Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Alan Daniel Brown"'
Autor:
Peter J. Bungay, Martin Corless, Sarah Elizabeth Skerratt, Joseph S. Warmus, Sharan K. Bagal, C. Elizabeth Payne, Miller Duncan Charles, Kemp Mark Ian, David R. Fenwick, Paul Blackwell, Yoshihisa Murata, Bruce Brown, Laia Malet Sanz, David Fengas, James Michael Crawforth, Victoria Gray, Wolfgang Klute, Alan Daniel Brown, David C. Blakemore, Edward B. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:230-239
The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1
Autor:
Jianmin Sun, Thomas Ryckmans, David Fengas, Colin R. Rose, M. Scott Johnson, Matthew Corbett, David James Rawson, Nigel Alan Swain, Joseph S. Warmus, Lyn H. Jones, Brian E. Marron, Aristos J. Alexandrou, David Printzenhoff, C. Elizabeth Payne, Bruce M. Bechle, Rubben Torella, Neil A. Castle, Jonathan W. Theile, Elaine Tseng, David C. Blakemore, Andrew Pike, R. Ian Storer, Neil J. Flanagan, Alan Daniel Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4805-4811
The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficac
Autor:
Alan Daniel Brown, Joseph S. Warmus, Matthew Corbett, Yoshihisa Murata, C. Elizabeth Payne, Kiyoyuki Omoto, Tanya L. Hay, Miller Duncan Charles, Sharan K. Bagal, Peter J. Bungay, David C. Blakemore, Edward B. Stevens, Kemp Mark Ian
Publikováno v:
MedChemComm. 7:1925-1931
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Nav1.8 inhibiting phenyl imidazole series that delivers chemical equi
Autor:
Bruce M. Bechle, Stephen Martin Denton, Sebastien Galan, David James Rawson, Marcel J. de Groot, Brian E. Marron, Matthew S Johnson, Jo Hannam, Shoko Nakagawa, Dave Batchelor, Nigel Alan Swain, Steven M Reister, David Ellis, Mark L. Chapman, David Printzenhoff, Sarah J Ransley, Beaudoin Serge, David S. Millan, Christopher W. West, Kenneth John Butcher, R. Ian Storer, Stephen M Gaulier, Stupple Paul Anthony, Andrew Pike, Alan Daniel Brown, Christopher John Markworth, Bruce Brown, Zhixin Lin, Sasaki Kosuke, Paul A. Bradley, Ian Gurrell, Richard P. Butt, Mel Glossop, Ben S. Greener
Publikováno v:
Journal of medicinal chemistry. 60(16)
A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cyto
Autor:
David Ellis, Adam Stennett, Malcolm MacKenny, Gordon McMurray, Tony Kirkup, Favor David, Alan Daniel Brown, Wolfgang Klute
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6118-6122
A new series of 2-(benzyloxy)benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerfu
Autor:
Paul Brennan, Dominique Westbrook, Colleen P. Gibbons, Robin Ward, Carly L. Nichols, Michael R. Sutton, Mark Holbrook, Julian Blagg, Nicholas J. Edmunds, Alison Bridgeland, Tiffini Brabham, Kelly Conlon, Andrews Mark David, Peter J. Bungay, Gavin A. Whitlock, Alan S. Jessiman, Karin McIntosh, James Root, Martin P. Green, Gordon McMurray, R. Ian Storer, Paul V. Fish, Alan Daniel Brown, Giles Hanton, Kerry af Forselles
New pyrimido[4,5-d]azepines 7 are disclosed as potent 5-HT2C receptor agonists. A preferred example, 7b had minimal activation at either the 5-HT2A or 5-HT2B receptors combined with robust efficacy in a preclinical canine model of stress urinary inco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05dc5f0ff0edfc935edd8d293ee1e0da
https://doi.org/10.1016/j.bmcl.2010.11.120
https://doi.org/10.1016/j.bmcl.2010.11.120
Autor:
Thomas Ryckmans, James Edward John Mills, Mark E. Bunnage, Miller Duncan Charles, Alan Daniel Brown, C M Barker, Sarah Elizabeth Skerratt
Publikováno v:
Med. Chem. Commun.. 3:174-178
Given the large amounts of screening data now available, empirical methods derived from matched-molecular pairs are being used as a means for suggesting bioisosteric replacements to the medicinal chemist. The pairwise analysis of compounds has been e
Autor:
J. Mark F. Gardner, Charles E. Mowbray, Stéphanie Braillard, Paul Alan Glossop, Karl Richard Gibson, Pim-Bart Feijens, Wen Hua, Garreth L. Morgans, Alan Daniel Brown, William Speed, Yafeng Cao, James Edward John Mills, An Matheeussen, Louis Maes, Gavin A. Whitlock
Publikováno v:
Journal of medicinal chemistry
Visceral leishmaniasis is a severe parasitic disease that is one of the most neglected tropical diseases. Treatment options are limited and there is an urgent need for new therapeutic agents. Following an HTS campaign and hit optimization, a novel se
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6108-6111
Optimisation of the potency of a bicyclic CRF antagonist whilst retaining metabolic stability is described. A core change and incorporation of metabolically stable lipophilic groups resulted in a further potency gain without increasing metabolic liab
Autor:
Malcolm MacKenny, Andrews Mark David, Jean-Yves Chiva, Mark Ian Lansdell, Alan Daniel Brown, David W. Gordon, David Sebastien Fradet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5893-5897
A second wave of potential SSRIs with high ease of synthetic accessibility were designed based on the reported selective serotonin re-uptake inhibitor litoxetine and our own previous work in this area. Preparation and subsequent optimisation yielded