862729-13-3Relevant academic research and scientific papers
Method for synthesizing 4 -chloropyrropyrimidine compound (by machine translation)
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, (2020/08/09)
The invention relates to a synthesis method of 4 -lopyrrolopyrimidine compound, which comprises the following steps: mixing 4 -hydroxypyrrolopyrimidine, phosphorus oxychloride and organic base in a temperature range &at;timetimewise and removing excess ethanol to obtain 3 - 7-amino-4 -iodopyrrolopyrimidine; thirdly, dissolving the product 4 -amino-4 -methyl pyrrolopyrimidine in DMF at room temperature and then drying and concentrating 4 -aminopyrrolopyridine. 4 -aminopyrimidine is dissolved in dichloromethane and then subjected to a heat preservation reaction to get -5 -aminopyrrolopyrimidine; and the mixture is dried to remove the solid insoluble matter and is dried and concentrated to yield 12 hours-aminopyrroyrimidine after the heat preservation reaction is carried out; and the solvent is evaporated to remove the solid insoluble matter and is dried and concentrated to remove the solid insoluble matter 4 -5 -7. (by machine translation)
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model
Li, Yueshan,Xiong, Yu,Zhang, Guo,Zhang, Liting,Yang, Wei,Yang, Jiao,Huang, Luyi,Qiao, Zeen,Miao, Zhuang,Lin, Guifeng,Sun, Qiu,Niu, Ting,Chen, Lijuan,Niu, Dawen,Li, Linli,Yang, Shengyong
, p. 11398 - 11414 (2019/01/08)
We herein report the structural optimization and structure-activity relationship studies of 5-(2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as a new class of receptor-interacting protein kinase 1 (RIPK1) inhibitors. Among all obtained RIPK1 inhibitors, 1-(5-{4-amino-7-ethyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl}-2,3-dihydro-1H-indol-1-yl)-2-[3-(trifluoromethoxy)phenyl]ethan-1-one (22b) is the most active one. This compound potently inhibited RIPK1 with a binding affinity (KD) of 0.004 μM and an enzymatic IC50 value of 0.011 μM and also showed good kinase selectivity. It could efficiently protect cells from necroptosis and attenuate the necrotic cell death of vascular endothelial cells induced by tumor cells both in vitro and in vivo. Importantly, compound 22b exhibited excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model. It also displayed favorable pharmacokinetic properties. Collectively, 22b could be a promising agent for preventing tumor metastasis.
N-(SUBSTITUTED-PHENYL)-SULFONAMIDE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 24, (2018/04/11)
The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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, (2014/12/12)
The present invention relates to 6-amino-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present
Kinase antagonists
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Page/Page column 25, (2008/06/13)
The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.
Aminobenzoxazoles as therapeutic agents
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Page/Page column 119, (2010/02/15)
A compound of Formula (I), wherein the substituents are as defined herein, which are useful as kinase inhibitors.
