Substituted aromatic radical biguanide compounds and the application of their medicine composition in preparing medicine for resisting malignant tumors

A technology of malignant tumors and compounds, applied in the direction of drug combinations, antineoplastic drugs, medical preparations containing active ingredients, etc., can solve problems that have not been studied

Inactive Publication Date: 2006-10-18
INST OF HEMATOLOGY & BLOOD HOSPITAL CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its application in anti-tumor, especially the inhibition of tumor invasion, metastasis and angiogenesis has not been studied.

Method used

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  • Substituted aromatic radical biguanide compounds and the application of their medicine composition in preparing medicine for resisting malignant tumors
  • Substituted aromatic radical biguanide compounds and the application of their medicine composition in preparing medicine for resisting malignant tumors
  • Substituted aromatic radical biguanide compounds and the application of their medicine composition in preparing medicine for resisting malignant tumors

Examples

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Embodiment Construction

[0091] In order to more fully illustrate the practice of the present invention, the following formulation examples are provided. These examples are merely illustrative, not limiting the scope of the present invention. Formulations may employ the active ingredient of any of the compounds of the present invention.

[0092] Preparation 1

[0093] Tablets each containing 10 mg of active ingredient are prepared as follows:

[0094] Dosage / tablet Weight concentration (%)

[0095] Compound (2) 100mg 10.0

[0096] Microcrystalline Cellulose 35mg 35.0

[0097] Starch 45mg 45.0

[0098] Polyvinylpyrrolidone 4mg 4.0

[0099] Carboxymethyl starch sodium salt 4.5mg 4.5

[0100] Magnesium stearate 0.5mg 0.5

[0101] Talc 1mg 1.0

[0102] Total 100 100.0

[0103] Sieve the active ingredients, starch and cellulose, and mix them well, mix the polyvinylpyrrolidone solution with the above powder, sieve, make wet granules and dry at 50-60°C, add carbox...

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Abstract

The present invention relates to substituted aromatic radical biguanide compounds and the application of their medicine composition in preparing medicine for treating malignant tumors. The substituted aromatic radical biguanide compounds possess, extracorporeal and intracorporeal experiments shows, obvious tumor cell inhibiting effect and the features of high efficiency and low toxicity, so that the medicine compounds are expected to be applied in inhibiting tumor attack and metastasis, inhibiting angiogenesis, and treating human melanoma, glioma, lung cancer and other malignant tumors with high expression of integrin.

Description

technical field [0001] The present invention relates to a method for treating malignant tumors with a series of substituted aryl biguanide compounds, more specifically a substituted aryl biguanide compound with antitumor activity and a pharmaceutical composition containing a therapeutically effective amount of such compounds in Inhibition of tumor invasion and metastasis and angiogenesis, as well as the treatment of human melanoma, glioma, lung cancer, gastric cancer, prostate cancer, ovarian cancer and other malignant tumors with high expression of integrin αvβ3. Background technique [0002] Malignant tumors are a large class of diseases that seriously threaten human health. Their abnormal proliferation is controlled by abnormal information in cells and is closely related to the abnormal activity and inactivation of corresponding genes in tumor cells. Traditional anticancer drugs are mainly cytotoxic drugs, which rely on the differences in the kinetics of growth, repair, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155A61P35/00
Inventor 彭晖周圆黄牛纪庆齐静肖瑛杨纯正
Owner INST OF HEMATOLOGY & BLOOD HOSPITAL CHINESE ACAD OF MEDICAL SCI
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