629645-53-0Relevant academic research and scientific papers
Macrocyclic JAK2 inhibitor and application thereof
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Paragraph 0133-0137, (2021/02/06)
The invention relates to a macrocyclic JAK2 inhibitor and an application thereof. Specifically, the invention relates to a compound shown as a formula I and an application of the compound in treatingJAK2-mediated related diseases and preparing medicines for treating the JAK2-mediated related diseases.
Design and Synthesis of a Series of Novel Macrocycle Janus Kinase 2 Inhibitors
Wang, Yanling,Ge, Huan,Wang, Disha,He, Huan,Li, Lu,Diao, Yanyan,Shen, Zihao,Zhu, Lili,Li, Shiliang,Zhao, Zhenjiang,Li, Honglin
supporting information, p. 1259 - 1263 (2019/11/21)
Macrocycle has attracted the attention of many researchers in the field of medicinal chemistry due to its unique advantages and good prospects, but the difficulties in drug design and synthesis of macrocycle limit its applications. In this study, a series of macrocyclic derivatives designed from anaplastic lymphoma kinase (ALK) inhibitor lorlatinib were synthesized as Janus kinase 2 (JAK2) selective inhibitors. Among them, 17f had the best inhibitory activity (IC50 = 0.177 μmol·L–1) and selectivity for JAK2 over JAK1 and JAK3, which indicated that design of the macrocyclic derivatives might be a feasible strategy for the discovery of novel selective JAK2 inhibitors.
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Paragraph 0081; 0082, (2016/04/10)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Paragraph 0103; 0107-0109, (2016/11/02)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
Synthesis of 2-(pyrimidin-4-yl)indoles
Franco, Laura Hernandez,Palermo, Jorge Alejandro
, p. 975 - 977 (2007/10/03)
The synthesis of 2-substituted isomers of the meridianins, a familiy of bioactive indole alkaloids isolated from the tunicate Aplidium meridianum, was undertaken. The synthetic route comprises six steps, with a microwave promoted Fischer cyclization as th
