204452-91-5Relevant articles and documents
Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors
Chen, Hao,Ding, Ke,Huang, Jing,Li, Jie,Peng, Lijie,Tu, Zheng-Chao,Zhang, Zhang,Zhang, Zhen,Zhou, Yang
supporting information, p. 3249 - 3265 (2022/02/16)
Aberrant FGF19/FGFR4 signaling is an oncogenic driver force for the development of human hepatocellular carcinoma (HCC). A series of 2-formyl tetrahydronaphthyridine urea derivatives were designed and synthesized as new covalently reversible inhibitors of
Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design
Zhang, Zhen,Wang, Yongjin,Chen, Xiaojuan,Song, Xiaojuan,Tu, Zhengchao,Chen, Yongheng,Zhang, Zhimin,Ding, Ke
supporting information, (2021/10/21)
An aromatic trifluoromethyl ketone moiety was characterized as a new warhead for covalently reversible kinase inhibitor design to target the non-catalytic cysteine residue. Potent and selective covalently reversible inhibitors of FGFR4 kinase were success
High-selectivity fibroblast growth factor receptor inhibitor and application
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Paragraph 0088; 0095-0098, (2021/07/08)
The invention discloses a high-selectivity fibroblast growth factor receptor inhibitor and application, and particularly relates to a compound shown in a formula (I) or a pharmaceutically acceptable salt, a solvate, a geometric isomer, a stereoisomer, a tautomer and any mixture thereof. The compound shown in the formula (I) or the pharmaceutically acceptable salt, the solvate and the pharmaceutical composition thereof can be applied to prevention or treatment of diseases related to FGFR4 activity or overexpression, and can also be combined with other medicines to be used for treating various related diseases, especially for treating various cancers, wherein the cancers may be liver cancer, lung cancer, gastric cancer, breast cancer, ovarian cancer, prostate cancer, renal cell carcinoma, skin cancer, colon cancer, bile duct cancer, glioma or sarcoma.
COMPOUNDS FOR INHIBITING FGFR4
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Paragraph 0215-0216, (2021/01/22)
Provided herein are compounds which inhibit FGFR4, compositions thereof, methods of their preparation, and methods for treating disorders mediated by FGFR4 such as cancer.
FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF
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Paragraph 0161; 0162, (2019/02/28)
The present invention relates to an FGFR4 inhibitor having a structure represented by formula (I), preparation method therefor, and applications thereof. A series of compounds represented by formula (I) in the present invention have a very-strong inhibiti
FGFR4 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0135; 0136, (2019/06/27)
Provided are an FGFR4 inhibitor with the structure of formula (I) and a preparation method and use thereof. The series of compounds of formula (I) have a very strong inhibitory effect on the FGFR4 kinase activity, and have a very high selectivity; and sam
COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE
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Page/Page column 19, (2016/10/11)
This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administrat
PHARMACEUTICAL COMBINATIONS
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Page/Page column 52, (2016/10/11)
A pharmaceutical combination comprising N-(5-cyano-4-((2-methoxyethyl)amino)pyridin- 2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine- 1(2H)-carboxamide, or a pharmaceutically acceptable salt thereof, and at least one active ingredient, as defined herein, or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, for simultaneous or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
PARTICLES OF N-(5-CYANO-4-((2-METHOXYETHYL)AMINO)PYRIDIN-2-YL)-7-FORMYL-6-((4-METHYL-2- OXOPIPERAZIN-1-YL)METHYL)-3,4-DIHYDRO-1,8-NAPHTHYRIDINE-1(2H)-CARBOXAMIDE
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Page/Page column 24; 25, (2016/10/11)
The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7- formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.
Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
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Paragraph 0568; 0569, (2015/05/05)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.