- Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy
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Nrf2 activators represent a good drug target for designing agents to treat diseases associated with oxidative stress. Building upon previous work, we designed and prepared a series of heterocyclic chalcone-based Nrf2 activators with reduced lipophilicity
- Lounsbury, Nicole,Mateo, George,Jones, Brielle,Papaiahgari, Srinivas,Thimmulappa, Rajash K.,Teijaro, Christiana,Gordon, John,Korzekwa, Kenneth,Ye, Min,Allaway, Graham,Abou-Gharbia, Magid,Biswal, Shyam,Childers, Wayne
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supporting information
p. 5352 - 5359
(2015/11/11)
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- FUNCTIONALIZED HETROARYL ENONES EXHIBITING NRF2 ACTIVATION AND THEIR METHOD OF USE
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Pharmaceutical compositions are disclosed, which include functionalized hetroaryl enones and are useful for treating or preventing a disease, disorder or condition associated with an NRF2-regulated pathway and/or which involves oxidative stress.
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Paragraph 0218
(2016/01/22)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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Paragraph 00100
(2014/10/04)
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- 10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE
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A 10a-azalide compound having a 4-membered ring structure crosslinked at the 10a- and 12-positions, which is represented by the formula (I), and is effective on even Haemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
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Page/Page column 38
(2011/04/14)
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- Synthesis of Pyridocyclobuten-5-one and 1-Azafulvenallene by Flash Vacuum Pyrolysis of 3-Chloroformyl-2-methylpyridine
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The temperature and pressure dependence of products formed on pyrolysis of 3-chloroformyl-2-methylpyridine (6) have been studied.Pyrolysis of 6 at 575 deg C and ca. 1 x 10-4 torr gives pyridocyclobuten-5-one (5) in 20percent yield.Pyrolysis of 6 at 575 and 800 deg C and under the pressure of ca. 1 x 10-2 torr give 1-azafulvenallene (7, 46percent) and 1-cyanocyclopentadiene (8, 42percent), respectively.Irradiation of 5 (λ > 300 nm) in methanol affords 2-methoxy-3-acetylpyridine (9) quantitatively.
- Chou, Chin-Hsing,Wu, Cheng-Chang,Chen, Wey-Kao
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p. 5065 - 5068
(2007/10/02)
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- Improved Synthesis of 2,3-Disubstituted Pyridines by Metallation of 2-Chloropyridine: a Convenient Route to Fused Polyheterocycles
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Chemoselective directed metallation of 2-chloropyridine allows the synthesis of 2-substituted 3-carbonylated pyridines, advantage being taken of the metallation ortho-directing effect of the halogen, as well as its reactivity towards nucleophiles.Thus (2-chloro-, 2-methoxy-, and 2-amino-3-pyridyl)-ethanones and -arylmethanones as well as carbaldehydes have been prepared.Some of these ortho-disubstituted intermediates have been readily cyclized to fused polyheterocycles such as naphthiridines and aza-analoges of coumarins, xanthones, and acridones.
- Trecourt, Francois,Marsais, Francis,Guengoer, Timur,Queguiner, Guy
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p. 2409 - 2415
(2007/10/02)
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