Unlock instant, AI-driven research and patent intelligence for your innovation.

Cabazitaxel acetic acid compound and crystal thereof

A technology of cabazitaxel and acetic acid compound, applied in the field of crystallization, can solve the problems that the solvate is not stable enough, the preparation method is complicated, and the industrialization cost is high, and the invention is suitable for industrial-scale preparation, the preparation process is simple, and the stability is good. Effect

Active Publication Date: 2014-07-09
SHANGHAI INST OF PHARMA IND CO LTD +1
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the applicant found that the cabazitaxel and its solvates disclosed in the prior art are not stable enough, and the preparation method is complicated, and the industrialization cost is high. In addition, some of the above solvates have certain toxicity, which is harmful to medicines. Words are not the best choice

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cabazitaxel acetic acid compound and crystal thereof
  • Cabazitaxel acetic acid compound and crystal thereof
  • Cabazitaxel acetic acid compound and crystal thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Cabazitaxel (2 g) was dissolved in 20 ml of acetic acid, and 30 ml of purified water was added dropwise with stirring at room temperature, a solid was precipitated, stirred for 1 h, filtered with suction, the solid was washed with purified water, and dried in vacuum (40°C) for about 3 hours to obtain 1.9 g white solid. The mass percentage of acetic acid in the product was determined by gas chromatography to be 4.85%.

Embodiment 2

[0037] Cabazitaxel (2 g) was dissolved in 10 ml of acetic acid, 15 ml of purified water was added dropwise with stirring at room temperature, a solid was precipitated, stirred for 1 h, filtered with suction, the solid was washed with purified water, and dried in vacuum (40°C) for about 3 hours to obtain 1.92 g white solid. The mass percentage of acetic acid in the product was determined by gas chromatography to be 2.87%.

Embodiment 3

[0039] Cabazitaxel (2 g) was dissolved in 30 ml of acetic acid, and 45 ml of purified water was added dropwise with stirring at room temperature, a solid was precipitated, stirred for 1 h, filtered with suction, the solid was washed with purified water, and dried in vacuum (40°C) for about 3 hours to obtain 1.85 g white solid. The mass percentage of acetic acid in the product was determined by gas chromatography to be 3.95%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
wavelengthaaaaaaaaaa
Login to View More

Abstract

The invention relates to a cabazitaxel acetic acid compound and a crystal thereof, and specifically, relates to the cabazitaxel acetic acid compound and the crystal thereof, methods for preparing the cabazitaxel acetic acid compound and the crystal thereof, pharmaceutical compositions containing the cabazitaxel acetic acid compound and the crystal thereof, and an application of the cabazitaxel acetic acid compound and the crystal thereof and the pharmaceutical compositions in preparing antitumor drugs. The cabazitaxel acetic acid compound and the crystal thereof have the advantages of being excellent in physicochemical properties, good in stability, simple in preparation technology, more suitable for industrialized scale preparation and the like.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the acetic acid compound of the anti-malignant tumor compound cabazitaxel, and also relates to its crystallization. technical background [0002] Taxane compounds have strong anti-tumor activity, and such compounds are currently on the market, such as paclitaxel, docetaxel and cabazitaxel, etc., which have good inhibitory activity on various solid tumor cells. Among them, cabazitaxel, namely 4-acetoxy-2α-benzoyloxy-5β, 20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxotaxane-11 -en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxyl-3-phenylpropionate (structure shown in the following formula), developed and marketed by Sanofi, France Taxane anti-tumor drugs, the drug has better curative effect on patients with advanced prostate cancer. Compared with other anti-tumor drugs, this drug can significantly improve the vitality of patients with advanced prostate cancer and prolong the life...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14A61K31/337A61P35/00A61P13/08
CPCC07D305/14
Inventor 袁哲东杨玉雷朱雪焱程兴栋张爱明孙键
Owner SHANGHAI INST OF PHARMA IND CO LTD