7552-07-0Relevant articles and documents
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
Storer, R. Ian,Pike, Andy,Swain, Nigel A.,Alexandrou, Aristos J.,Bechle, Bruce M.,Blakemore, David C.,Brown, Alan D.,Castle, Neil A.,Corbett, Matthew S.,Flanagan, Neil J.,Fengas, David,Johnson, M. Scott,Jones, Lyn H.,Marron, Brian E.,Payne, C. Elizabeth,Printzenhoff, David,Rawson, David J.,Rose, Colin R.,Ryckmans, Thomas,Sun, Jianmin,Theile, Jonathan W.,Torella, Rubben,Tseng, Elaine,Warmus, Joseph S.
supporting information, p. 4805 - 4811 (2017/10/17)
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 efficacy model data are discussed. A proposed protein–ligand binding mode for this compound is also provided to rationalise the high levels of potency and selectivity over inhibition of related sodium channels. To further support the proposed binding mode, potent conjugates are described which illustrate the potential for development of chemical probes to enable further target evaluation.
HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS
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Page/Page column 19, (2009/05/28)
The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
2-amino-4-dimethylamino-1-thia-3-azabutadienes as precursors of thiazoles
Landreau,Deniaud,Reliquet,Meslin
, p. 2651 - 2659 (2007/10/03)
The reaction of 2-amino-4-dimethylamino-1-thia-3-azabutadienes 1 with α-bromoketones gave rise to 2-aminothiazoles 2 together with 2-(N,N-dimethylaminomethylenamino)thiazoles 3. Competitive mechanisms are described. Furthermore, reaction of diene 1a with