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Application of substituted aryl hydrazone compound serving as anti-tumor necrosis factor inhibitor medicament

A technology of aromatic hydrazone and necrosis factor, which is used in antitumor drugs, drug combinations, pharmaceutical formulations, etc.

Active Publication Date: 2010-07-07
INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Before the present invention, there were no related reports and patent applications of aryl hydrazone compounds as inhibitors that directly combined with TNF-β and TNF-a and inhibited the biological activity of TNF-β and TNF-a

Method used

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  • Application of substituted aryl hydrazone compound serving as anti-tumor necrosis factor inhibitor medicament
  • Application of substituted aryl hydrazone compound serving as anti-tumor necrosis factor inhibitor medicament
  • Application of substituted aryl hydrazone compound serving as anti-tumor necrosis factor inhibitor medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Preparation of tablets each containing 100 mg of active ingredient:

[0116] mg / tablet

[0117] C-12 100

[0118] Lactose 50

[0119] Microcrystalline Cellulose 80

[0120] Starch 50

[0121] Hydroxymethylcellulose 40

[0122] Magnesium Stearate 5

[0123] Pass the active ingredients, lactose, starch, and microcrystalline cellulose through a 100-mesh sieve, and mix thoroughly, add 2% carboxymethylcellulose aqueous solution to the above mixed powder and mix, pass through a 20-mesh sieve to make a soft material, and obtain wet granules Dry at 45-55°C, add sodium carboxymethyl starch and magnesium stearate to the above-mentioned dry granules and press into tablets.

Embodiment 2

[0125] Capsules containing 100 mg of active ingredient per capsule are prepared as follows:

[0126] Dosage / Capsule Weight Concentration (%)

[0127] C-12 100mg 30.0

[0128] Polyoxyethylene sorrel 0.05mg 0.02

[0129] Sugar Alcohol Monooleate

[0130] Starch 250mg 69.98

[0131] Total 350.05mg 100.00

Embodiment 3

[0133] Preparation of Injections

[0134] C-12 200mg

[0135] Mannitol 700mg

[0136] PEG3000 10mg

[0137] Distilled water 100ml

[0138] Make the pH value 7.0-7.5 and filter the filtrate concentration to be 3 mg / ml, divide into 2 ml per ampoule, freeze-dry to obtain the injection.

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Abstract

The invention relates to clinical application of a substituted aryl hydrazone compound and a derivative thereof serving as an anti-tumor necrosis factor inhibitor. A test result shows that the compound has a lower cytotoxicity in animal bodies, so the medical compound is expected to be used as an anti-TNF-alpha and TNF-beta inhibitor in the clinical application and is mainly used for treating some TNF related immunological diseases such as rheumatic arthritis, inflammatory bowel diseases, diabetes, hematosepsis, psoriasis, ankylosing spondylitis and some communicable diseases including HIV. A current TNF related research also shows that the medical compound can be used for treating clinical blood and solid tumor such as myelodysplastic syndrome, myelofibrosis, acute bone marrow cell leucocythemia, acute / chronic graft-versus-host reaction, ovarian cancer, nephrocyte cancer and the like.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and relates to the clinical application of substituted aryl hydrazone compounds, derivatives and salts thereof as anti-tumor necrosis factor (tumor necrosis factor, TNF) TNF-a and TNF-beta inhibitors. Background technique [0002] The immune system is the most important defense system in the human body. A normal immune response endows the human body with the ability to resist infection, identify self and non-self, and remove aging and diseased cells in the body in time. However, abnormal immune response also has the possibility of causing disease, that is, the transformation of physiological response to pathological response. Studies have shown that the body can release a large number of inflammatory factors, such as interleukin 1, interleukin 6, tumor necrosis factor, etc., during the process of immune response to antigens, which can damage local tissues and organs. Common clinical rheum...

Claims

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Application Information

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IPC IPC(8): A61K31/427A61K31/415A61P35/00
Inventor 许元富谷岳纪庆郭红星熊冬生杨纯正
Owner INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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