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New application of substituted piperazinylphenylisoxazoline derivatives in the preparation of antitumor drugs

A piperazinyl and isoxazole-based technology, applied in the field of tumor-related drugs, can solve problems such as toxic side effects, new uses of anti-tumor drugs not involved, poor selectivity, etc.

Inactive Publication Date: 2011-12-07
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Tumor is a common disease that threatens human life. According to statistics, the total number of cancer deaths in the world reaches 7 million people every year. In my country, more than 1 million people die from tumors every year, and gradually increase. It has become the first cause of death of urban population. Traditional chemotherapy The clinical therapeutic effect of the drug is obvious, but the disadvantages are: low specificity and poor selectivity, leading to obvious toxic and side effects, prone to serious multi-drug resistance of tumors, and limiting clinical application. Finding safe and effective anti-tumor drugs has always been a challenge. The pursuit of goals in the pharmaceutical industry
[0003] The substituted piperazinyl phenyl isoxazoline derivatives described in the Chinese patent application (Application No.: 200610130717.3) submitted by the applicant on December 30, 2006 disclose compounds of the general formula, their preparation methods, containing them The pharmaceutical composition and the use of preparing antibacterial drugs, the application specification does not involve the new use of these substances in the preparation of antitumor drugs

Method used

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  • New application of substituted piperazinylphenylisoxazoline derivatives in the preparation of antitumor drugs
  • New application of substituted piperazinylphenylisoxazoline derivatives in the preparation of antitumor drugs
  • New application of substituted piperazinylphenylisoxazoline derivatives in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Tablets 100 pieces

[0099] I-1 10.0g

[0100] Lactose 13.0g

[0101] Pregelatinized starch 3.5g

[0102] Microcrystalline Cellulose 2.5g

[0103] Carboxymethyl starch sodium 0.8g

[0104] 10% povidone solution QS

[0105] Magnesium stearate QS

[0106] Talc QS

[0107] Preparation process: The active ingredients and auxiliary materials are pre-grinded and sieved to 100 mesh, the main drug plus auxiliary materials lactose, pregelatinized starch carboxymethyl starch sodium, and microcrystalline cellulose are fully mixed, passed through a 60-mesh sieve three times, and povidone is added Solution, mixing, making soft material, passing through 20 mesh sieve, making wet granules, drying at 50-60°C, adding magnesium stearate and talcum powder to pre-screen, then adding to the above granules and mixing thoroughly, measuring the middle Body granules, compressed into tablets.

Embodiment 2

[0109] Capsules 100 capsules

[0110] I-3 98.0g

[0111] Silica 1.8g

[0112] Magnesium stearate QS

[0113] Preparation process: crush the active ingredient through a 100-mesh sieve, add auxiliary materials such as silicon dioxide and magnesium stearate, mix evenly, measure the content of intermediates, and fill it into No. 4 capsules.

Embodiment 3

[0115] Dispersible Tablets 100 Tablets

[0116] I-4 15.0g

[0117] Lactose 20.0g

[0118] Microcrystalline Cellulose 5.0g

[0119] Crospovidone 2.0g

[0120] Aspartame 0.1g

[0121] Orange flavor 0.1g

[0122] 2% Hypromellose QS

[0123] Silica QS

[0124] Magnesium stearate QS

[0125] Preparation process: sieve the active ingredient plus excipients lactose, partially cross-linked povidone, microcrystalline cellulose, aspartame and orange flavor and mix well, add 2% hypromellose solution, mix, and make soft material , through a 24-mesh sieve, make wet granules, dry at 50-60°C, and granulate with a 20-mesh sieve. After sieving the remaining crospovidone, magnesium stearate and talcum powder, add them to the above granules and mix thoroughly, measure the intermediate granules, and compress into tablets.

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Abstract

The present invention relates to the field of anti-tumor related medicines, in particular, the present invention relates to a new method for the preparation of anti-tumor drugs by the pharmaceutical composition of substituted piperazinyl phenyl isoxazoline derivatives as described in Chinese patent application (CN200610130717). use.

Description

technical field [0001] The invention belongs to the field of tumor-related drugs, and more specifically relates to a new application of a substituted piperazinyl phenyl isoxazoline derivative in the preparation of anti-tumor drugs. Background technique [0002] Tumor is a common disease that threatens human life. According to statistics, the total number of cancer deaths in the world reaches 7 million people every year. In my country, more than 1 million people die from tumors every year, and gradually increase. It has become the first cause of death of urban population. Traditional chemotherapy The clinical therapeutic effect of the drug is obvious, but the disadvantages are: low specificity and poor selectivity, leading to obvious toxic and side effects, prone to serious multi-drug resistance of tumors, and limiting clinical application. Finding safe and effective anti-tumor drugs has always been a challenge. The pursuit of the goal of the pharmaceutical industry. [0003] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61P35/00
Inventor 刘巍刘默刘登科徐为人刘颖任晓文王玉丽张士俊汤立达王景阳
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH