2746-14-7Relevant articles and documents
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Siegel,Bergstrom
, p. 3815,3816 (1950)
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Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2
Farmer, Luc J.,Clark, Michael P.,Boyd, Michael J.,Perola, Emanuele,Jones, Steven M.,Tsai, Alice,Jacobs, Marc D.,Bandarage, Upul K.,Ledeboer, Mark W.,Wang, Tiansheng,Deng, Hongbo,Ledford, Brian,Gu, Wenxin,Duffy, John P.,Bethiel, Randy S.,Shannon, Dean,Byrn, Randal A.,Leeman, Joshua R.,Rijnbrand, Rene,Bennett, Hamilton B.,O’Brien, Colleen,Memmott, Christine,Nti-Addae, Kwame,Bennani, Youssef L.,Charifson, Paul S.
supporting information, p. 256 - 260 (2017/03/08)
In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the PB2 subunit of the influenza polymerase to optimize a series of acyclic β-amino acid inhibitors, highlighted by compound 4. Compound 4 showed good oral exposure in both rat and mouse. More importantly, it showed strong potency versus multiple influenza-A strains, including pandemic 2009 H1N1 and avian H5N1 strains and showed a strong efficacy profile in a mouse influenza model even when treatment was initiated 48 h after infection. Compound 4 offers good oral bioavailability with great potential for the treatment of both pandemic and seasonal influenza.
Substituted pyrazolylpyrazole derivative and use thereof as herbicide
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Paragraph 0076; 0077, (2016/10/07)
The invention provides a compound which can effectively control major weeds having higher leaf ages which become a practical problem. Disclosed is a specific pyrazolylpyrazole derivative which is represented by formula (I) and can solve the above-mentioned problem.
