849217-48-7Relevant academic research and scientific papers
Methylpyrazole derivatives as RET inhibitor
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, (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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, (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
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis
Huang, Zhi,Zhao,Qin, Zhongxiang,Li, Yongtao,Wang, Tianqi,Zhou, Wei,Zheng, Jianyu,Yang, Shengyong,Shi, Yi,Fan, Yan,Xiang, Rong
, (2019/08/07)
Based on the significantly synergistic effects of CDK4 and VEGFR2 inhibitors on growth of cancer cells, a series of novel multi-kinase inhibitors targeting CDK4 and VEGFR2 were designed, synthesized and evaluated, among which Roxyl-ZV-5J exhibited potent and balanced activities against both CDK4 and VEGFR2 with half-maximal inhibitory concentration at the nanomolar level. It effectively induced breast and cervical cancer cell cycle arrest and cell apoptosis. Roxyl-ZV-5J also inhibited the proliferation, tube formation and VEGFR2 downstream signaling pathways of HUVECs. Oral administration of Roxyl-ZV-5J led to significant tumor regression and anti-angiogenesis without obvious toxicity in SiHa xenograft mouse model. In addition, this compound showed good pharmacokinetics. This study confirmed a new tool for dual CDK-VEGFR2 pathways inhibition achieved with a single molecule, which provided valuable leads for further structural optimization and anti-angiogenesis and anti-tumor mechanism study.
Compound with sulfonyl phenylamine pyrimidine structure and application of compound as antitumor medicine
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Paragraph 0072; 0075; 0076, (2019/11/13)
The invention discloses a compound with a sulfonyl phenylamine pyrimidine structure and application of the compound as an antitumor medicine. Pharmacology experiments show that the compound has multi-target inhibition activity, has good multi-target inhib
