1186609-08-4Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Paragraph 0611; 0613, (2017/09/30)
Disclosed are compounds of Formula I(b): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Ring A, Ring HD, J, each T, R3, R4, R5, each R7, and m are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
N-(3-ethynyl-2,4-difluorophenyl)sulfonamide derivatives as selective Raf inhibitors
Li, Yingjun,Cheng, Huimin,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Long, Huoyou,Zhou, Yang,Xu, Yong,Taghipouran, Rana,Li, Dan,Patterson, Adam,Smaill, Jeff,Tu, Zhengchao,Wu, Donghai,Ren, Xiaomei,Ding, Ke
supporting information, p. 543 - 547 (2015/05/27)
A series of N-(3-ethynyl-2,4-difluorophenyl)sulfonamides were identified as new selective Raf inhibitors. The compounds potently inhibit B-RafV600E with low nanomolar IC50 values and exhibit excellent target specificity in a selectivity profiling investigation against 468 kinases. They strongly suppress proliferation of a panel of human cancer cell lines and patient-derived melanoma cells with B-RafV600E mutation while being significantly less potent to the cells with B-RafWT. The compounds also display favorable pharmacokinetic properties with a preferred example (3s) demonstrating significant in vivo antitumor efficacy in a xenograft mouse model of B-RafV600E mutated Colo205 human colorectal cancer cells, supporting it as a promising lead compound for further anticancer drug discovery.
BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF
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, (2015/03/16)
Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS
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Page/Page column 117, (2009/10/22)
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
