- Benzenesulfonamide IDH mutant inhibitor, preparation method and application thereof
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The invention discloses a benzenesulfonamide compound represented by a general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. Compared with the prior art, the benzenesulfonamide compound disclosed by the invention can be used as an isocitrate dehydrogenase 2 (IDH2) mutant inhibitor. According to the invention, pharmacological experiment results show that the compound disclosed by the invention has an obvious inhibiting effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process of catalyzing alpha-ketoglutaricacid to generate 2-hydroxyglutaric acid by mIDH2, and can be used for preventing and/or treating various related diseases including cancers and the like caused by IDH2 mutation.
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Paragraph 0069; 0084-0086
(2020/09/23)
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- Selective C-H trifluoromethylation of benzimidazoles through photoredox catalysis
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The protocol presented here is a new strategy for visible light induced C-H trifluoromethylation at C4 of benzimidazoles using Togni's reagent in the presence of fac-Ir(ppy)3. Its advantages are its operational simplicity, mild reaction conditions, low catalyst loading and wide substrate scope in which electron-withdrawing, electron-donating groups and different protecting groups are tolerated.
- Gao, Guo-Lin,Yang, Chao,Xia, Wujiong
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supporting information
p. 1041 - 1044
(2017/02/05)
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- QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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There are disclosed a series of quinuclidines having the Formula (I). which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.
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Page/Page column 59
(2016/06/01)
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- Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives
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Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, orally available, and brain-penetrable Y5 selective antagonist (5k). Crown Copyright
- Ogino, Yoshio,Ohtake, Norikazu,Nagae, Yoshikazu,Matsuda, Kenji,Moriya, Minoru,Suga, Takuya,Ishikawa, Makoto,Kanesaka, Maki,Mitobe, Yuko,Ito, Junko,Kanno, Tetsuya,Ishihara, Akane,Iwaasa, Hisashi,Ohe, Tomoyuki,Kanatani, Akio,Fukami, Takehiro
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scheme or table
p. 5010 - 5014
(2009/05/07)
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