- Pyrazole derivative for FGFR inhibitor and preparation method of pyrazole derivative
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The invention provides a pyrazole derivative for an FGFR inhibitor and a preparation method of the pyrazole derivative. The invention specifically relates to an amide pyrazole compound serving as an FGFR irreversible inhibitor, and a preparation method and application thereof. The present invention provides a compound as shown in Formula I, or a pharmaceutically acceptable salt, or solvate, isotope substitute, prodrug, or metabolite thereof. The compound as shown in general formula I have FGFR inhibitory activity, and is capable of preventing or treating disorders associated with FGFR activityor expression, preferably such as cancer.
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Paragraph 0324-0326; 0329-0330
(2021/03/06)
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- BICYCLIC ETHER O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLUCOPYRANOSIDASE INHIBITORS
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Described herein are compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R1, R3, R 4, Y1, Y2, n and p are as defined herein.
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Paragraph 00260
(2020/08/22)
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- Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors
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Fibroblast growth factor receptors (FGFRs) are important oncology targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. We identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound 29 strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that 29 was a potent pan-FGFR inhibitor. The flexibility of our structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy.
- Fan, Jun,Dai, Yang,Shao, Jingwei,Peng, Xia,Wang, Chen,Cao, Sufen,Zhao, Bin,Ai, Jing,Geng, Meiyu,Duan, Wenhu
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supporting information
p. 2594 - 2599
(2016/05/09)
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- QUINAZOLINONE DERIVATIVE
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PROBLEM TO BE SOLVED: To provide a novel compound having effects on 5-HT5A receptor and useful as a therapeutic agent and/or a preventive agent of psychiatric disorders and neurodegenerative diseases to which 5-HT5A receptor relates such as schizophrenia,
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Paragraph 0160
(2016/10/08)
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- Facile synthesis of 7-amino anilinoquinazolines via direct amination of the quinazoline core
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The facile preparation of 4-(3-chloro-4-fluoroanilino)-6-alkoxy-7- aminoquinazolines from their corresponding 7-triflate and 7-fluoro precursors are highlighted.
- Harris, Craig S.,Kettle, Jason G.,Williams, Emma J.
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p. 7381 - 7384
(2007/10/03)
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- Quinazoline derivatives
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The invention concerns quinazoline derivatives of the formula I STR1 wherein R 1 includes hydroxy, amino, hydroxyamino, (1-4C)alkoxy, (1-4C)alkylamino and di-[(1-4C)alkyl]amino;R 3 is halogeno;n is 1, 2 or 3 and R 2 includes hydrogen, hydroxy, halogeno and (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.
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