Search Results - "GAINES, Simon"

N of 1 randomised controlled trials of oral ketamine in patients with chronic pain by Haines, D R, Gaines, S P

“…Anecdotal reports suggest that the general anaesthetic drug ketamine, taken orally in low doses, can give rise to some extra analgesia in patients with…”
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A reversed sulfonamide series of selective RORc inverse agonists by van Niel, Monique B., Fauber, Benjamin P., Cartwright, Matthew, Gaines, Simon, Killen, Jonathan C., René, Olivier, Ward, Stuart I., de Leon Boenig, Gladys, Deng, Yuzhong, Eidenschenk, Céline, Everett, Christine, Gancia, Emanuela, Ganguli, Arunima, Gobbi, Alberto, Hawkins, Julie, Johnson, Adam R., Kiefer, James R., La, Hank, Lockey, Peter, Norman, Maxine, Ouyang, Wenjun, Qin, Ann, Wakes, Nicole, Waszkowycz, Bohdan, Wong, Harvey

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Palladium-Catalyzed Ring Expansion of Spirocyclopropanes to Form Caprolactams and Azepanes by René, Olivier, Stepek, Iain A, Gobbi, Alberto, Fauber, Benjamin P, Gaines, Simon

“…A palladium(0)-catalyzed rearrangement of piperidones and piperidines bearing a spirocyclopropane ring was developed. The ring expansion reaction led to a…”
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Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2 by Zak, Mark, Hurley, Christopher A, Ward, Stuart I, Bergeron, Philippe, Barrett, Kathy, Balazs, Mercedesz, Blair, Wade S, Bull, Richard, Chakravarty, Paroma, Chang, Christine, Crackett, Peter, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ellwood, Charles, Gaines, Simon, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Gribling, Peter, Hamman, Chris, Harstad, Eric, Hewitt, Peter, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Labadie, Sharada, Lee, Wyne P, Liao, Jiangpeng, Liimatta, Marya, Mendonca, Rohan, Narukulla, Raman, Pulk, Rebecca, Reeve, Austin, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, van Abbema, Anne, Aliagas, Ignacio, Avitabile-Woo, Barbara, Xiao, Yisong, Yang, Jing, Kulagowski, Janusz J

“…Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the…”
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A reversed sulfonamide series of selective RORc inverse agonists by van Niel, Monique B, Fauber, Benjamin P, Cartwright, Matthew, Gaines, Simon, Killen, Jonathan C, René, Olivier, Ward, Stuart I, de Leon Boenig, Gladys, Deng, Yuzhong, Eidenschenk, Céline, Everett, Christine, Gancia, Emanuela, Ganguli, Arunima, Gobbi, Alberto, Hawkins, Julie, Johnson, Adam R, Kiefer, James R, La, Hank, Lockey, Peter, Norman, Maxine, Ouyang, Wenjun, Qin, Ann, Wakes, Nicole, Waszkowycz, Bohdan, Wong, Harvey

“…The identification of a new series of RORc inverse agonists is described. Comprehensive structure-activity relationship studies of this reversed sulfonamide…”
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From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome by Henley, Zoë A, Bax, Benjamin D, Inglesby, Laura M, Champigny, Aurélie, Gaines, Simon, Faulder, Paul, Le, Joelle, Thomas, Daniel A, Washio, Yoshiaki, Baldwin, Ian R

“…Selective inhibitors of phosphoinositide 3-kinase delta are of interest for the treatment of inflammatory diseases. Initial optimization of a 3-substituted…”
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Identification of a sulfonamide series of CCR2 antagonists by Peace, Simon, Philp, Joanne, Brooks, Carl, Piercy, Val, Moores, Kitty, Smethurst, Chris, Watson, Steve, Gaines, Simon, Zippoli, Mara, Mookherjee, Claudette, Ife, Robert

“…A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular…”
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Irreversible 4‑Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease by Prime, Michael E, Brookfield, Frederick A, Courtney, Stephen M, Gaines, Simon, Marston, Richard W, Ichihara, Osamu, Li, Marie, Vaidya, Darshan, Williams, Helen, Pedret-Dunn, Anna, Reed, Laura, Schaertl, Sabine, Toledo-Sherman, Leticia, Beconi, Maria, Macdonald, Douglas, Muñoz-Sanjuan, Ignacio, Dominguez, Celia, Wityak, John

“…A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure–activity…”
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Dopamine D 3 receptor antagonists: The quest for a potentially selective PET ligand. Part one: Lead identification by Holmes, Ian P., Micheli, Fabrizio, Gaines, Simon, Lorthioir, Olivier, Watson, Steve P., Fabio, Romano Di, Gentile, Gabriella, Heidbreder, Christian, Savoia, Chiara, Worby, Angela

“…The synthesis of a new class of potent and selective D 3 antagonists is reported. The synthesis and SAR of a new series of potent and selective dopamine D 3…”
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The characterization of a novel V1b antagonist lead series by Smethurst, Chris A., Borthwick, Jennifer A., Gaines, Simon, Watson, Steve, Green, Andrew, Schulz, Mark J., Burton, George, Buson, Alberto A., Arban, Roberto

“…The SAR around a V1b antagonist HTS hit 3 was explored to produce a series of thiazole sulfonamides as a lead series with selectivity over the related V1 and…”
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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part one: Lead identification by HOLMES, Ian P, MICHELI, Fabrizio, GAINES, Simon, LORTHIOIR, Olivier, WATSON, Steve P, DI FABIO, Romano, GENTILE, Gabriella, HEIDBREDER, Christian, SAVOIA, Chiara, WORBY, Angela

“…The synthesis and SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported…”
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The identification of β-hydroxy carboxylic acids as selective MMP-12 inhibitors by Holmes, Ian P., Gaines, Simon, Watson, Steve P., Lorthioir, Olivier, Walker, Adam, Baddeley, Suzanne J., Herbert, Shane, Egan, Danielle, Convery, Máire A., Singh, Onkar M.P., Gross, Jeffrey W., Strelow, John M., Smith, Robert H., Amour, Augustin J., Brown, David, Martin, Stephen L.

“…A new class of selective MMP-12 inhibitors have been identified via high throughput screening. Crystallization with MMP-12 confirmed the mode of binding and…”
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Large Molecular Quadratic Hyperpolarizabilities in Donor/Acceptor-Substituted trans-Tetraammineruthenium(II) Complexes by Coe, Benjamin J, Chamberlain, Michelle C, Essex-Lopresti, Jonathan P, Gaines, Simon, Jeffery, John C, Houbrechts, Stephan, Persoons, André

“…A series of new Ru(II) complex salts trans-[Ru(NH3)4(L1)(L2)](PF6) n [n = 2, L1 = 4-acetylpyridine (4-acpy) and L2 = 4-(dimethylamino)pyridine (dmap) (1),…”
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