- Oral liquid containing naphthyridine compound and preparation method thereof
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The invention relates to the field of medicines, in particular to oral liquid containing naphthyridine compounds and a preparation method of the oral liquid. Every 100 mL of the oral liquid containing the naphthyridine compound is prepared from the following raw materials: 40 to 70 g of pharmaceutically acceptable salt of 5-((3-fluoro-4-((7-(2-hydroxy-2-methylpropyl) quinoline-4-yl) oxo) phenyl) amino)-3-(4-fluorophenyl)-1, 6-naphthyridine-4 (1H)-ketone, 5 to 10 g of stabilizer and 0.3 to 6 g of solubilizer. A pH regulator is used for regulating the pH value to 5.5-6.2; according to the oral liquid containing the naphthyridine compounds, the pH value of the oral liquid containing the naphthyridine compounds is adjusted to 5.5-6.2, and the dosage of each raw material is limited, so that the stability of the oral liquid containing the naphthyridine compounds can be remarkably improved.
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Paragraph 0028; 0031
(2021/10/27)
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- Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate
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A series of 1,6-naphthyridinone-based MET kinase inhibitors bearing quinoline moiety in block A were designed and synthesized based on the structures of Cabozantinib and our reported compound IV. Extensive SAR and DMPK studies led to the identification of 20j, a potent and orally bioavailable MET kinase inhibitor with favorable kinase selectivity. More importantly, 20j exhibited statistically significant tumor growth inhibition (Tumor growth inhibition/TGI of 131%, 4/6 partial regression/PR) in the U-87 MG xeograft model, which is superior to that of Cabozantinib (TGI of 97%, 2/6 PR), and significantly better than that of compound IV (TGI of 15%, 0/6 PR) at the same dose (12.5 mg/kg). Combined with favorable in vitro potency, kinase selectivity, pharmacokinetic profile and in vivo efficacy, the promising antitumor drug candidate 20j has subsequently advanced into preclinical research.
- Chen, Tao,Fang, Wei-Rong,Huang, Wei,Li, Yun-Man,Liu, Peng-Fei,Zhuo, Lin-Sheng
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- Naphthyridine compound and pharmaceutical composition as well as applications thereof
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The invention relates to the field of biological medicines and discloses a naphthyridine compound and a pharmaceutical composition as well as applications thereof. The naphthyridine compound has a structure shown in a formula (I) or a stereisomer, a geometric isomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, a pharmaceutically acceptable salt or a prodrug. The naphthyridine compound disclosed by the invention has an anti-tumor effect which is obviously superior to the anti-tumor effect of the prior art. And moreover, the naphthyridine compound disclosed by the invention can treat diseases mediated by protein kinase.
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Paragraph 0116; 0117; 0122; 0123
(2017/08/02)
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- SUBSTITUTED QUINOLINE COMPOUNDS AND METHODS OF USE
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The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Page/Page column 21
(2012/09/10)
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