The use of azepane as a scaffold for drug discovery remains of interest. The azepane linker is the key to efficient activity. A number of seven-membered ring derivatives have been prepared or investigated for their potential or actual pharmacological properties. Examples include azaalkane derivatives as PKB (protein kinase B) inhibitors.
Nocion Therapeutics presents data on preclinical and clinical development of Taplucainium, a novel, charged sodium channel blocker, as a potential treatment for chronic cough at the 13th London International Cough Symposium.
Taplucainium is a proprietary molecule in the novel class of charged sodium channel blockers that allows for specific silencing of activated/inflamed nociceptors while having minimal local off-target effects or systemic exposure. Unlike other investigative cough therapies, such as P2X3-antagonists, TRPA1-antagonists and TRPM8-agonists, which target a specific large pore channel, taplucainium works downstream by selectively targeting the sodium channels in activated nociceptors which are the target of these large pore channels.
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