- Development and Scale-up of Continuous Electrocatalytic Hydrogenation of Functionalized Nitro Arenes, Nitriles, and Unsaturated Aldehydes
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Electrolysis flow reactors based on the filter-press architecture of redox flow batteries have proven to be effective and scalable toward the production of commercially relevant, pharmaceutical quantities of anilines (>500 kg/year) from halogen-, hydroxyl-, and carbonyl-substituted nitroarenes. Turbulent flow through the carbon felts on which the catalysts were supported facilitated scaling toward production levels because it conferred on the reactors scale-independent, plug flow-like residence time distributions and high mass transfer coefficients. Equipping the cells with microreference electrodes made it possible to transfer reaction conditions first developed in batch systems to the continuous flow reactors. The catalysts prepared by incipient wetness impregnation of metal salts into lightly oxidized carbon felt supports were readily generalizable.
- Egbert, Jonathan D.,Thomsen, Edwin C.,O'Neill-Slawecki, Stacy A.,Mans, Douglas M.,Leitch, David C.,Edwards, Lee J.,Wade, Charles E.,Weber, Robert S.
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supporting information
p. 1803 - 1812
(2019/08/15)
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- SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE
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The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell pr
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Page/Page column 146
(2019/01/21)
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- Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation
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A series of AG014699 derivatives containing a novel scaffold of 2,3-dihydro-1H-[1,2]diazepino[4,5,6-cd]indole-1,4(6H)-dione were synthesized and evaluated for their inhibitory activities toward PARP-1 enzyme and two cell lines, MCF-7 cells and the BRCA1-deficient MDA-MB-436 cells. Our results demonstrated that of all AG014699 derivatives synthesized in this work, compounds 6 and 7 showed strong PARP-1 inhibitory activity (IC50 = 3.5 nM and 2.4 nM, respectively), only four and three times less potent than AG014699. Compound 6 also had significantly cell inhibitory activity against both MCF-7 cells (CC50 = 25.8 μM) and the BRCA1-deficient MDA-MB-436 cells (CC50 = 5.4 μM), nearly as good as AG014699, indicating that it can be a promising compound for further evaluation.
- Xie, Zhouling,Zhou, Youli,Zhao, Wei,Jiao, He,Chen, Yu,Yang, Yong,Li, Zhiyu
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p. 4557 - 4561
(2015/10/12)
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- SUBSTITUTED BENZENE AND 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
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The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
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Paragraph 0655; 0660-0661
(2016/05/02)
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- 1,4-PYRIDONE BICYCLIC HETEROARYL COMPOUNDS
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The present invention relates to 1,4-pyridone bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical co
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Paragraph 0554; 0555
(2014/07/08)
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- METHOD OF TREATMENT
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The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
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- INDAZOLES
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Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
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