79257-61-7Relevant academic research and scientific papers
Heterocyclic compounds as FGFR4 inhibitors
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Paragraph 0127; 0138-0142, (2021/02/10)
The present invention provides heterocyclic compounds as selective inhibitors of fibroblast growth factor receptor 4 (FGFR4), pharmaceutical compositions containing the compounds, methods of preparingthe compounds, and methods of treating cell proliferative diseases, such as cancer, using the compounds of the invention.
Pyrido[2,3-b]pyrazine-3(4H)-ketone derivative and application thereof
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Paragraph 0019-0020; 0038, (2021/03/13)
The invention provides a pyrido[2,3-b]pyrazine-3(4H)-ketone derivative and application thereof. The structural general formula of the pyrido[2,3-b]pyrazine-3(4H)-ketone derivative is a formula V, andthe pyrido[2,3-b]pyrazine-3(4H)-ketone derivative comprises pharmaceutically acceptable salt, solvate, hydrate or crystal form thereof. The compound provided by the invention is an active ligand of afibroblast growth factor receptor (FGFR), and research shows that the compound shown in the structure V has good anti-proliferative activity on KATO III gastric cancer cells (FGFR2 amplification) andHuh-7 liver cancer cells (FGFR4 overexpression), and is applied to preparation of drugs for treating tumor-related diseases caused by FGFR abnormal activation as an FGFR inhibitor. The structural general formula V is shown in the description.
Concentration-Dependent Thermal Isomerization of Nitrile N-Oxide
Bando, Shiho,Koyama, Yasuhito,Takata, Toshikazu
, (2020/08/13)
Kinetically stabilized nitrile N-oxides (NOs) have been regarded as viable tools for the postpolymerization functionalization of common polymers. However, thermal isomerization of NO to isocyanate restricts the applications of NO to industrial use. The re
KOtBu-Promoted Transition-Metal-Free Transamidation of Primary and Tertiary Amides with Amines
Ghosh, Tridev,Jana, Snehasish,Dash, Jyotirmayee
supporting information, p. 6690 - 6694 (2019/09/12)
This work discloses transamidation of primary and tertiary amides with a range of aryl, heteroaryl, and aliphatic amines using potassium tert-butoxide. The reaction proceeds at room temperature under transition-metal-free conditions providing secondary amides in high yields. Moreover, reaction of cyclopropyl amine with tertiary amides proceeds with ring-opening to provide a rapid access to enamides.
Substituent effects in solid-state assembly of activated benzotriazoles
Wenholz, Daniel S.,Bhadbhade, Mohan,Kandemir, Hakan,Ho, Junming,Kumar, Naresh,Black, David Stc.
, p. 835 - 842 (2019/02/05)
Aromatic donor-acceptor stacking involving electron-rich π-donors and electron-deficient π-acceptors has been utilized in a broad spectrum of diverse applications to great effect. We report the discovery of unprecedented donor-acceptor stacking from a non
Selective Oxidative Coupling Reaction of Isocyanides Using Peroxide as Switchable Alkylating and Alkoxylating Reagent
Zhang, Xinglu,Liu, Zhiqiang,Gao, Yu,Li, Feng,Tian, Yaming,Li, Chunju,Jia, Xueshun,Li, Jian
supporting information, p. 272 - 277 (2017/11/13)
A switchable oxidative coupling reaction of isocyanide and peroxide has been disclosed. In the presence of iron catalyst, the coupling reaction affords N-arylacetamides in good yields. By simply replacing the iron with copper catalyst, another different coupling reaction takes place in which peroxide can serve as alkoxylating source. This protocol represents a new fundamental coupling of two basic chemicals involving C?C and C?O bond-forming process. The unusual reactivity of an isocyano group in a radical reaction acting formally as an amidoyl synthon has also been well established. The experiment outcome reveals that aromatic isocyanides are particularly compatible reaction partners in present coupling reaction, whereas no desired products are observed when aliphatic isocyanides are used. (Figure presented.).
Regioselective nitration of anilines with Fe(NO3)3·9H2O as a promoter and a nitro source
Gao, Yang,Mao, Yuanyou,Zhang, Biwei,Zhan, Yingying,Huo, Yanping
supporting information, p. 3881 - 3884 (2018/06/08)
An efficient Fe(NO3)3·9H2O promoted ortho-nitration reaction of aniline derivatives has been developed. This reaction may go through a nitrogen dioxide radical (NO2) intermediate, which is generated by the thermal decomposition of iron(iii) nitrate. The practicality of the present method using nontoxic and inexpensive iron reagents has been shown by the broad substrate scope and applications.
FGFR4 INHIBITORS
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Page/Page column 35, (2016/10/31)
Methods, compounds, pharmaceutical compositions, and methods of preparing medicaments for treating hepatocellular carcinoma having an altered FGFR4 and/or FGF19 status.
FGFR4 INHIBITORS
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Page/Page column 33, (2016/10/31)
We provide FGFR inhibitors, their salts, methods of manufacture, and methods of use.
HETEROARYLAMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Paragraph 0094; 0095, (2016/06/21)
A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an act
