77476-95-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant
Li, Yupeng,Shen, Mengjie,Zhang, Zhang,Luo, Jinfeng,Pan, Xiaofen,Lu, Xiaoyun,Long, Huoyou,Wen, Donghai,Zhang, Fengxiang,Leng, Fang,Li, Yingjun,Tu, Zhengchao,Ren, Xiaomei,Ding, Ke
, p. 10033 - 10046 (2013/01/16)
A series of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p-loop mutations, which are associated with disease progression in CML. The most potent compounds 6q and 6qo strongly inhibited the kinase activities of Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.60, 0.36 and 1.12, 0.98 nM, respectively. They also potently suppressed the proliferation of K562, KU812 human CML cells, and a panel of murine Ba/F3 cells ectopically expressing either Bcr-AblWT or any of a panel of other Bcr-Abl mutants that have been shown to contribute to clinical acquired resistance, including Bcr-AblT315I, with IC50 values in low nanomolar ranges. These compounds may serve as lead compounds for further development of new Bcr-Abl inhibitors capable of overcoming clinical acquired resistance against imatinib.
OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
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Page/Page column 136, (2012/03/11)
The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
BIARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 168, (2011/04/13)
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
NEW COMPOUNDS
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Page/Page column 17, (2010/04/03)
The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use
Halogeno derivatives of isopropylamino pyrimidine and therapeutic use
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, (2008/06/13)
The invention relates to new isopropylamino pyrimidine halogeno derivatives of the formula: STR1 in which X represents a fluorine, a chlorine or a bromine atom. These compounds, when X stands for chlorine or bromine, are prepared by reacting, at room temperature and in stoichiometric proportions, 2-isopropylamino pyrimidine on the appropriate N-halogeno succinimide, in the presence of acetic acid.
