Search Results - "Giblin, Gerard M.P."

Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain by Healy, Mark P., Allan, Amanda C., Bailey, Kristin, Billinton, Andy, Chessell, Iain P., Clayton, Nicholas M., Giblin, Gerard M.P., Kay, Melanie A., Khaznadar, Tarik, Michel, Anton D., Naylor, Alan, Price, Helen, Spalding, David J., Stevens, David A., Swarbrick, Martin E., Wilson, Alexander W.

“…[Display omitted] •A novel series of selective and potent EP4 receptor partial agonists identified.•GSK726701A has good PK in rat, dog and monkey.•Robust…”
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Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist by Sime, Mairi, Allan, Amanda C., Chapman, Paul, Fieldhouse, Charlotte, Giblin, Gerard M.P., Healy, Mark P., Lambert, Millard H., Leesnitzer, Lisa M., Lewis, Ann, Merrihew, Raymond V., Rutter, Richard A., Sasse, Rosemary, Shearer, Barry G., Wilson, Timothy M., Xu, Robert X., Virley, David J.

“…The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose…”
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Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists by HALL, Adrian, ATKINSON, Stephen, MICHEL, Anton D, NAYLOR, Alan, SWEETING, Jennifer A, BROWN, Susan H, CHESSELL, Iain P, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HEALY, Mark P, JANDU, Karamjit S, JOHNSON, Matthew R

“…Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel…”
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P2-329: Lowering of brain and plasma Abeta42 in rats using gamma-secretase modulators by Harrison, David C, Hawkins, Julie, Ahmed, Sharlin, Davis, Robert, Hussain, Ishrut, Smith, Beverley, Healy, Mark, Giblin, Gerard M.P, Richardson, Jill C, Hall, Adrian, Gonzalez, M. Isabel

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P2-332: Gamma-secretase modulation alters levels of Aβ38 peptide in vitro and in vivo by Hussain, Ishrut, Hawkins, Julie, Harrison, David C, Brackenborough, Kim, Ahmed, Sharlin, Facci, Laura, Skaper, Stephen D, Richardson, Jill C, Healy, Mark, Giblin, Gerard M.P, Gonzalez, Maria I, Hall, Adrian

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Asymmetric synthesis of epibatidine by use of a novel enantioselective sulfinate elimination reaction by Jones, Clifford D., Simpkins, Nigel S., Giblin, Gerard M.P.

“…A vicinal bis-sulfone having the 7-azabicyclo[2.2.1]heptane skeleton undergoes a novel type of asymmetric elimination on treatment with the sodium alkoxide…”
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Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia by Witty, David R, Alvaro, Giuseppe, Derjean, Dominique, Giblin, Gerard M. P, Gunn, Kevin, Large, Charles, Macpherson, David T, Morisset, Valerie, Owen, Davina, Palmer, Joanne, Rugiero, Francois, Tate, Simon, Hinckley, Christopher A, Naik, Himanshu

“…Drugs that block voltage-gated sodium channels (NaVs) have utility in treating conditions including pain, epilepsy, and cardiac arrhythmias and as anesthetics…”
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Evaluation of the Pharmacokinetic Interaction Between the Voltage‐ and Use‐Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers by Dunbar, Joi, Versavel, Mark, Zhao, Yuan, Tate, Simon, Morisset, Valerie, Giblin, Gerard M. P., Palmer, Joanne, Tidemann‐Miller, Beth, Naik, Himanshu

“…Vixotrigine is a voltage‐ and use‐dependent Nav1.7 channel blocker under investigation for the treatment of peripheral neuropathic pain conditions, including…”
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6,6′-Bis(2-hydroxyphenyl)-2,2′-bipyridine manganese(III) complexes: A novel series of superoxide dismutase and catalase mimetics by Giblin, Gerard M.P, Box, Philip C, Campbell, Ian B, Hancock, Ashley P, Roomans, Susan, Mills, Gary I, Molloy, Christopher, Tranter, George E, Walker, Ann L, Doctrow, Susan R, Huffman, Karl, Malfroy, Bernard

“…A series of novel manganese(III) complexes is described based on a 6,6′-bis(2-hydroxyphenyl)-2,2′-bipyridine template. These complexes show superoxide…”
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Piperidine-derived γ-secretase modulators by Hall, Adrian, Elliott, Richard L., Giblin, Gerard M.P., Hussain, Ishrut, Musgrave, James, Naylor, Alan, Sasse, Rosemary, Smith, Beverley

“…Compound 10h was found to be a potent modulator in vitro and was found to decrease Aβ42, increase Aβ38 and have no effect on Aβ40 levels. Furthermore, 10h…”
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Discovery of 2-[(2,4-Dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a Selective CB2 Receptor Agonist for the Treatment of Inflammatory Pain by Giblin, Gerard M. P, O'Shaughnessy, Celestine T, Naylor, Alan, Mitchell, William L, Eatherton, Andrew J, Slingsby, Brian P, Rawlings, D. Anthony, Goldsmith, Paul, Brown, Andrew J, Haslam, Carl P, Clayton, Nick M, Wilson, Alex W, Chessell, Iain P, Wittington, Andrew R, Green, Richard

“…Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified…”
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Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia by Zakrzewska, Joanna M, Palmer, Joanne, Ettlin, Dominik A, Obermann, Mark, Giblin, Gerard M P, Morisset, Valerie, Tate, Simon, Gunn, Kevin

“…Trigeminal neuralgia (TN) is a rare severe unilateral facial pain condition. Current guidelines in trigeminal neuralgia management recommend sodium channel…”
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GW627368X (( N ‐{2‐[4‐(4,9‐diethoxy‐1‐oxo‐1,3‐dihydro‐2 H ‐benzo[ f ]isoindol‐2‐yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP 4 receptor antagonist by Wilson, Richard J, Giblin, Gerard M P, Roomans, Susan, Rhodes, Sharron A, Cartwright, Kerri‐Ann, Shield, Vanessa J, Brown, Jason, Wise, Alan, Chowdhury, Jannatara, Pritchard, Sara, Coote, Jim, Noel, Lloyd S, Kenakin, Terry, Burns‐Kurtis, Cynthia L, Morrison, Valerie, Gray, David W, Giles, Heather

“…N ‐{2‐[4‐(4,9‐diethoxy‐1‐oxo‐1,3‐dihydro‐2 H ‐benzo[ f ]isoindol‐2‐yl)phenyl]acetyl}benzene sulphonamide (GW627368X) is a novel, potent and selective…”
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Discovery of 1-[4-(3-Chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a Brain Penetrant 5-Azaindole CB2 Agonist for the Treatment of Chronic Pain by Giblin, Gerard M. P, Billinton, Andrew, Briggs, Michael, Brown, Andrew J, Chessell, Iain P, Clayton, Nick M, Eatherton, Andrew J, Goldsmith, Paul, Haslam, Carl, Johnson, Matthew R, Mitchell, William L, Naylor, Alan, Perboni, Alcide, Slingsby, Brian P, Wilson, Alex W

“…We report the synthesis and SAR of a series of novel azaindole CB2 agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a…”
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Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy by HALL, Adrian, BILLINTON, Andy, NAYLOR, Alan, PASSINGHAM, Barry, WINYARD, Lisa, BROWN, Susan H, CLAYTON, Nicholas M, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HAYHOW, Thomas G, HURST, David N, KILFORD, Ian R

“…Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of…”
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Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB2 agonists for the treatment of inflammatory pain by GLEAVE, Robert J, BESWICK, Paul J, ROOMANS, Susan, SLINGSBY, Brian P, SWARBRICK, Martin E, BROWN, Andrew J, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HASLAM, Carl P, MITCHELL, William L, NICHOLSON, Neville H, PAGE, Lee W, PATEL, Sadhana

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Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists by ALLAN, Amanda C, BILLINTON, Andy, NAYLOR, Alan, RAWLINGS, D. Anthony, SIME, Mairi, SCOCCITTI, Tiziana, THEOBALD, Pamela J, BROWN, Susan H, CHOWDHURY, Anita, EATHERTON, Andrew J, FIELDHOUSE, Charlotte, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HALL, Adrian, HURST, David N

“…We describe the discovery and optimization of a novel series of benzofuran EP(1) antagonists, leading to the identification of 26d, a novel nonacidic EP(1)…”
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Corrigendum to “Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist” [Bioorg. Med. Chem. Lett. 21 (2011) 5568–5572] by Sime, Mairi, Allan, Amanda C., Chapman, Paul, Fieldhouse, Charlotte, Giblin, Gerard M.P., Healy, Mark P., Lambert, Millard H., Leesnitzer, Lisa M., Lewis, Ann, Merrihew, Raymond V., Rutter, Richard A., Sasse, Rosemary, Shearer, Barry G., Willson, Timothy M., Xu, Robert X., Virley, David J.

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Discovery of GSK345931A : An EP1 receptor antagonist with efficacy in preclinical models of inflammatory pain by HALL, Adrian, BROWN, Susan H, SCOCCITTI, Tiziana, WILSON, Alexander W, WINCHESTER, Wendy J, BUDD, Christopher, CLAYTON, Nicholas M, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HAYHOW, Thomas G, HURST, David N, NAYLOR, Alan, RAWLINGS, D. Anthony

“…Herein we describe the medicinal chemistry programme to identify a potential back-up compound to the EP1 receptor antagonist GW848687X. This work started with…”
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Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)-methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP1 receptor antagonist for the treatment of inflammatory pain by HALL, Adrian, BILLINTON, Andy, PEET, Caroline F, SCOCCITTI, Tiziana, WILSON, Alexander W, WINCHESTER, Wendy, BROWN, Susan H, CHOWDHURY, Anita, CLAYTON, Nicholas M, GIBLIN, Gerard M. P, GIBSON, Mairi, GOLDSMITH, Paul A, HURST, David N, NAYLOR, Alan

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