- Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors
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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
- Chen, Hao,Ding, Ke,Huang, Jing,Li, Jie,Peng, Lijie,Tu, Zheng-Chao,Zhang, Zhang,Zhang, Zhen,Zhou, Yang
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supporting information
p. 3249 - 3265
(2022/02/16)
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- Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design
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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
- Zhang, Zhen,Wang, Yongjin,Chen, Xiaojuan,Song, Xiaojuan,Tu, Zhengchao,Chen, Yongheng,Zhang, Zhimin,Ding, Ke
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supporting information
(2021/10/21)
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- High-selectivity fibroblast growth factor receptor inhibitor and application
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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.
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Paragraph 0088; 0095-0098
(2021/07/08)
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- COMPOUNDS FOR INHIBITING FGFR4
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Provided herein are compounds which inhibit FGFR4, compositions thereof, methods of their preparation, and methods for treating disorders mediated by FGFR4 such as cancer.
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Paragraph 0215-0216
(2021/01/22)
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- FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF
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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
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Paragraph 0161; 0162
(2019/02/28)
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- FGFR4 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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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
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Paragraph 0135; 0136
(2019/06/27)
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- COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE
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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
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Page/Page column 19
(2016/10/11)
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- PHARMACEUTICAL COMBINATIONS
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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.
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Page/Page column 52
(2016/10/11)
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- 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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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.
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Page/Page column 24; 25
(2016/10/11)
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- Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
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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.
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Paragraph 0568; 0569
(2015/05/05)
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- RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS
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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.
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Page/Page column 78
(2015/05/06)
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- PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.
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Page/Page column 37
(2012/01/13)
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- Prokineticin 1 receptor antagonists
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The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
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Page/Page column 37-38
(2008/12/04)
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- PROKINETICIN 2 RECEPTOR ANTAGONISTS
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The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.
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Page/Page column 102
(2010/11/28)
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- An efficient synthesis of an alphavbeta3 antagonist.
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A practical preparation of an alpha(v)beta(3) antagonist is reported. The antagonist consists of three key components, a tetrahydronaphthyridine moiety, a beta-alanine moiety, and a central imidazolidone moiety. The tetrahydronaphthyridine component was p
- Yasuda, Nobuyoshi,Hsiao,Jensen, Mark S,Rivera, Nelo R,Yang, Chunhua,Wells, Kenneth M,Yau, James,Palucki, Michael,Tan, Lushi,Dormer, Peter G,Volante, Ralph P,Hughes, David L,Reider, Paul J
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p. 1959 - 1966
(2007/10/03)
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- 1-(Aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
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Certain 1-(aromatic- or heteroaromatic-substituted-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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