The importance of synthetic chemistry in the pharmaceutical industry
Campos, Kevin R, Coleman, Paul J, Alvarez, Juan C, Dreher, Spencer D, Garbaccio, Robert M, Terrett, Nicholas K, Tillyer, Richard D, Truppo, Matthew D, Parmee, Emma R
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Published in Science (American Association for the Advancement of Science) (18.01.2019)
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Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia
Roecker, Anthony J, Cox, Christopher D, Coleman, Paul J
Published in Journal of medicinal chemistry (28.01.2016)
Published in Journal of medicinal chemistry (28.01.2016)
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Discovery of 6‑(Fluoro-18 F)‑3-(1H‑pyrrolo[2,3‑c]pyridin-1-yl)isoquinolin-5-amine ([18F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs)
Walji, Abbas M, Hostetler, Eric D, Selnick, Harold, Zeng, Zhizhen, Miller, Patricia, Bennacef, Idriss, Salinas, Cristian, Connolly, Brett, Gantert, Liza, Holahan, Marie, O’Malley, Stacey, Purcell, Mona, Riffel, Kerry, Li, Jing, Balsells, Jaume, OBrien, Julie A, Melquist, Stacey, Soriano, Aileen, Zhang, Xiaoping, Ogawa, Aimie, Xu, Serena, Joshi, Elizabeth, Della Rocca, Joseph, Hess, Fred J, Schachter, Joel, Hesk, David, Schenk, David, Struyk, Arie, Babaoglu, Kerim, Lohith, Talakad G, Wang, Yaode, Yang, Kun, Fu, Jianmin, Evelhoch, Jeffrey L, Coleman, Paul J
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors
Yin, Jie, Babaoglu, Kerim, Brautigam, Chad A, Clark, Lindsay, Shao, Zhenhua, Scheuermann, Thomas H, Harrell, Charles M, Gotter, Anthony L, Roecker, Anthony J, Winrow, Christopher J, Renger, John J, Coleman, Paul J, Rosenbaum, Daniel M
Published in Nature structural & molecular biology (01.04.2016)
Published in Nature structural & molecular biology (01.04.2016)
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MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants
SUMMA, Vincenzo, LUDMERER, Steven W, GATES, Adam T, GRAHAM, Donald J, HARPER, Steven, HAZUDA, Daria J, MCHALE, Carolyn, MONTEAGUDO, Edith, PUCCI, Vincenzo, ROWLEY, Michael, RUDD, Michael T, SORIANO, Aileen, MCCAULEY, John A, STAHLHUT, Mark W, VACCA, Joseph P, OLSEN, David B, LIVERTON, Nigel J, CARROLL, Steven S, FANDOZZI, Christine, BURLEIN, Christine, CLAUDIO, Giuliano, COLEMAN, Paul J, DIMUZIO, Jillian M, FERRARA, Marco, DI FILIPPO, Marcello
Published in Antimicrobial Agents and Chemotherapy (01.08.2012)
Published in Antimicrobial Agents and Chemotherapy (01.08.2012)
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Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia
Cox, Christopher D, Breslin, Michael J, Whitman, David B, Schreier, John D, McGaughey, Georgia B, Bogusky, Michael J, Roecker, Anthony J, Mercer, Swati P, Bednar, Rodney A, Lemaire, Wei, Bruno, Joseph G, Reiss, Duane R, Harrell, C. Meacham, Murphy, Kathy L, Garson, Susan L, Doran, Scott M, Prueksaritanont, Thomayant, Anderson, Wayne B, Tang, Cuyue, Roller, Shane, Cabalu, Tamara D, Cui, Donghui, Hartman, George D, Young, Steven D, Koblan, Ken S, Winrow, Christopher J, Renger, John J, Coleman, Paul J
Published in Journal of medicinal chemistry (22.07.2010)
Published in Journal of medicinal chemistry (22.07.2010)
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Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man
Gotter, Anthony L., Forman, Mark S., Harrell, Charles M., Stevens, Joanne, Svetnik, Vladimir, Yee, Ka Lai, Li, Xiaodong, Roecker, Anthony J., Fox, Steven V., Tannenbaum, Pamela L., Garson, Susan L., Lepeleire, Inge De, Calder, Nicole, Rosen, Laura, Struyk, Arie, Coleman, Paul J., Herring, W. Joseph, Renger, John J., Winrow, Christopher J.
Published in Scientific reports (03.06.2016)
Published in Scientific reports (03.06.2016)
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Orexin receptors as therapeutic drug targets
Gotter, Anthony L., Roecker, Anthony J., Hargreaves, Richard, Coleman, Paul J., Winrow, Christopher J., Renger, John J.
Published in Orexin/Hypocretin System (2012)
Published in Orexin/Hypocretin System (2012)
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Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys
Tannenbaum, Pamela L, Tye, Spencer J, Stevens, Joanne, Gotter, Anthony L, Fox, Steven V, Savitz, Alan T, Coleman, Paul J, Uslaner, Jason M, Kuduk, Scott D, Hargreaves, Richard, Winrow, Christopher J, Renger, John J
Published in Sleep (New York, N.Y.) (01.03.2016)
Published in Sleep (New York, N.Y.) (01.03.2016)
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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia
Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Tannenbaum, Pamela L., Garson, Susan L., Doran, Scott M., Breslin, Michael J., Schreier, John D., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.
Published in Neuropharmacology (01.02.2012)
Published in Neuropharmacology (01.02.2012)
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Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor
Harper, Steven, McCauley, John A, Rudd, Michael T, Ferrara, Marco, DiFilippo, Marcello, Crescenzi, Benedetta, Koch, Uwe, Petrocchi, Alessia, Holloway, M. Katharine, Butcher, John W, Romano, Joseph J, Bush, Kimberly J, Gilbert, Kevin F, McIntyre, Charles J, Nguyen, Kevin T, Nizi, Emanuela, Carroll, Steven S, Ludmerer, Steven W, Burlein, Christine, DiMuzio, Jillian M, Graham, Donald J, McHale, Carolyn M, Stahlhut, Mark W, Olsen, David B, Monteagudo, Edith, Cianetti, Simona, Giuliano, Claudio, Pucci, Vincenzo, Trainor, Nicole, Fandozzi, Christine M, Rowley, Michael, Coleman, Paul J, Vacca, Joseph P, Summa, Vincenzo, Liverton, Nigel J
Published in ACS medicinal chemistry letters (12.04.2012)
Published in ACS medicinal chemistry letters (12.04.2012)
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Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist
Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Doran, Scott M., Tannenbaum, Pamela L., Breslin, Michael J., Garson, Susan L., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.
Published in Journal of neurogenetics (01.03.2011)
Published in Journal of neurogenetics (01.03.2011)
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Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia
Coleman, Paul J, Cox, Christopher D, Roecker, Anthony J
Published in Current topics in medicinal chemistry (01.03.2011)
Published in Current topics in medicinal chemistry (01.03.2011)
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Journal Article
The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold
Gotter, Anthony L, Winrow, Christopher J, Brunner, Joseph, Garson, Susan L, Fox, Steven V, Binns, Jacquelyn, Harrell, Charles M, Cui, Donghui, Yee, Ka Lai, Stiteler, Mark, Stevens, Joanne, Savitz, Alan, Tannenbaum, Pamela L, Tye, Spencer J, McDonald, Terrence, Yao, Leon, Kuduk, Scott D, Uslaner, Jason, Coleman, Paul J, Renger, John J
Published in BMC neuroscience (28.08.2013)
Published in BMC neuroscience (28.08.2013)
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Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer
Cox, Christopher D, Coleman, Paul J, Breslin, Michael J, Whitman, David B, Garbaccio, Robert M, Fraley, Mark E, Buser, Carolyn A, Walsh, Eileen S, Hamilton, Kelly, Schaber, Michael D, Lobell, Robert B, Tao, Weikang, Davide, Joseph P, Diehl, Ronald E, Abrams, Marc T, South, Vicki J, Huber, Hans E, Torrent, Maricel, Prueksaritanont, Thomayant, Li, Chunze, Slaughter, Donald E, Mahan, Elizabeth, Fernandez-Metzler, Carmen, Yan, Youwei, Kuo, Lawrence C, Kohl, Nancy E, Hartman, George D
Published in Journal of medicinal chemistry (24.07.2008)
Published in Journal of medicinal chemistry (24.07.2008)
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Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology
Stump, Craig A., Cooke, Andrew J., Bruno, Joseph, Cabalu, Tamara D., Gotter, Anthony L., Harell, C. Meacham, Kuduk, Scott D., McDonald, Terrence P., O’Brien, Julie, Renger, John J., Williams, Peter D., Winrow, Christopher J., Coleman, Paul J.
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
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The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine
Yao, Lihang, Ramirez, Andres D., Roecker, Anthony J., Fox, Steven V., Uslaner, Jason M., Smith, Sean M., Hodgson, Robert, Coleman, Paul J., Renger, John J., Winrow, Christopher J., Gotter, Anthony L.
Published in Journal of neurochemistry (01.07.2017)
Published in Journal of neurochemistry (01.07.2017)
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