868665-68-3Relevant academic research and scientific papers
Discovery of a novel class of pyridine derivatives that selectively inhibits mutant isocitrate dehydrogenase 2
Wang, Fangying,Li, Zhuoling,Zhang, Tao,Yan, Guoyi,Hu, Mingxing,Zhao, Lifeng,Zhao, Yinglan,Chen, Yuanwei
, p. 1087 - 1093 (2018)
This paper presents synthesis and structure–activity relationship of pyridine derivatives as inhibitors of mutant isocitrate dehydrogenase 2 (IDH2). A series of 2,4,6-trisubstituted pyridine derivatives have been prepared and evaluated in vitro. Among these compounds, 14n exhibited excellent inhibition activity with the IC50 of 54.6?nm, which is approximately onefold improvement compared to drug candidate AG-221 (Enasidenib) that is in Phase III trial. Exquisite selectivity of 14n for IDH2 R140Q mutant isoform was demonstrated by the poor activity against the wild-type IDH1 and IDH2.
2, 4, 6-SUBSTITUTED PYRIDYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER’S DISEASE
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Page/Page column 99, (2010/02/14)
The present invention is directed to 2, 4, 6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer’s disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
