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Quinoline and application thereof

A derivative, quinoline technology, applied in the field of quinoline derivatives and its application, can solve the problems of affecting physiological functions, failing to achieve specificity, side effects, etc.

Inactive Publication Date: 2015-04-22
华国媛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current clinical anti-cancer drugs still cannot achieve a satisfactory level of specificity. When patients undergo chemotherapy, normal cells in the body are often poisoned, which seriously affects physiological functions and produces many side effects

Method used

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  • Quinoline and application thereof
  • Quinoline and application thereof
  • Quinoline and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0050] [Compound analysis method]

[0051] The melting point of the compound was measured with an Electrothermal IA9100 melting point analyzer (purchased from Clarkson Laboratory). Nuclear magnetic resonance (NMR) spectroscopy ( 1 H and 13 C) Measure and record with Varian Gemini 200 spectrometer or Varian-Unity-400 spectrometer (purchased from Varian Company). Chemical shifts are expressed in "δ" and tetramethylsilane (TMS) was used as an internal standard. Thin-layer chromatography was performed on a silica gel 60F-254 plate (purchased from E. Merck and Co.). Elemental analysis was performed using the Instrument Center of the National Science Committee of the Executive Yuan at National Cheng Kung University and the Heraeus CHN-O Rapid elemental analyzer (purchased from Heraeus) of Chung Hsing University, Taiwan. All values ​​were within ±0.4% of theoretical composition (theoretical composition) Inside.

preparation example

[0053] The compound of the present invention is prepared by the method shown in the following flow chart, and the preparation method of the compound will be described in detail below:

[0054]

[0055] A. Preparation of 1-(4-aminophenyl)-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound 3) or 1-(4- Amino-2-fluorophenyl)-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound 4)

[0056] With 0.69 g (2 mmol) of 6,7-difluoro-1-(4-nitrophenyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound 1 ) or 6,7-difluoro-1-(2-fluoro-4-nitrophenyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound 2) dissolved in di Chloromethane (100 milliliters) (the preparation method of compound 1 and 2 can refer to Chen et al., J.Med.Chem., 2001, 44, 2374-2377, and this document is quoted here for reference), at normal temperature Hydrogenation was carried out with palladium on carbon (0.23 g) under pressure and hydrogen over 4 hours (monitored by TLC). Th...

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Abstract

The invention provides a quinoline (I), wherein R1 is substituted or unsubstituted phenyl; R2 is halogen; and R3 is substituted or unsubstituted phenyl, or substituted or unsubstituted phenyl of which a benzene ring includes N heteroatom. According to the quinoline, the cancer cell proliferation can be effectively restrained, so that the quinoline can be used for treating cancer, and particularly can be used for treating the cancer related with the Janus kinase-transcription information converter and the activator (JAK-STAT) ways and / or the mitogen-activated protein kinase (MAPK) way.

Description

technical field [0001] The present invention relates to a quinoline derivative and its application, in particular to a quinoline derivative which can be used for cancer treatment and its application. Background technique [0002] Cancer can occur in various organs and tissues at any age and is responsible for approximately six million deaths worldwide each year. All cancer types begin with abnormal and uncontrolled growth of cells, and the course consists of abnormal or neoplastic cells forming and multiplying tumors, which then invade adjacent tissues and spread via the blood or lymphatic system to regional lymph nodes, eventually via The metastatic process spreads to distant places in the body. The etiology of cancer is still unclear, but known factors such as heredity, chromosomal breaks, viruses, environment and immune diseases are all related to the growth and metastasis of tumor cells. [0003] Regarding cancer treatment, various treatment methods have been developed...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/56C07D401/12A61K31/4709A61K31/47A61P35/00A61P1/00A61P15/14
Inventor 华国媛李玉梅陈义龙曾诚齐卓心媛
Owner 华国媛