. David, Schulz, David W., Davis, Thomas I., Sands, Steven B., Mansbach, Robert S., Rollema, Hans, O’Neill, Brian T.

“…3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2…”
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Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates - subtype selective, high affinity alpha 7 nicotinic acetylcholine receptor agonists by O'Donnell, Christopher J, Peng, Langu, O'Neill, Brian T, Arnold, Eric P, Mather, Robert J, Sands, Steven B, Shrikhande, Alka, Lebel, Lorraine A, Spracklin, Douglas K, Nedza, Frank M

“…The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4- diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha…”
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Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates – subtype selective, high affinity α7 nicotinic acetylcholine receptor agonists by O’Donnell, Christopher J., Peng, Langu, O’Neill, Brian T., Arnold, Eric P., Mather, Robert J., Sands, Steven B., Shrikhande, Alka, Lebel, Lorraine A., Spracklin, Douglas K., Nedza, Frank M.

“…The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of α7…”
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Total Synthesis of (±)-Cytisine by O'Neill, Brian T, Yohannes, Daniel, Bundesmann, Mark W, Arnold, Eric P

“…The nicotine partial agonist cytisine was prepared in five steps featuring an “in situ” Stille or Suzuki biaryl pyridine coupling. Differentiation of the…”
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Steric redirection of alkylation in 1H-pyrazole-3-carboxylate esters by Wright, Stephen W., Arnold, Eric P., Yang, Xiaojing

“…[Display omitted] •Alkylation of 1H-pyrazole-3-carboxylate esters favors distal pyrazole ring nitrogen atom.•It is possible to bias the alkylation reaction…”
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Steric redirection of alkylation in 1 H -pyrazole-3-carboxylate esters by Wright, Stephen W., Arnold, Eric P., Yang, Xiaojing

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Varenicline:  An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation by Coe, Jotham W, Brooks, Paige R, Vetelino, Michael G, Wirtz, Michael C, Arnold, Eric P, Huang, Jianhua, Sands, Steven B, Davis, Thomas I, Lebel, Lorraine A, Fox, Carol B, Shrikhande, Alka, Heym, James H, Schaeffer, Eric, Rollema, Hans, Lu, Yi, Mansbach, Robert S, Chambers, Leslie K, Rovetti, Charles C, Schulz, David W, Tingley, F. David, O'Neill, Brian T

“…Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified…”
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Pyridine analogs of (−)-cytisine and varenicline: cholinergic receptor probes by Demers, Sebastien, Stevenson, Heather, Candler, John, Bashore, Crystal G., Arnold, Eric P., O’Neill, Brian T., Coe, Jotham W.

“…A series of bicyclic pyridine containing alkaloids related to (−)-cytisine and varenicline are described. Synthetic access via regioisomeric metalation of…”
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Low efficacy partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Does functional efficacy govern in vivo response? by Coe, Jotham W., Brooks, Paige R., Wirtz, Michael C., Vetelino, Michael G., Arnold, Eric P., Sands, Steven B., Davis, Thomas I., Lebel, Lorraine A., Fox, Carol B., Shrikhande, Alka, Mansbach, Robert S., Chambers, Leslie K., Rovetti, Charles C., Schulz, David W., Tingley, F. David, O’Neill, Brian T., Rollema, Hans

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Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists by O'Donnell, Christopher J, Peng, Langu, O'Neill, Brian T, Arnold, Eric P, Mather, Robert J, Sands, Steven B, Shrikhande, Alka, Lebel, Lorraine A, Spracklin, Douglas K, Nedza, Frank M

“…The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha7…”
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Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation by Coe, Jotham W, Brooks, Paige R, Vetelino, Michael G, Wirtz, Michael C, Arnold, Eric P, Huang, Jianhua, Sands, Steven B, Davis, Thomas I, Lebel, Lorraine A, Fox, Carol B, Shrikhande, Alka, Heym, James H, Schaeffer, Eric, Rollema, Hans, Lu, Yi, Mansbach, Robert S, Chambers, Leslie K, Rovetti, Charles C, Schulz, David W, Tingley, 3rd, F David, O'Neill, Brian T

“…Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified…”
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3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation by Coe, Jotham W, Brooks, Paige R, Wirtz, Michael C, Bashore, Crystal G, Bianco, Krista E, Vetelino, Michael G, Arnold, Eric P, Lebel, Lorraine A, Fox, Carol B, Tingley, 3rd, F David, Schulz, David W, Davis, Thomas I, Sands, Steven B, Mansbach, Robert S, Rollema, Hans, O'Neill, Brian T

“…3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha4beta2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the…”
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In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine by Coe, Jotham W, Vetelino, Michael G, Bashore, Crystal G, Wirtz, Michael C, Brooks, Paige R, Arnold, Eric P, Lebel, Lorraine A, Fox, Carol B, Sands, Steven B, Davis, Thomas I, Schulz, David W, Rollema, Hans, Tingley, 3rd, F David, O'Neill, Brian T

“…The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 nicotinic receptor partial agonist, are discussed. All-carbon-containing…”
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