Zobrazeno 1 - 10
of 17
pro vyhledávání: '"David James Rawson"'
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:
Mark L. Lewis, Charlotte Alice Louise Lane, Blanda Luzia Christa Stammen, David James Rawson, Peter J. Bungay, William A. Million, Stephen Martin Denton, Sharan K. Bagal, Tanya L. Hay, C. Elizabeth Payne, Lisa R. Thompson, Maw Graham Nigel, Cedric Poinsard, Karl Richard Gibson, Kemp Mark Ian, Edward B. Stevens, Melanie S. Glossop
Publikováno v:
ACS Medicinal Chemistry Letters. 6:650-654
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemi
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:
Charlotte Alice Louise Lane, David Ellis, Rachel Russel, Mathias John Paul, Lesa Watson, James R. Gosset, David James Rawson, Maw Graham Nigel, Street Stephen Derek Albert, Martin Corless, Mark E. Bunnage, Stephen Martin Denton, Kevin Beaumont, Laura Foster, Susan Cole, Stephen Ballard, Marion Floc’h, Jenny Price, William A. Million, Barber Christopher Gordon, Cedric Poinsard, David Leahy, Laura Barker, Frances Holmwood
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:498-509
This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and go
Autor:
Barber Christopher Gordon, David James Rawson, Maw Graham Nigel, Natalie M. Mount, David G. Brown, Charlotte Moira Norfor Allerton, Susan M. Cole, Charlotte Alice Louise Lane, David Ellis, Nicholas W. Summerhill, Colin Robinson, Kevin Beaumont, Street Stephen Derek Albert
Publikováno v:
Journal of Medicinal Chemistry. 49:3581-3594
Sildenafil (5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one), a potent and selective phosphodiesterase type 5 (PDE5) inhibitor, provided the first oral treatment for male erectil
Autor:
David James Rawson, D. K. Walker, Clive J. Long, Kim James, Dack Kevin Neil, Dickinson Roger Peter
Publikováno v:
Medicinal Chemistry Research. 13:149-157
The potency and pharmacokinetic properties of an indole-based series of endothelin antagonists have been optimised using in vitro, in silico and in vivo methods. Compound 8 is oxidised in vivo to the active metabolite 7 and has been highlighted as an
Publikováno v:
Tetrahedron: Asymmetry. 9:3723-3730
Enantioselective palladium catalysed allylic substitution reactions have been employed as the asymmetry-producing step in the synthesis of enantiomerically enriched γ-amino acids.
Autor:
Linda Kitching, Peter J. Cox, Kiyoyuki Omoto, David James Rawson, Julie Newman, Thomas Dupont, Aisah A. Aubdool, Emma Fairman, Yoshinobu Hashizume, Jennifer V. Bodkin, Teruhisa Kato, Naoko Ishii, Thomas Ryckmans, Jade Strover, Susan D. Brain
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(16)
TrpA1 is an ion channel involved in nociceptive and inflammatory pain. It is implicated in the detection of chemical irritants through covalent binding to a cysteine-rich intracellular region of the protein. While performing an HTS of the Pfizer chem
Autor:
Steve England, David James Rawson
Publikováno v:
Future medicinal chemistry. 2(5)
For many patients the current therapies for controlling chronic pain are inadequate. This has driven the search for analgesics with improved efficacy and side effect profiles. Some anticonvulsants have voltage-gated Na+ channels (VGSCs) as their mole
Autor:
David James Rawson, Delphine Brugier, Maw Graham Nigel, Paul Turnpenny, Jo Hough, Anthony Harrison, Julie Newman, Lisa R. Thompson, Jenny Price, Joe Otterburn, Andrew N. Warren
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(12)
A potent series of substituted (2 S ,4 S )-benzylproline α 2 δ ligands have been designed from the readily available starting material (2 S ,4 R )-hydroxy- l -proline. The ligands have improved pharmacokinetic profile over the (4 S )-phenoxyproline