- QUINOLIN-4-ONE AND 4(1H)-CINNOLINONE COMPOUNDS AND METHODS OF USING SAME
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The present disclosure relates to quinolin-4-one and 4(1H)-cinnolinone compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
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Paragraph 00882; 00885-00886
(2020/08/22)
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- Preparation method of ethyl (pentafluorobenzoyl)acetate
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The invention discloses a preparation method of ethyl (pentafluorobenzoyl)acetate. The preparation method comprises the following steps: replacing air in a reaction bottle with nitrogen which serves as protective gas, adding potassium ethyl malonate, acetonitrile and a catalyst A into the reaction bottle, carrying out stirring for 4-6 hours, performing cooling to -5 DEG C, dropwise adding pentafluorobenzoyl chloride, performing stirring for a reaction for 8 hours, and conducting drying by distillation under reduced pressure after the reaction is finished so as to obtain light yellow liquid, namely ethyl (pentafluorobenzoyl)acetate. The method is high in conversion rate and convenient for industrial production.
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Paragraph 0006
(2020/04/17)
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- Inhibition of the signal transducer and activator of transcription-3 (STAT3) signaling pathway by 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid esters
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The JAK-STAT3 pathway regulates genes that are important in cell proliferation and thus is a promising target for cancer therapy. A high-throughput screening (HTS) campaign using an Apo-ONE Homogenous Caspase 3/7 assay in U266 cells identified 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 4 as a potential STAT3 pathway inhibitor. Optimization of this HTS hit led to the identification of the 7-cyano analogue 8, which inhibited STAT3-Y705 phosphorylation with an EC50 of 170 nM. Compound 8 also inhibited cytokine induced JAK activation but did not inhibit BCR-ABL activated STAT5 phosphorylation in K562 cells.
- Xu, Jun,Cole, Derek C.,Chang, Chao-Pei Betty,Ayyad, Ramzi,Asselin, Magda,Hao, Wenshan,Gibbons, James,Jelinsky, Scott A.,Saraf, Kathryn A.,Park, Kaapjoo
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experimental part
p. 4115 - 4121
(2009/05/27)
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- Aminoquinolones as GSK-3 inhibitors
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Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.
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Page/Page column 75
(2008/06/13)
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- ANTIMICROBIAL QUINOLONES, THEIR COMPOSITIONS AND USES
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Compounds of the following formula (I) are effective antimicrobial agents.
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- 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof
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2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
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- Quinobenzoxazine, antineoplastic agents
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Quinobenzoxazine, derivatives of the formula STR1 as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R1 is hydrogen or a carboxy-protecting group, R2 and R3 are substitutents, A is oxygen, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.
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- A safe, economical method for the preparation of β-oxo esters
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A high yield, economical method for preparation of β-oxo esters has been developed involving the reaction of acid chlorides with potassium ethyl malonate using a magnesium chloride-triethylamine base system in either acetonitrile or ethyl acetate solvents. The method is suitable for the preparation of high purity β-oxo esters in the laboratory and also in large scale production.
- Clay,Collom,Karrick,Wemple
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p. 290 - 292
(2007/10/02)
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- 7-(substituted)piperazinyl-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
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7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.
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- Trifluoro- quinoline -3- carboxylic acids and their use as anti-bacterial agents
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Novel difluoro-naphthyridine- and trifluoroquinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
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