317806-87-4Relevant academic research and scientific papers
POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES
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Page/Page column 166, (2021/01/29)
The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition associated with muscle cells and/or satellite cells, such as Duchenne muscular dystrophy, Becker muscular dystrophy, cachexia or sarcopenia.
Substituted benzo pyrazole diaryl urea compound, its preparation method and medical use thereof (by machine translation)
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, (2017/04/25)
The invention substituted benzo pyrazole diaryl urea compound, its preparation method and medical use thereof relates to a compound of formula I, or an isomer, a pharmaceutically acceptable salt and solvates; the invention also relates to the general formula I compound or its isomer, pharmaceutically acceptable salt and solvates, and a pharmaceutically acceptable carrier, excipient or diluent composition; the invention also relates to the compounds of the formula I, or an isomer, a pharmaceutically acceptable salt and solvates, used for overcoming the inflammation, inflammation-related diseases, tumor and asphyxiating gas or irritant gas caused by the use of acute lung injury; in particular with the P38 MAPK pathway-related diseases or symptoms in use. (by machine translation)
Novel diaryl urea compounds, and preparation method and medical applications thereof
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, (2017/06/02)
The invention relates to compounds represented by the formula (I), and isomers, pharmaceutically acceptable salts, and solvates thereof. The invention further relates to a composition, which comprises abovementioned compounds, isomers, salts, and solvates, and a pharmaceutically acceptable carrier, excipient, or diluent; and applications of abovementioned compounds, isomers, salts, and solvates in treating diseases and symptoms of acute lung injury caused by inflammation, diseases related with inflammation, tumor, suffocating gas, and irritant gas, especially an application of treating P38MAPK related diseases and symptoms.
Substituted benzothiazole diaryl urea compounds, and preparation method and medical application thereof
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, (2017/08/28)
The invention relates to compounds as shown in a general formula I which is described in the specification, or isomers, medicinal salts and solvates thereof. The invention also relates to a composition containing the compounds as shown in the general formula I or the isomers, medicinal salts and solvates thereof, and a pharmaceutically acceptable carrier, an excipient or a diluent. The invention also relates to application of the compounds as shown in the general formula I or the isomers, medicinal salts and solvates thereof to treatment of inflammations, inflammation-related diseases, tumors and acute lung injury or symptoms caused by suffocating gas or irritant gas, especially to diseases or symptoms related to a P38 MAPK pathway.
Synthesis and p38 inhibitory activity of some novel substituted N,N′-diarylurea derivatives
Zhu, Dianxi,Xing, Qifeng,Cao, Ruiyuan,Zhao, Dongmei,Zhong, Wu
, (2016/07/06)
We have identified a novel series of substituted N,N′-diarylurea p38α inhibitors. The inhibitory activity of the target compounds against the enzyme p38α, MAPKAPK2 in BHK cells, TNF-α release in LPS-stimulated THP-1 cells and p38α binding experiments were
P38 MAP KINASE INHIBITING INDANYL UREA COMPOUNDS
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Page/Page column 31, (2016/03/22)
The present application relates to p38 MAPK inhibiting indanyl urea derivatives and its process of preparation, pharmaceutical composition and use for the preparation of medicament for treatment of inflammatory diseases such as airway diseases.
Design, synthesis and biological evaluation of novel substituted N,N′-diaryl ureas as potent p38 inhibitors
Zhu, Dianxi,Li, Xingzhou,Zhong, Wu,Zhao, Dongmei
, p. 16604 - 16619 (2015/12/01)
A novel series of substituted N,N′-diaryl ureas that act as p38α inhibitors have been designed and synthesized based on two key residues (Gly110 and Thr106) that are different in p38α MAPK than in other kinases. Preliminary biological evaluation indicated
2,3-DIHYDRO-1H-INDENE-2-YL UREA DERIVATIVE AND PHARMACEUTICAL APPLICATION OF SAME
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, (2012/07/28)
A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
Short Synthesis of 1-(3-tert-Butyl-1-phenyl-1H-pyrazol-5-yl)-3-(5-(2- morpholinoethoxy)-2H-chromen-8-yl) urea derivatives
Li, Xingzhou,Zhou, Xinming,Zheng, Zhibing,Zhong, Wu,Xiao, Junhai,Li, Song
experimental part, p. 3999 - 4009 (2009/12/24)
A short and efficient synthesis of 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5- yl)-3-(5-(2-morpholinoethoxy)-2H-chromen-8-yl) urea derivatives (1a-c), a novel type of p38 MAPK inhibitors, is described. The Claisen thermal rearrangement of arylpropargyl ethers
Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors
Simard, Jeffrey R.,Getlik, Matthaeus,Gruetter, Christian,Pawar, Vijaykumar,Wulfert, Sabine,Rabiller, Matthias,Rauh, Daniel
supporting information; experimental part, p. 13286 - 13296 (2010/01/30)
Kinase disregulation disrupts the intricate network of intracellular signaling pathways and contributes to the onset of diseases such as cancer. Although several kinase inhibitors are on the market, inhibitor selectivity and drug resistance mutations persist as fundamental challenges in the development of effective long-term treatments. Chemical entities binding to less conserved allosteric sites would be expected to offer new opportunities for scaffold development. Because no high-throughput method was previously available, we developed a fluorescence-based kinase binding assay for identifying and characterizing ligands which stabilize the inactive kinase conformation. Here, we present a description of the development and validation of this assay using the serine/threonine kinase p38R. By covalently attaching fluorophores to the activation loop of the kinase, we were able to detect conformational changes and measure the Kd, kon, and koff associated with the binding and dissociation of ligands to the allosteric pocket. We report the SAR of a synthesized focused library of pyrazolourea derivatives, a scaffold known to bind with high affinity to the allosteric pocket of p38R. Additionally, we used protein X-ray crystallography together with our assay to examine the binding and dissociation kinetics to characterize potent quinazoline- and quinoline-based type II inhibitors, which also utilize this binding pocket in p38α. Last, we identified the b-Raf inhibitor sorafenib as a potent low nanomolar inhibitor of p38α and used protein X-ray crystallography to confirm a unique binding mode to the inactive kinase conformation.
