558443-53-1Relevant academic research and scientific papers
2, 3-dihydrobenzofuranamide derivatives and application thereof
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Paragraph 0248-0253, (2020/04/17)
The invention discloses 2,3-dihydrobenzofuranamide derivatives and an application thereof, and particularly relates to novel 2,3-dihydrobenzofuranamide derivatives and a pharmaceutical composition containing the compounds. The compounds can be used as a 5-HT4 receptor agonist. The invention also relates to methods for preparing the compounds and the pharmaceutical composition, and an application of the compounds and the pharmaceutical composition in the preparation of drugs for treating diseases related to the activity of the 5-HT4 receptor, especially constipation type allergic bowel syndrome(IBS-C).
Substituted benzamide derivative and application thereof
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Paragraph 0236-0241, (2020/04/17)
The invention discloses a substituted benzamide derivative and application thereof and particularly relates to a novel substituted benzamide derivative and a pharmaceutical composition containing thecompound, and the substituted benzamide derivative can b
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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Page/Page column 82, (2016/12/16)
Compounds of formula (I) that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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Page/Page column 135, (2015/09/23)
Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for
NOVEL COMPOUND HAVING ANGIOGENESIS INHIBITORY ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0083; 0084, (2014/07/23)
Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formular I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.
Novel Compound Having Angiogenesis Inhibitory Activity, Method for Preparing Same, and Pharmaceutical Composition Comprising Same
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Paragraph 0197; 0198; 0199, (2014/09/29)
Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.
INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 35, (2014/05/07)
The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.
Bioorthogonal imaging of Aurora Kinase A in live cells
Yang, Katherine S.,Budin, Ghyslain,Reiner, Thomas,Vinegoni, Claudio,Weissleder, Ralph
supporting information; experimental part, p. 6598 - 6603 (2012/09/22)
In living color: Aurora kinase A (AKA) was imaged in live cells using a bioorthogonal two-step reaction with a small molecule AKA inhibitor (see scheme) and a fluorescent reporter. The fluorescent molecule was localized to spindle poles and microtubules d
GAS CAPTURE PROCESS
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Page/Page column 49, (2012/11/07)
A process for the capture of CO2 from gas streams, the process including contacting a CO2 containing gas stream with a compound including: a primary or non-sterically hindered secondary amine group and at least one tertiary amine or sterically hindered secondary amine group; wherein the primary or non-sterically hindered secondary amine and the nearest tertiary or sterically hindered secondary amine group are separated by a carbon chain including 3 or 4 carbon atoms and wherein the compound is a compound of Formula (I).
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activity
Reck, Folkert,Alm, Richard,Brassil, Patrick,Newman, Joseph,Dejonge, Boudewijn,Eyermann, Charles J.,Breault, Gloria,Breen, John,Comita-Prevoir, Janelle,Cronin, Mark,Davis, Hajnalka,Ehmann, David,Galullo, Vincent,Geng, Bolin,Grebe, Tyler,Morningstar, Marshall,Walker, Phil,Hayter, Barry,Fisher, Stewart
experimental part, p. 7834 - 7847 (2012/01/06)
Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-resistance with fluoroquinolones. Aminopiperidines that have a bicyclic aromatic moiety linked through a carbon to an ethyl bridge, such as 1, generally show potent broad-spectrum antibacterial activity, including quinolone-resistant isolates, but suffer from potent hERG inhibition (IC50= 3 M for 1). We now disclose the finding that new analogues of 1 with an N-linked cyclic amide moiety attached to the ethyl bridge, such as 24m, retain the broad-spectrum antibacterial activity of 1 but show significantly less hERG inhibition (IC 50= 31 M for 24m) and higher free fraction than 1. One optimized analogue, compound 24l, showed moderate clearance in the dog and promising efficacy against Staphylococcus aureus in a mouse thigh infection model.
