96013-95-5Relevant articles and documents
Chromium-Salen Complex/Nitroxyl Radical Cooperative Catalysis: A Combination for Aerobic Intramolecular Dearomative Coupling of Phenols
Nagasawa, Shota,Fujiki, Shogo,Sasano, Yusuke,Iwabuchi, Yoshiharu
, p. 6952 - 6968 (2021/05/29)
We describe an aerobic intramolecular dearomative coupling reaction of tethered phenols using a catalytic system consisting of a chromium-salen (Cr-salen) complex combined with a nitroxyl radical. This novel catalytic system enables formation of various spirocyclic dienone products including those unable to be accessed by previously reported methods efficiently under mild reaction conditions.
ANTIVIRAL 1,3-DI-OXO-INDENE COMPOUNDS
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Paragraph 0322, (2021/10/22)
The invention provides compounds of Formula (I): as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists
Fotsing, Joseph R.,Darmohusodo, Vincent,Patron, Andrew P.,Ching, Brett W.,Brady, Thomas,Arellano, Melissa,Chen, Qing,Davis, Timothy J.,Liu, Hanghui,Servant, Guy,Zhang, Lan,Williams, Mark,Saganich, Michael,Ditschun, Tanya,Tachdjian, Catherine,Karanewsky, Donald S.
, p. 4957 - 4977 (2020/05/25)
In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blockers that can either suppress or reduce the bitterness of these compounds have not been described. We are hereby reporting a series of novel 3-(pyrazol-4-yl) imidazolidine-2,4-diones as potent and selective TAS2R8 antagonists. In human sensory tests, S6821 and S7958, two of the most potent analogues from the series, demonstrated efficacy in blocking TAS2R8-mediated bitterness and were selected for development. Following data evaluation by expert panels of a number of national and multinational regulatory bodies, including the US, the EU, and Japan, S6821 and S7958 were approved as safe under conditions of intended use as bitter taste blockers.