Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Nigel Alan Swain"'
Autor:
R. Ian Storer, Ron O. Dror, Robert M. Owen, Nigel Alan Swain, Brendan D. Kelly, Rubben Torella, Deniz Aydin, David C. Blakemore, Scott A. Hollingsworth, Joseph S. Warmus
Publikováno v:
Journal of chemical information and modeling. 61(7)
Biased agonists, which selectively stimulate certain signaling pathways controlled by a G protein-coupled receptor (GPCR), hold great promise as drugs that maximize efficacy while minimizing dangerous side effects. Biased agonists of the μ-opioid re
Publikováno v:
Biopharmaceutics & Drug Disposition. 39:388-393
PF-06456384 is an extremely potent and selective blocker of the Nav 1.7 sodium channel designed as a potential intravenous (i.v.) analgesic targeting high potency and rapid clearance to minimize the potential for residual effects following the end of
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:
Christopher William West, Nigel Alan Swain, Peter J. Cox, Joseph S. Warmus, Kiyoyuki Omoto, David C. Pryde, George Salvatore Amato, Steven Michael Reister, Jamie Turner, Brett M Antonio, Aaron C. Gerlach, Brian E. Marron, Karen Padilla, Katrina Yoger, John H. Mahoney
Publikováno v:
ACS Medicinal Chemistry Letters. 8:666-671
A series of TRPA1 antagonists is described which has as its core structure an indazole moiety. The physical properties and in vitro DMPK profiles are discussed. Good in vivo exposure was obtained with several analogs, allowing efficacy to be assessed
Autor:
David C. Pryde, Brian E. Marron, Peter J. Cox, C. J. Markworth, Joseph S. Warmus, Christopher William West, David Printzenhoff, S. McMurray, Stupple Paul Anthony, Zhixin Lin, Nigel Alan Swain, Mark L. Chapman, C. E. Payne, Ryoichi Suzuki, Gareth Waldron
Publikováno v:
MedChemComm. 8:1255-1267
In this article, we describe the discovery of an aryl ether series of potent and selective Nav1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Nav cha
Autor:
Joseph S. Warmus, Sarah Elizabeth Skerratt, Steven M Reister, David C. Pryde, Thomas Ryckmans, J. Turner, Karen M. Padilla, Katrina E. Yoger, A. C. Gerlach, Nigel Alan Swain, G. Amato, Peter J. Cox, C. G. West, Brian E. Marron, David C. Blakemore
Publikováno v:
MedChemComm. 7:2145-2158
A series of potent and selective carboxamide TRPA1 antagonists were identified by a high throughput screen. Structure–activity relationship studies around this series are described, resulting in a highly potent example of the series. Pharmacokineti
Publikováno v:
Channels
Voltage-gated sodium (NaV) channels are a family of transmembrane ion channel proteins. They function by forming a gated, water-filled pore to help establish and control cell membrane potential via control of the flow of ions between the intracellula
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:
Sharan K. Bagal, Nigel Alan Swain, R. Ian Storer, Mark L. Chapman, Brian E. Marron, Rebecca L. Prime
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24(16):3690-3699
Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav drug discovery is an exciting field. Pharmaceutical investment in Navs for pain therapeutics has expanded exponentially due to genetic data suc
Autor:
Nigel Alan Swain, Rainer Gewald
Publikováno v:
Phosphodiesterases and Their Inhibitors