191725-82-3Relevant articles and documents
FUNCTIONALIZED HETROARYL ENONES EXHIBITING NRF2 ACTIVATION AND THEIR METHOD OF USE
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, (2016/01/22)
Pharmaceutical compositions are disclosed, which include functionalized hetroaryl enones and are useful for treating or preventing a disease, disorder or condition associated with an NRF2-regulated pathway and/or which involves oxidative stress.
Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy
Lounsbury, Nicole,Mateo, George,Jones, Brielle,Papaiahgari, Srinivas,Thimmulappa, Rajash K.,Teijaro, Christiana,Gordon, John,Korzekwa, Kenneth,Ye, Min,Allaway, Graham,Abou-Gharbia, Magid,Biswal, Shyam,Childers, Wayne
supporting information, p. 5352 - 5359 (2015/11/11)
Nrf2 activators represent a good drug target for designing agents to treat diseases associated with oxidative stress. Building upon previous work, we designed and prepared a series of heterocyclic chalcone-based Nrf2 activators with reduced lipophilicity
Piperidine and tetrahydropyridine derivatives
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, (2008/06/13)
A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT1Dα; receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT1Dα; receptor subtype relative to the 5-HT1Dβ; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.