Search Results - "Coleman, Paul J"

The importance of synthetic chemistry in the pharmaceutical industry by 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

“…Innovations in synthetic chemistry have enabled the discovery of many breakthrough therapies that have improved human health over the past century. In the face…”
Get full text

Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia by Roecker, Anthony J, Cox, Christopher D, Coleman, Paul J

“…Since its discovery in 1998, the orexin system, composed of two G-protein coupled receptors, orexins 1 and 2, and two neuropeptide agonists, orexins A and B,…”
Get full text

The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia by Coleman, Paul J, Gotter, Anthony L, Herring, W. Joseph, Winrow, Christopher J, Renger, John J

“…Historically, pharmacological therapies have used mechanisms such as γ-aminobutyric acid A (GABA A ) receptor potentiation to drive sleep through broad…”
Get full text

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) by 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

“…Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases…”
Get full text

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors by 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

“…Human orexin receptors (hOX 1 R and hOX 2 R) are GPCRs involved in sleep regulation. Structures of hOX 1 R bound to a selective antagonist or to a dual…”
Get full text

International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology by Gotter, Anthony L, Webber, Andrea L, Coleman, Paul J, Renger, John J, Winrow, Christopher J

“…Orexin signaling is essential for normal regulation of arousal and behavioral state control and represents an attractive target for therapeutics combating…”
Get full text

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants by 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

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
Get full text

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 by 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

“…Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified…”
Get full text

Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man by 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.

“…Orexin neuropeptides regulate sleep/wake through orexin receptors (OX 1 R, OX 2 R); OX 2 R is the predominant mediator of arousal promotion. The potential for…”
Get full text

Orexin receptors as therapeutic drug targets by Gotter, Anthony L, Roecker, Anthony J, Hargreaves, Richard, Coleman, Paul J, Winrow, Christopher J, Renger, John J

“…Orexin (hypocretin) receptor antagonists stand as a model for the development of targeted CNS small-molecule therapeutics. The identification of mutations in…”
Get more information

Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys by 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

“…In addition to enhancing sleep onset and maintenance, a desirable insomnia therapeutic agent would preserve healthy sleep's ability to wake and respond to…”
Get full text

Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia by 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.

“…Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX 1R) and Orexin 2 Receptor (OX…”
Get full text

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor by 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

“…A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint was designed using a molecular modeling-derived strategy. Building…”
Get full text

Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist by 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.

“…Orexins/hypocretins are key neuropeptides responsible for regulating central arousal and reward circuits. Two receptors respond to orexin signaling, orexin 1…”
Get full text

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia by Coleman, Paul J, Cox, Christopher D, Roecker, Anthony J

“…Orexins are excitatory neuropeptides that have a critical role in maintaining wakefulness. Orexin receptor antagonists promote sleep in animals and humans…”
Get more information

The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold by 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

“…Drugs targeting insomnia ideally promote sleep throughout the night, maintain normal sleep architecture, and are devoid of residual effects associated with…”
Get full text

Orexin receptor antagonists: a review of promising compounds patented since 2006 by Coleman, Paul J, Renger, John J

“…The orexin neuropeptide system plays a central role in maintaining arousal and wakefulness. It has been demonstrated that small molecule antagonists to the…”
Get more information

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 by 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

“…Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently…”
Get full text

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology by 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.

“…[Display omitted] While a correlation between blockade of the orexin 2 receptor (OX2R) with either a dual orexin receptor antagonist (DORA) or a selective…”
Get full text

The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine by 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.

“…Chronic insomnia is defined as a persistent difficulty with sleep initiation maintenance or non‐restorative sleep. The therapeutic standard of care for this…”
Get full text