- SUBSTITUTED TETRAHYDROISOQUINOLINE ETHYLBENZAMIDE ANTI-CANCER AGENTS
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The compounds herein disclosed are N-substituted tetrahydroisoquinoline ethylbenzamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline ethylbenzamide compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6- to 10-fold less than the IC50 of Tamoxifen.
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Paragraph 0032; 0132
(2019/04/18)
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- Visible Light as a Sole Requirement for Intramolecular C(sp3)-H Imination
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A novel, simple, and practical visible-light-mediated intramolecular α-C(sp3)-H imination of tertiary aliphatic amines containing β-O-aryl oximes leading to N-heterocycles has been developed. The reaction was performed well at rt with tolerance of some functional groups. Importantly, the selective C-H functionalization did not require added catalyst, oxidant, additive, acid, and base; visible light was the sole requirement.
- Li, Jingjing,Zhang, Pengxiang,Jiang, Min,Yang, Haijun,Zhao, Yufen,Fu, Hua
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supporting information
p. 1994 - 1997
(2017/04/28)
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- Enantioselective Synthesis of Chiral Oxime Ethers: Desymmetrization and Dynamic Kinetic Resolution of Substituted Cyclohexanones
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Axially chiral cyclohexylidene oxime ethers exhibit unique chirality because of the restricted rotation of C=N. The first catalytic enantioselective synthesis of novel axially chiral cyclohexylidene oximes has been developed by catalytic desymmetrization of 4-substituted cyclohexanones with O-arylhydroxylamines and is catalyzed by a chiral BINOL-derived strontium phosphate with excellent yields and good enantioselectivities. In addition, chiral BINOL-derived phosphoric acid catalyzed dynamic kinetic resolution of α-substituted cyclohexanones has been performed and yields versatile intermediates in high yields and enantioselectivities.
- Nimmagadda, Sri Krishna,Mallojjala, Sharath Chandra,Woztas, Lukasz,Wheeler, Steven E.,Antilla, Jon C.
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supporting information
p. 2454 - 2458
(2017/02/23)
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- POLYCYCLIC COMPOUND INCLUDING PYRAZOLE AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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The present invention refers to pyrazole containing an alkali-soluble polymer resin compound including multi annular ring relates to organic light emitting device.
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Paragraph 0172; 0178-0179
(2016/10/08)
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- PYRAZOLE-BASED COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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The present invention relates to a pyrazole-based compound and an organic light emitting device comprising the same. The organic light emitting device comprises a positive electrode, a negative electrode, and one or more layers of organic layers formed between the positive electrode and the negative electrode, wherein one or more layers of organic layers comprise the pyrazole-based compound.COPYRIGHT KIPO 2015
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Paragraph 0093-0096
(2016/10/08)
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- PYRAZOLE-BASED COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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The present invention relates to a pyrazole-based compound and an organic light emitting device comprising the same. The organic light emitting device comprises a positive electrode, a negative electrode, and one or more organic layers formed between the positive electrode and the negative electrode, wherein the organic layers comprise the pyrazole-based compound.COPYRIGHT KIPO 2015
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Paragraph 0134-0137; 0191-193
(2016/10/08)
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- Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
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HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
- Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
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supporting information
p. 7577 - 7589
(2014/12/11)
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- COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
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Page/Page column 101-102
(2012/09/11)
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- Elusive metal-free primary amination of arylboronic acids: Synthetic studies and mechanism by density functional theory
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Herein, we disclose the first metal-free synthesis of primary aromatic amines from arylboronic acids, a reaction that has eluded synthetic chemists for decades. This remarkable transformation affords structurally diverse primary arylamines in good chemical yields, including a variety of halogenated primary anilines that often cannot be prepared via transition-metal-catalyzed amination. The reaction is operationally simple, requires only a slight excess of aminating agent, proceeds under neutral or basic conditions, and, importantly, can be scaled up to provide multigram quantities of primary anilines. Density functional calculations reveal that the most likely mechanism involves a facile 1,2-aryl migration and that the presence of an ortho nitro group in the aminating agent plays a critical role in lowering the free energy barrier of the 1,2-aryl migration step.
- Zhu, Chen,Li, Gongqiang,Ess, Daniel H.,Falck, John R.,Kürti, László
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supporting information
p. 18253 - 18256
(2013/01/15)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 26
(2012/10/08)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 42
(2011/07/30)
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- NOVEL COMPOUNDS HAVING INDAZOLE FRAMEWORKS, METHODS FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Novel compounds having indazole frameworks, as well as a method for preparing the same and a pharmaceutical composition comprising the same are provided. The compounds of the present invention can inhibit protein kinase activity and thus the pharmaceutical composition of the present invention can be used to prevent or treat diseases or disorders which are related to protein kinase activity.
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Page/Page column 8
(2010/10/19)
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- New N-aryloxy-phthalimide derivatives. synthesis, physico-chemical properties, and QSPR studies
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Starting from N-hydroxyphthalimide 1 and the reactive fluoro- or chloro-nitroaryl derivatives 2, 3 and 4a-e (2-chloro-3,5-dinitropyridine; 3, NBD-chloride; 4a, 1-fluoro-2,4-dinitrobenzene; 4b, picryl chloride; 4c, 4-chloro-3,5-dinitrobenzotrifluoride; 4d,
- Tudose, Madalina,Badea, Florin D.,Caproiu, Miron T.,Beteringhe, Adrian,Maganu, Maria,Ionita, Petre,Constantinescu, Titus,Balaban, Alexandru T.
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experimental part
p. 789 - 796
(2011/11/06)
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- IMIDAZOPYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 87
(2009/12/27)
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- NOVEL COMPOUNDS HAVING INDAZOLE FRAMEWORKS, METHODS FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Novel compounds having indazole frameworks, as well as a method for preparing the same and a pharmaceutical composition comprising the same are provided. The compounds of the present invention can inhibit protein kinase activity and thus the pharmaceutical composition of the present invention can be used to prevent or treat diseases or disorders which are related to protein kinase activity.
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Page/Page column 11
(2009/04/25)
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- Highly efficient synthesis of o-(2,4-dinitrophenyl)hydroxylamine. Application to the synthesis of substituted N-benzoyliminopyridinium ylides
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An efficient two-step synthesis of O-(2,4-dinitrophenyl)hydroxylamine is described along with a comparison of its aminating efficiency with O-mesitylenesulfonylhydroxylamine (MSH). It was used in an expedient N-amination/benzoylation procedure involving various substituted pyridines, leading to polysubstituted N-benzoyliminopyridinium ylides, and the scope of its amination power was studied.
- Legault, Claude,Charette, Andre B.
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p. 7119 - 7122
(2007/10/03)
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