84547-59-1Relevant articles and documents
FUSED AZOLE HETEROCYCLES AS AHR ANTAGONISTS
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Paragraph 00116; 00122, (2021/12/08)
The present disclosure relates to thiazolo-pyridine, oxazolo-pyridine, pyrrolo-pyridine, pyrrolo-pyrazine and pyrrolo-pyrimidine compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing
Vinylogous Elimination/C-H Functionalization/Allylation Cascade Reaction of Allenoate Adducts: Synthesis of Ring-Fused Dihydropyridinones
Sun, Manman,Chen, Weida,Wu, Haijian,Xia, Xiangyu,Yang, Jianguo,Wang, Lei,Shen, Guodong,Wang, Zhiming
supporting information, p. 8313 - 8319 (2020/11/03)
A palladium-catalyzed cascade reaction of β′-allenoate adducts with aryl/heteroaryl carboxamides through a vinylogous elimination/C-H functionalization/intramolecular allylation reaction sequence has been developed with high Z stereoselectivity. Various ring-fused dihydropyridinones bearing an α,β-unsaturated ester substituent are obtained. It is the first example of application of the allenoate adducts to C-H functionalization annulations as practical precursors of hard-to-get functionalized electron-deficient 1,3-butadienes. Using air as the terminal oxidant also shows a great advantage in environmental friendliness.
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain
Bagal, Sharan K.,Bungay, Peter J.,Denton, Stephen M.,Gibson, Karl R.,Glossop, Melanie S.,Hay, Tanya L.,Kemp, Mark I.,Lane, Charlotte A. L.,Lewis, Mark L.,Maw, Graham N.,Million, William A.,Payne, C. Elizabeth,Poinsard, Cedric,Rawson, David J.,Stammen, Blanda L.,Stevens, Edward B.,Thompson, Lisa R.
supporting information, p. 650 - 654 (2015/06/30)
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemical matter that is efficacious in preclinical models of neuropathic and inflammatory pain. (Chemical Presented).