950509-80-5Relevant academic research and scientific papers
Benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain
Hoyt, Scott B.,London, Clare,Ok, Hyun,Gonzalez, Edward,Duffy, Joseph L.,Abbadie, Catherine,Dean, Brian,Felix, John P.,Garcia, Maria L.,Jochnowitz, Nina,Karanam, Bindhu V.,Li, Xiaohua,Lyons, Kathryn A.,McGowan, Erin,MacIntyre, D. Euan,Martin, William J.,Priest, Birgit T.,Smith, McHardy M.,Tschirret-Guth, Richard,Warren, Vivien A.,Williams, Brande S.,Kaczorowski, Gregory J.,Parsons, William H.
, p. 6172 - 6177 (2007)
A series of benzazepinones were synthesized and evaluated as hNav1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain
Hoyt, Scott B.,London, Clare,Abbadie, Catherine,Felix, John P.,Garcia, Maria L.,Jochnowitz, Nina,Karanam, Bindhu V.,Li, Xiaohua,Lyons, Kathryn A.,McGowan, Erin,Priest, Birgit T.,Smith, McHardy M.,Warren, Vivien A.,Thomas-Fowlkes, Brande S.,Kaczorowski, Gregory J.,Duffy, Joseph L.
, p. 3640 - 3645 (2013/07/11)
A series of benzazepinones were synthesized and evaluated for block of Nav1.7 sodium channels. Compound 30 from this series displayed potent channel block, good selectivity versus other targets, and dose-dependent oral efficacy in a rat model of neuropathic pain.
BENZAZEPINONES AS SODIUM CHANNEL BLOCKERS
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, (2008/06/13)
Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically act
Discovery of a novel class of benzazepinone Nav1.7 blockers: Potential treatments for neuropathic pain
Hoyt, Scott B.,London, Clare,Gorin, David,Wyvratt, Matthew J.,Fisher, Michael H.,Abbadie, Catherine,Felix, John P.,Garcia, Maria L.,Li, Xiaohua,Lyons, Kathryn A.,McGowan, Erin,MacIntyre, D. Euan,Martin, William J.,Priest, Birgit T.,Ritter, Amy,Smith, McHardy M.,Warren, Vivien A.,Williams, Brande S.,Kaczorowski, Gregory J.,Parsons, William H.
, p. 4630 - 4634 (2008/02/10)
A series of benzodiazepines and benzazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of the benzazepinone series, compound 47, displayed potent, state-dependent block of hNav1.7, and was orally efficacious in a rat model of neuropathic pain.
