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New uses of acyl chloride and sulfonyl chloride derivatives in preparing anti-tumor drug

A use and pharmaceutical technology, applied in the field of preparation of antitumor drugs by acid chlorides and sulfonyl chloride isoxazoline derivatives, can solve the problems of new uses of antitumor drugs, lack of effective drugs, low selectivity, etc.

Inactive Publication Date: 2010-03-24
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional chemotherapy drugs are mainly cytotoxic drugs. In recent years, the research and development of anti-tumor drugs has made great progress. Many drugs with different mechanisms of action are emerging, but there are still some problems: for example, solid tumors that account for 90% of tumors There is still a lack of effective drugs; the existing anti-tumor drugs have large toxic and side effects, low selectivity and easy drug resistance, etc.
[0003] The acyl chloride and sulfonyl chloride derivatives described in the Chinese patent application (Application No.: 200710060530.5) disclose compounds of the general formula, their preparation methods, pharmaceutical compositions containing them, and the use of preparing antibacterial drugs. The new application of these substances in the preparation of antitumor drugs

Method used

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  • New uses of acyl chloride and sulfonyl chloride derivatives in preparing anti-tumor drug
  • New uses of acyl chloride and sulfonyl chloride derivatives in preparing anti-tumor drug
  • New uses of acyl chloride and sulfonyl chloride derivatives in preparing anti-tumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Tablets 100 pieces

[0057] I-1 5.0g

[0058] Lactose 15.0g

[0059] Pregelatinized starch 2.5g

[0060] Microcrystalline Cellulose 3.5g

[0061] Carboxymethyl starch sodium 0.8g

[0062] 10% povidone solution QS

[0063] Magnesium stearate QS

[0064] Talc QS

[0065] 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

[0067] Capsules 100 capsules

[0068] I-2 99.0g

[0069] Silica 1.0g

[0070] Magnesium stearate QS

[0071] 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 in No. 4 capsules.

Embodiment 3

[0073] Dispersible Tablets 100 Tablets

[0074] I-3 20.0g

[0075] Lactose 20.0g

[0076] Microcrystalline Cellulose 5.0g

[0077] Crospovidone 2.0g

[0078] Aspartame 0.2g

[0079] Orange essence 0.2g

[0080] 2% Hypromellose QS

[0081] Silica QS

[0082] Magnesium stearate QS

[0083] Preparation process: sieve the active ingredient plus excipients lactose, partially cross-linked povidone, microcrystalline cellulose, aspartame and orange essence, mix well, add 2% hypromellose solution, mix, and make a 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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PUM

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Abstract

The invention relates to new medical uses of acyl chloride and sulfonyl chloride derivatives having a general formula I structure described in the Chinese patent application (CN 200710060530.5) in aspect of anti-tumor, especially new uses of this type compounds and pharmaceutically acceptable salts or medicinal compositions thereof in preparing anti-tumor drugs. Specifically speaking, the presentinvention relates to application in treating colorectal carcinoma, leukemia, gastric adenocarcinoma, breast cancer, oral cancer, lung cancer, sarcoma and melanoma. Wherein, the definition of each group is described as the specification.

Description

technical field [0001] The invention belongs to the field of tumor-related drugs, and more specifically relates to a new application of a class of acid chloride and sulfonyl chloride isoxazoline derivatives in the preparation of antitumor drugs. Background technique [0002] Tumor is a malignant disease that seriously endangers human health, and its mortality rate is second only to cardiovascular disease, ranking second in the mortality rate of various diseases. Since 1996, more than 10.3 million cancer patients have been newly diagnosed every year in the world, and the total number of cancer deaths in the world has reached 7 million people every year. WHO reported in 2001 that the incidence and mortality of cancer in the world increased by 22% compared with 1990, and will increase by about 50% in the next 20 years. The most common cancers in western developed countries are breast cancer, lung cancer, prostate cancer, colon cancer, rectal cancer and ovarian cancer. In rece...

Claims

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Application Information

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Patent Type & Authority Applications(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
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