1345847-71-3Relevant academic research and scientific papers
Methylpyrazole derivatives as RET inhibitor
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Paragraph 0432-0437, (2021/07/21)
The invention relates to a methylpyrazole derivative as an RET inhibitor, in particular to a compound as shown in a formula (I), a stereoisomer and pharmaceutically acceptable salt thereof, a preparation method and a pharmaceutical composition thereof. The compound of the formula (I) can be used for preventing or treating diseases mediated by abnormal RET activity.
COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
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Paragraph 00245; 00295-00296, (2020/08/13)
The present invention relates to compounds that modulate cellular activities such as proliferation, differentiation, programmed cell death, migration, and chemoinvasion, by modulating protein kinase enzymatic activity, and compositions thereof, and methods of using such compounds.
Preparation method of broad-spectrum anti-cancer drug kimatinib (by machine translation)
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Paragraph 0075-0104, (2020/04/02)
The preparation method is simple, the reaction conditions are mild . the reaction conditions are mild, the intermediate stability is good, the side reaction: is less likely to occur, and the preparation method is very suitable for industrial production: a
Synthesis and anti-tumor activity of [1,4] dioxino [2,3-f] quinazoline derivatives as dual inhibitors of c-Met and VEGFR-2
Wei, Dengshuai,Fan, Haoru,Zheng, Kun,Qin, Xuemei,Yang, Leifu,Yang, Yajuan,Duan, Ye,Zhang, Qiang,Zeng, Chengchu,Hu, Liming
, (2019/04/27)
Both c-Met and VEGFR-2 were important targets for cancer therapies. In order to develop reversible and non-covalent c-Met and VEGFR-2 dual inhibitors, a series of [1,4]dioxino[2,3-f]quinazoline derivatives were designed and synthesized. The enzyme assay demonstrated that most target compounds had inhibition potency on both c-Met and VEGFR-2 with IC50 values in nanomolar range especially compounds 7m and 7k. Based on further cell proliferation assay in vitro, compound 7k showed significantly anti-tumor activity in vivo on a hepatocellular carcinoma (MHCC97H cells) xenograft mouse model. We docked the compound 7m with c-Met and VEGFR-2 kinases, and interpreted the SAR of these analogues. All results indicated that the target compounds were dual inhibitors of c-Met and VEGFR-2 kinases that held promising potential in cancer therapy.
Preparation method of Cabozantinib
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Paragraph 0053-0055, (2019/08/12)
The invention belongs to the field of pharmaceutical chemistry, and relates to a preparation method of Cabozantinib. The preparation method comprises following steps: 4-halogenated-6, 7-dimethoxyquinoline is reacted with 4-aminophenol to prepare a compoun
Preparation method of cabozantinib (S)-malate and intermediate thereof
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Paragraph 0078-0079, (2019/07/04)
The invention relates to a preparation method of cabozantinib (S)-malate and an intermediate thereof. The method includes: taking 4-chloro-6, 7-dimethoxyquinoline (I) as the starting raw material, andconducting substitution, condensation and salt formatio
PYRIDO-AZAHETERECYDIC COMPOUND AND PREPARATION METHOD AND USE THEREOF
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, (2018/09/21)
The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.
ASYMMETRIC BISAMIDATION OF MALONIC ESTER DERIVATIVES
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Page/Page column 87; 88, (2017/03/14)
The present invention relates to processes, process steps and intermediates useful in the asymmetric bisamidation of malonic ester derivatives wherein the new processes, process steps and intermediates are, for example, useful in the preparation of asymme
COMPOUNDS AS C-MET KINASE INHIBITORS
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Page/Page column 23, (2012/03/27)
The present invention relates to compounds, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with the inhibition of the protein tyrosine kinase activi
CYCLOPROPYL DICARBOXAMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITES
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Page/Page column 33, (2011/11/13)
The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: Formula I or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
