887583-52-0Relevant articles and documents
Compound with IDH mutant inhibitory activity, preparation method and application thereof
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Paragraph 0037-0040, (2020/09/23)
The invention belongs to the field of medicines, and particularly relates to a s-triazine compound with structural characteristics of a general formula I or a pharmaceutically acceptable salt thereof,a pharmaceutical composition and a preparation method thereof, and application of the s-triazine compound or the pharmaceutically acceptable salt and the pharmaceutical composition in preparation ofIDH2 mutant inhibitors. According to the invention, pharmacological experiment results show that the compound disclosed by the invention has an obvious inhibition effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process that alpha-ketoglutaric acid is catalyzed by mIDH2 to generate 2-hydroxyglutaric acid, and can be used for preparing drugs for preventing and/or treating various related diseases caused by IDH2 mutation, wherein the diseases comprise cancers carrying IDH2 mutation.
Copper-mediated perfluoroalkylation of heteroaryl bromides with (phen)CuRF
Mormino, Michael G.,Fier, Patrick S.,Hartwig, John F.
supporting information, p. 1744 - 1747 (2014/04/17)
The attachment of perfluoroalkyl groups onto organic compounds has been a major synthetic goal over the past several decades. Previously, our group reported phenanthroline-ligated perfluoroalkyl copper reagents, (phen)CuR F, which react with aryl iodides and aryl boronates to form the corresponding benzotrifluorides. Herein the perfluoroalkylation of a series of heteroaryl bromides with (phen)CuCF3 and (phen)CuCF 2CF3 is reported. The mild reaction conditions allow the process to tolerate many common functional groups. Perfluoroethylation with (phen)CuCF2CF3 occurs in somewhat higher yields than trifluoromethylation with (phen)CuCF3, creating a method to generate fluoroalkyl heteroarenes that are less accessible from trifluoroacetic acid derivatives.
HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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Page/Page column 159, (2008/06/13)
The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.