1080671-49-3Relevant academic research and scientific papers
Cyclic hydroxyamidines as amide isosteres: Discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo
Sun, Zhong-Yue,Asberom, Theodros,Bara, Thomas,Bennett, Chad,Burnett, Duane,Chu, Inhou,Clader, John,Cohen-Williams, Mary,Cole, David,Czarniecki, Michael,Durkin, James,Gallo, Gioconda,Greenlee, William,Josien, Hubert,Huang, Xianhai,Hyde, Lynn,Jones, Nicholas,Kazakevich, Irina,Li, Hongmei,Liu, Xiaoxiang,Lee, Julie,MacCoss, Malcolm,Mandal, Mihir B.,McCracken, Troy,Nomeir, Amin,Mazzola, Robert,Palani, Anandan,Parker, Eric M.,Pissarnitski, Dmitri A.,Qin, Jun,Song, Lixin,Terracina, Giuseppe,Vicarel, Monica,Voigt, Johannes,Xu, Ruo,Zhang, Lili,Zhang, Qi,Zhao, Zhiqiang,Zhu, Xiaohong,Zhu, Zhaoning
, p. 489 - 502 (2012/03/11)
Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic profiles. These designs were applied in the identification of γ-secretase modulators leading to highly efficacious agents for reduction of central nervous system Aβ42 in various animal models.
GAMMA SECRETASE MODULATORS
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, (2009/01/20)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing
