Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Gerard M P, Giblin"'
Autor:
Michael Williams, William F. Kiesman, Gerard M. P. Giblin, Adrian Heseltine, David T. MacPherson, James A. Ramsden, Ravi Vadali, David R Witty
Publikováno v:
Organic Process Research & Development. 24:2802-2813
Two syntheses of vixotrigine are reported. Route 1, adapted from the medicinal chemistry route, enabled rapid delivery of drug substance for clinical development. Route 2, which was developed to ad...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b6912304c8c05f1fa22e5aed2df15343
https://doi.org/10.1021/acs.oprd.0c00382
https://doi.org/10.1021/acs.oprd.0c00382
Autor:
Davina Owen, Kevin Gunn, Himanshu Naik, Francois Rugiero, Giuseppe Alvaro, Gerard M. P. Giblin, Dominique Derjean, David R Witty, Valerie Morisset, Simon Tate, David T. MacPherson, Charles Large, Christopher A Hinckley, Joanne Palmer
Publikováno v:
ACS Med Chem Lett
[Image: see text] Drugs that block voltage-gated sodium channels (Na(V)s) have utility in treating conditions including pain, epilepsy, and cardiac arrhythmias and as anesthetics (Lancet Neurol.2010941342420298965; Expert Opin. Ther. Pat.201020755779
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bc02f6ba0cd11da6a81a972adc7f95a
https://doi.org/10.1021/acsmedchemlett.0c00263
https://doi.org/10.1021/acsmedchemlett.0c00263
Autor:
Robbie Chen, Michael Williams, Erwin Irdam, William F. Kiesman, Erin M. O’Brien, David T. MacPherson, John Guzowski, Stefan Sahli, Daw-Iong Albert Kwok, Suzanne M. Opalka, Daniel Patience, Tamera Mack, Couming Vinny, David R. Witty, Gerard M. P. Giblin, Wenli Liang, Frederick Osei-Yeboah, Donald G. Walker
Publikováno v:
ACS Symposium Series ISBN: 9780841298644
ACS Symposium Series
ACS Symposium Series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2e4cceca12b83c7db91f5153ed597b3c
https://doi.org/10.1021/bk-2020-1369.ch001
https://doi.org/10.1021/bk-2020-1369.ch001
Autor:
Joi Dunbar, Simon Tate, Beth Tidemann-Miller, Mark Versavel, Himanshu Naik, Joanne Palmer, Valerie Morisset, Yuan Zhao, Gerard M. P. Giblin
Publikováno v:
Clinical pharmacology in drug developmentReferences. 9(1)
Vixotrigine is a voltage- and use-dependent Nav1.7 channel blocker under investigation for the treatment of peripheral neuropathic pain conditions, including trigeminal neuralgia. Vixotrigine is metabolized primarily via uridine diphosphate-glucurono
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9b06790c78dfdc5b8febd48a577209c
https://pubmed.ncbi.nlm.nih.gov/31650711
https://pubmed.ncbi.nlm.nih.gov/31650711
Autor:
Mark P, Healy, Amanda C, Allan, Kristin, Bailey, Andy, Billinton, Iain P, Chessell, Nicholas M, Clayton, Gerard M P, Giblin, Melanie A, Kay, Tarik, Khaznadar, Anton D, Michel, Alan, Naylor, Helen, Price, David J, Spalding, David A, Stevens, Martin E, Swarbrick, Alexander W, Wilson
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(10)
A novel series of EP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::255dabcd721101fa188cc075e86d442a
https://pubmed.ncbi.nlm.nih.gov/29636218
https://pubmed.ncbi.nlm.nih.gov/29636218
Autor:
Joanna M Zakrzewska, Valerie Morisset, Gary Layton, Gerard M. P. Giblin, Mark Estacion, Giorgio Cruccu, Dominique Derjean, Kevin Gunn, Simon Tate, Lars Bendtsen, Joanne Palmer, Stephen G. Waxman, Dominik A Ettlin, Mark Obermann
Summary Background Current standard of care for trigeminal neuralgia is treatment with the sodium channel blockers carbamazepine and oxcarbazepine, which although effective are associated with poor tolerability and the need for titration. BIIB074, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bc52cc15917e63cd6eb6494cf9fc018
https://doi.org/10.5167/uzh-135668
https://doi.org/10.5167/uzh-135668
Blockade of sodium channels for the treatment of pain has been validated as a successful mechanism by a number of commercial drugs. Their therapeutic use is currently limited by lack of channel or mode specificity, low potency, and by polypharmacolog
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2c4d3bcab33ba492e648c0e93e7c328a
https://doi.org/10.1016/b978-0-12-409547-2.12439-4
https://doi.org/10.1016/b978-0-12-409547-2.12439-4
Autor:
Mairi, Sime, Amanda C, Allan, Paul, Chapman, Charlotte, Fieldhouse, Gerard M P, Giblin, Mark P, Healy, Millard H, Lambert, Lisa M, Leesnitzer, Ann, Lewis, Raymond V, Merrihew, Richard A, Rutter, Rosemary, Sasse, Barry G, Shearer, Timothy M, Willson, Timothy M, Wilson, Robert X, Xu, David J, Virley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5568-5572
The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. A novel benzimidazole series of centrally pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5143219bc12d3d56c29263c9ead0fc44
https://doi.org/10.1016/j.bmcl.2011.06.088
https://doi.org/10.1016/j.bmcl.2011.06.088
Publikováno v:
Organic Letters. 5:4441-4444
[reaction: see text] The first synthesis of the tetracyclic nucleus of the Integrastatins, natural products that have been shown to selectively inhibit HIV-1 integrase, is reported. Key steps of this synthesis involve a novel cis-selective Ramberg-B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72da0fa158686af2304720460be1b75d
https://doi.org/10.1021/ol035786v
https://doi.org/10.1021/ol035786v
Autor:
Barry Clive Ross, Gerard M. P. Giblin, Graham G. A. Inglis, Nigel S. Watson, Panayiotis A. Procopiou, Michael G. Lester
Publikováno v:
Tetrahedron Letters. 34:4357-4360
The squalestatin 1 , has been converted into the 6,7-unsubstituted analogue, 3 , via inversion of the alcohol at C7, selective removal of the α,β-unsaturated ester at C6 followed by a Corey-Hopkins deoxygenation of the generated 6 R ,7 S -diol.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::94e04c10c9ebd24b730921904cf39ae8
https://doi.org/10.1016/s0040-4039(00)79351-8
https://doi.org/10.1016/s0040-4039(00)79351-8