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

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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Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trial by Zakrzewska, Joanna M, Prof, Palmer, Joanne, PhD, Morisset, Valerie, PhD, Giblin, Gerard MP, PhD, Obermann, Mark, MD, Ettlin, Dominik A, MD, Cruccu, Giorgio, Prof, Bendtsen, Lars, MD, Estacion, Mark, PhD, Derjean, Dominique, PhD, Waxman, Stephen G, Prof, Layton, Gary, MSc, Gunn, Kevin, MD, Tate, Simon, PhD

“…Summary Background Current standard of care for trigeminal neuralgia is treatment with the sodium channel blockers carbamazepine and oxcarbazepine, which…”
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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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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 of the Integrastatin Nucleus Using the Ramberg−Bäcklund Reaction by Foot, Jonathan S, Giblin, Gerard M. P, Taylor, Richard J. K

“…The first synthesis of the tetracyclic nucleus of the Integrastatins, natural products that have been shown to selectively inhibit HIV-1 integrase, is…”
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Unexpected Z-stereoselectivity in the Ramberg-Bäcklund reaction of diarylsulfones leading to cis-stilbenes: the effect of aryl substituents and application in the synthesis of the integrastatin nucleus by Foot, Jonathan S, Giblin, Gerard M P, Whitwood, A C, Taylor, R J K

“…With certain substituent patterns, benzyl benzyl sulfone systems have been found to give unexpectedly high Z-stereoselectivity (up to E:Z = 1:16) in the Meyers…”
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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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Bridgehead Enolates:  Substitution and Asymmetric Desymmetrization of Small Bridged Carbonyl Compounds by Lithium Amide Bases by Giblin, Gerard M. P, Kirk, Douglas T, Mitchell, Lee, Simpkins, Nigel S

“…Contrary to expectations, a number of bridged carbonyl compounds undergo facile bridgehead metalation with lithium amide bases. Diketone, lactone, lactam, and…”
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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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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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Biological and Medicinal Chemistry Sector of The Royal Society of Chemistry: Promoting Chemistry Learning, Networking and Excellence for Baby Boomers through to Gen Alpha by Bagal, Sharan K., Giblin, Gerard M. P., Hall, Adrian, Jones, Philip S.

“…The Biological and Medicinal Chemistry Sector (BMCS) is an important interest group within the UK's Royal Society of Chemistry (RSC). Operating through a…”
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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 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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2-Amino-5-aryl-pyridines as selective CB2 agonists: Synthesis and investigation of structure-activity relationships by GLEAVE, Robert J, BESWICK, Paul J, SWARBRICK, Martin E, BROWN, Andrew J, GIBLIN, Gerard M. P, HASLAM, Carl P, LIVERMORE, David, MOSES, Andrew, NICHOLSON, Neville H, PAGE, Lee W, SLINGSBY, Brian

“…2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB(2) agonists from a high-throughput screen of…”
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Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping by HALL, Adrian, BILLINTON, Andy, THEOBALD, Pamela J, BROWN, Susan H, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HURST, David N, NAYLOR, Alan, PATEL, Sadhana, SCOCCITTI, Tiziana

“…We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and…”
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Identification of novel pyrazole acid antagonists for the EP1 receptor by McKeown, Stephen C., Hall, Adrian, Giblin, Gerard M.P., Lorthioir, Olivier, Blunt, Richard, Lewell, Xiao Q., Wilson, Richard J., Brown, Susan H., Chowdhury, Anita, Coleman, Tanya, Watson, Stephen P., Chessell, Iain P., Pipe, Adrian, Clayton, Nick, Goldsmith, Paul

“…The discovery, synthesis, pharmacokinetic profile and structure–activity relationships of a novel series of EP1 receptor antagonists is described. The…”
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Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists by HALL, Adrian, ATKINSON, Stephen, HEALY, Mark P, JOHNSON, Matthew R, MICHEL, Anton D, NAYLOR, Alan, NOVELLI, Riccardo, SPALDING, David J, TANG, Sac P, BROWN, Susan H, CHESSELL, Iain P, CHOWDHURY, Anita, CLAYTON, Nicholas M, COLEMAN, Tanya, GIBLIN, Gerard M. P, GLEAVE, Robert J, HAMMOND, Beverley

“…The preliminary SAR of a series of novel 1,5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described. Replacement of the benzyl group of 1…”
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Novel methylene-linked heterocyclic EP1 receptor antagonists by HALL, Adrian, BIT, Rino A, BROWN, Susan H, CHOWDHURY, Anita, GIBLIN, Gerard M. P, HURST, David N, KILFORD, Ian R, LEWELL, Xiao, NAYLOR, Alan, SCOCCITTI, Tiziana

“…We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of…”
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