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Quinoline for treating cholangiocarcinoma

A technology for cholangiocarcinoma and intrahepatic cholangiocarcinoma, applied in the field of medicine, which can solve the problems of lack of conclusive evidence of effectiveness

Pending Publication Date: 2019-10-18
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Local therapy for intrahepatic cholangiocarcinoma, but firm evidence of efficacy lacks

Method used

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  • Quinoline for treating cholangiocarcinoma
  • Quinoline for treating cholangiocarcinoma
  • Quinoline for treating cholangiocarcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine di Hydrochloride

[0054]

Embodiment 2

[0057] 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine di The preparation of the capsule of hydrochloride (embodiment 1 compound)

[0058]

[0059] The compound of Example 1 was pulverized and passed through a 80-mesh sieve; then mixed evenly with mannitol and hydroxypropyl cellulose; then added the prescribed amount of microcrystalline cellulose, mixed evenly, and passed through a 0.8mm sieve; finally added the prescribed amount of stearin Magnesium acid is mixed well and filled into capsules.

[0060] Capsules with other contents of the dihydrochloride of Compound I can be prepared with reference to the same ratio and prescription as above.

Embodiment 3

[0062] cell experiment

[0063] With the compound of Example 1 as the test drug, the present invention is used to measure the proliferation inhibition test of the human cholangiocarcinoma cell line huh28 by the CKK-8 (Cell Counting Kit-8) method: the cell suspension digested with trypsin is used in a volume of 100 μL per hole 3,000 cells were inoculated in each well of a 96-well plate, and the edges were cleaned with sterile PBS. After 24 hours of attachment, the culture medium (RMPI 1640 medium) was replaced, and 100 μL of culture medium with gradient concentrations of drugs was added to each well. Concentrations, respectively: 0, 2, 4, 6, 8, 10μM. Placed at 37°C, 5% CO 2 cultured in an incubator. Cell viability was measured with CCK-8 every 24 hours after drug addition, that is, CCK-8 diluted 1:10 was added, incubated at 37°C for 2 hours, and finally the optical density value of each well was detected with an automatic microplate reader at a wavelength of 450 nm. Accordin...

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PUM

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Abstract

The invention provides quinoline for treating cholangiocarcinoma, and an application thereof to preparation of a medical composition for treating tumors, and particularly relates to an application ofquinoline derivative 1-[[[4-(4-fluoro-2-methyl-1H-indole -5-)oxy-6-methoxyquinolin-7-yl]oxy]methyl cyclopropylamine to treatment cholangiocarcinoma: as shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the use of quinoline derivatives in the preparation of medicines or pharmaceutical compositions for treating cholangiocarcinoma. Background technique [0002] Cholangiocarcinoma is a kind of malignant tumor originating from epithelial cells. Medically, cholangiocarcinoma can be divided into: Perihilar cholangiocarcinoma (PHA), distal cholangiocarcinoma (DCCA) and intrahepatic cholangiocarcinoma according to the different anatomical locations. Cholangiocarcinoma (intrahepatic cholangiocarcinoma, ICCA), hilar cholangiocarcinoma is the most common. [0003] Nataliya et al pointed out in Lancet.Jun 21, 2014; 383(9935):2168–2179 that all subtypes of cholangiocarcinoma are the first choice for surgical treatment, but if noticed, it is also necessary to consider whether the tumor has invaded blood vessels and lymph nodes, bile ducts The cancer's highly pro-proliferative cap...

Claims

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Application Information

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IPC IPC(8): A61K31/4709A61P35/00
CPCA61K31/4709A61P35/00
Inventor 杨玲王善春张喜全徐宏江陆萌英杜桂芳董政陆莹董金珂王训强江海杨朝强张弛
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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