1231930-27-0Relevant articles and documents
KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
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Paragraph 0170; 0325, (2020/07/21)
Disclosed are kinase inhibitor compounds having the following structure: (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3,R4, R5, R6, N-Ar, X, Y, Z, and AA are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
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Paragraph 0329, (2020/07/21)
Disclosed herein are kinase inhibitor compounds having structure (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, X, Y, Z, and (AA) are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
Substituted benzimidazole derivatives
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, (2018/01/09)
The invention belongs to the field of pharmaceutical chemistry, particularly relates to substituted benzimidazole derivatives as well as a preparation method and pharmaceutical composition thereof and further relates to an application of the substituted b
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor
Hu, Jianping,Wang, Yingqing,Li, Yanlian,Xu, Lin,Cao, Danyan,Song, ShanShan,Damaneh, Mohammadali Soleimani,Wang, Xin,Meng, Tao,Chen, Yue-Lei,Shen, Jingkang,Miao, Zehong,Xiong, Bing
, p. 176 - 195 (2017/06/07)
Recent years have seen much effort to discover new chemotypes of BRD4 inhibitors. Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 μM and 0.13 μM, respectively. Although the concept of dual inhibition is intriguing, selective BRD4 inhibitors are preferred as they may diminish off-target effects and provide more flexibility in anticancer drug combination therapy. Inspired by BI-2536, we designed and prepared a series of dihydroquinoxalin-2(1H)-one derivatives as selective bromodomain inhibitors. We found compound 54 had slightly higher activity than (+)-JQ1 in the fluorescence anisotropy assay and potent antiproliferative cellular activity in the MM.1S cell line. We have successfully solved the cocrystal structure of 52 in complex with BRD4-BD1, providing a solid structural basis for the binding mode of compounds of this series. Compound 54 exhibited high selectivity over most non-BET subfamily members and did not show bioactivity towards the PLK1 kinase at 10 or 1 μM. From in vivo studies, compound 54 demonstrated a good PK profile, and the results from in vivo pharmacological studies clearly showed the efficacy of 54 in the mouse MM.1S xenograft model.
BENZIMIDAZOLE DERIVATIVES AS ANTIVIRAL AGENTS
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, (2013/02/28)
Provided are compounds of Formulas I, II, III, IV, V, and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
PROTEIN KINASE INHIBITORS
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Page/Page column 9-10, (2010/07/04)
The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof which is useful in the treatment of cell proliferative diseases.
