Inhibitors of voltage-gated sodium channel Nav1.7: patent applications since 2010.
There has been intense interest in developing inhibitors of the sodium channel Nav1.7 because genetic studies have established very strong validation for the efficacy to alleviate both inflammatory and neuropathic pain. This review summarizes patent applications targeting Nav1.7 since 2010 until May, 2014. We have classified the patents into three categories as follows: small molecules with well-defined molecular selectivity among sodium channel isoforms; biologicals with well-defined molecular selectivity; and, small molecules that inhibit Nav1.7 with unknown molecular selectivity. Most of the review is dedicated to small molecule selective compounds.
Xenon Pharmaceuticals Inc., 200-3650 Gilmore Way, Burnaby, BC, V5G 4W8, Canada.
Shaoyi
S
Sun
Charles J
CJ
Cohen
Christoph M
CM
Dehnhardt
D017277:Drug Approval / Q000706:statistics & numerical data; D004345:Drug Industry / Q000331:legislation & jurisprudence*; D006801:Humans; D015394:Molecular Structure; D062556:NAV1.7 Voltage-Gated Sodium Channel / Q000235:genetics / Q000378:metabolism*; D010330:Patents as Topic / Q000706:statistics & numerical data; D061567:Voltage-Gated Sodium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*
D062556:NAV1.7 Voltage-Gated Sodium Channel; C486866:SCN9A protein, human; D061567:Voltage-Gated Sodium Channel Blockers
Nav1.7; analgesia; molecular selectivity; pain; voltage sensor domain; voltage–gated sodium channel