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Water-soluble cabazitaxel anticancer medicine compounds, preparing method thereof and applications of the compounds

A cabazitaxel and anticancer drug technology, which is applied to the water-soluble cabazitaxel anticancer drug compound and the fields of preparation and application thereof, can solve the problems of no selective recognition effect, adverse reactions and the like, and achieves good water solubility and high Anticancer activity, enhances the effect of Kabbah

Active Publication Date: 2017-04-05
NANJING YOUYI MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Cabazitaxel has high anti-tumor activity, good safety and tolerance, and its clinical application has become more and more extensive since it was launched on the market. However, like other anti-tumor drugs, it has no selective recognition effect on tumor cells and normal cells, which makes its side effects The performance is also particularly prominent, and the reports on its adverse reactions are gradually increasing. The main adverse reactions found so far are common adverse reactions in clinical trials, including neutropenia, anemia, leukopenia, thrombocytopenia, diarrhea, fatigue, nausea, Vomiting, constipation, and kidney failure
Therefore, it cannot be used to treat neutrophil counts less than 1500mm 3 and patients with a history of severe hypersensitivity to Jevtana or Sorbitol 80

Method used

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  • Water-soluble cabazitaxel anticancer medicine compounds, preparing method thereof and applications of the compounds
  • Water-soluble cabazitaxel anticancer medicine compounds, preparing method thereof and applications of the compounds
  • Water-soluble cabazitaxel anticancer medicine compounds, preparing method thereof and applications of the compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1. Synthesis of polyethylene glycol monomethyl ether (Mn=1000) cabazitaxel-2'-diglycolate

[0052] The synthesis of the water-soluble cabazitaxel anticancer drug compound comprises the following steps:

[0053] 1) Synthesis of Polyethylene Glycol Monomethyl Ether (Mn=1000) Diglycolate

[0054] method one:

[0055] The reaction formula is as follows:

[0056]

[0057] Experimental steps:

[0058] In a 100mL round bottom flask, add 2.400g (2.4mmol) of dried polyethylene glycol monomethyl ether (Mn=1000), 0.557g (4mmol) of diglycolic anhydride and 200mg of 2-ethylhexanoic acid tin (II ), then add 30mL dimethylbenzene, stir, and under nitrogen protection, heat and reflux until the reaction is complete, follow the reaction process with thin-layer chromatography (developing agent is: 1,4-dioxane:DMF (volume ratio)=6:1 ). After removing the xylene in the reaction solution with a rotary evaporator, add 20 mL of ethyl acetate, stir, then add 10 mL of diethyl e...

Embodiment 2

[0068] Example 2. Preparation of water-soluble cabazitaxel anticancer drug compound (XBB-022)

[0069] Include the injection that water, normal saline (0.9% sodium chloride), 5% glucose injection are made among the present embodiment, contain the water-soluble cabazitaxel anticancer drug compound of the present invention in the preparation formula, each component is in The content in the formula is calculated by weight percentage.

[0070] A. Deionized Water Injection of Water-Soluble Cabazitaxel Anticancer Drug Compound

[0071] Add 100mg of water-soluble cabazitaxel anticancer drug compound (XBB-022) into a 10mL volumetric flask, dilute it to 10mL with deionized water, and shake the composition of the produced injection as follows:

[0072] XBB-022 1.0%

[0073] Deionized water 99.0%.

[0074] The prepared injection was filtered through a 0.2 micron filter and filled into sterile glass vials.

[0075] B. Saline Injection of Water-Soluble Cabazitaxel Anticancer Drug Compo...

Embodiment 3

[0085] Example 3. Determination of Water-Soluble Cabazitaxel Anticancer Drug Compound (XBB-022) Micelle Particle Size

[0086] XBB-022 dissolves in water to form micelles. The particle size of the micelles is measured by a ZetaPlus laser scattering particle size analyzer from BROOKHAVEN, USA. The measurement method is: weigh 5 mg of the drug (XBB-022), add it to 2 mL of distilled water, and stir Make it fully dissolved, let it stand for 10 minutes, and add the liquid into the sample cell (cuvette) after the bubbles disappear, pay attention to the fact that no bubbles are generated during adding the sample, and then put the cuvette into the corresponding groove of the base of the sample cell Within, the measurement is started, and the sample is measured in parallel three times to obtain the average value.

[0087] See the experimental results image 3 . The results showed that: when the concentration of XBB-022 aqueous solution was 2.5 mg / mL, its average particle size was 129...

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Abstract

Water-soluble cabazitaxel anticancer medicine compounds are disclosed and have structures shown as a following formula I. Cabazitaxel and polyethylene glycol monoalkyl ether which are anticancer medicine active parts are covalently bonded through a connecting group that is diglycoloyl (carbonyl methoxy acetyl) to form the compounds. The invention also relates to a preparing method and an application of the compounds, wherein R is -CH3, -CH2CH3, -CH2CH2CH3 and -CH2CH2CH2CH3 and n is 5-500.

Description

technical field [0001] The present invention relates to a new anticancer drug compound and its preparation method and application, in particular to a water-soluble cabazitaxel anticancer drug compound, including the preparation method, preparation and application of the compound as an anticancer drug. Background technique [0002] Many compounds with anticancer activity have been an obstacle to drug development due to insolubility or poor stability in water and / or other biocompatible solvents, often leading to delays in drug development time. It is estimated that as many as 40 percent of screened potentially valuable drug candidates are rejected from formulation research and development due to their poor water solubility, and 30 percent of existing drugs are poorly soluble. Several technologies are currently being researched and developed to address the poor solubility of pharmaceutical compounds, including complexing agent technology to increase solubility, nanoparticle tec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K31/785A61P35/00
Inventor 张跃华
Owner NANJING YOUYI MEDICAL TECH CO LTD