849217-48-7Relevant academic research and scientific papers
Methylpyrazole derivatives as RET inhibitor
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Paragraph 0432-0434; 0438-0440, (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.
Preparation method of broad-spectrum anti-cancer drug kimatinib (by machine translation)
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Paragraph 0075; 0077-0105, (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
DIOXAZOLINE COMPOUND, PREPARATION METHOD THEREFOR, AND USES THEREOF
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Paragraph 0059-0060, (2020/12/22)
The present invention relates to a dioxazoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2 and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
Method of Treating Cancer and Bone Cancer Pain
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Paragraph 0111; 0115; 0119; 0124, (2020/08/25)
This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in a
Method of Treating Cancer
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Paragraph 0110; 0117-0118; 0126; 0134-0135, (2020/11/30)
This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
Preparation method of cabozantinib nitrogen oxide impurity
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, (2020/08/27)
The invention discloses a preparation method of a cabozantinib nitrogen oxide impurity. The method comprises the following steps: preparation of an intermediate 1, preparation of 4-chloro-6, 7-dimethoxyquinoline, preparation of an intermediate 2, and prep
AN IMPROVED PROCESS FOR THE PREPARATION OF CABOZANTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Page/Page column 10-11, (2019/12/28)
The present invention relates to an improved process for the preparation of N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide compound of formula-1 which is represented by the following structural formula:
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.
