757995-80-5Relevant academic research and scientific papers
A series of F-Element chelators; diaza crown ethers functionalized with catecholate binding substituents
Stein, Benjamin W.,Cary, Samantha K.,Berg, John M.,Birnbaum, Eva R.,Kozimor, Stosh A.,Mocko, Veronika,Scott, Brian L.
, p. 170 - 179 (2018)
Reported here is the preparation of azacrown ethers functionalized with catechol groups. The synthetic approach was (1st) novel in that it made use of the Mannich reaction and (2nd) valuable in that it provided an improved synthesis (in terms of practical
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.
Bi-Aromatic And Tri-Aromatic Compounds As NADPH Oxidase 2 (Nox2) Inhibitors
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Paragraph 0156; 0157-0158, (2015/02/25)
Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflamma
BI-AROMATIC AND TRI-AROMATIC COMPOUNDS AS NADPH OXIDASE 2 (Nox2) INHIBITORS
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Page/Page column 36; 38, (2013/03/28)
Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflamma
