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Compound and new usage of composition thereof

A compound and composition technology, applied in the field of pharmacy, can solve problems such as increasing white blood cells

Active Publication Date: 2009-06-03
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, there is still a lack of clinically significant, inexpensive, and easy-to-use drugs for increasing leukocytes in this field.

Method used

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  • Compound and new usage of composition thereof
  • Compound and new usage of composition thereof
  • Compound and new usage of composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Synthetic routes of three genistein compounds

[0122]

[0123] Genistein analog 1 (AG-1, formula III)

[0124] The preparation method of formula III compound:

[0125] 1. In a 50ml round-bottomed three-neck flask treated with anhydrous and oxygen-free treatment, under nitrogen protection, add 25ml of newly distilled boron trifluoride ether, resorcinol (5mmol) and p-hydroxyphenylacetic acid (5mmol), oil Heating the bath to 60-90°C, stirring electromagnetically, and reacting for 8-10 hours, then cooling to room temperature;

[0126] 2. Add 8ml of anhydrous N, N-dimethylformamide, reheat to 50°C, slowly add a mixture of 1.2ml methanesulfonyl chloride and 2ml N, N-dimethylformamide, and continue heating to 60-70 ℃, react for 8-10 hours, and cool to room temperature;

[0127] 3. Pour the reaction product in batches into 100-200 ml of cooled 10% sodium acetate aqueous solution, filter, collect the solid crude product, and obtain the pure product (compound of formula II...

Embodiment 2

[0141] Therapeutic effect of genistein compounds on cyclophosphamide-induced leukopenia in mice

[0142] Experimental animals:

[0143] Eighty male SPF grade C57 BL / 6 mice were purchased from Shanghai Slack Experimental Animal Co., Ltd., weighing 22-24 g. Animals were housed in an SPF-grade animal room with 12 hours of light / 12 hours of darkness and free access to feed and water.

[0144] Experimental Drugs:

[0145]Genistein (compound of formula II), with a purity of 98%, was purchased from Nanjing Qingze Pharmaceutical Technology Development Co., Ltd.; AG-1, AG-2, and AG-3 (prepared in Example 1); Produced by Bell Pharmaceutical Co., Ltd.; Cyclophosphamide for Injection, produced by Jiangsu Hengrui Pharmaceutical Co., Ltd.

[0146] experimental method:

[0147] 1. Modeling method:

[0148] The animals were randomly divided into 8 groups. Except for the normal control group, the mice in the other groups were given intraperitoneal injection of cyclophosphamide 100 mg / kg, ...

Embodiment 3

[0166] Therapeutic effect of apigenin on cyclophosphamide-induced leukopenia in mice

[0167] Experimental animals: 60 male SPF grade C57BL / 6 mice, purchased from Shanghai Slack Experimental Animal Co., Ltd., weighing 18-22 g. Animals were housed in an SPF-grade animal room with 12 hours of light / 12 hours of darkness and free access to feed and water.

[0168] Experimental drugs: apigenin (compound of formula VI), with a purity of 98%, was purchased from Nanjing Qingze Pharmaceutical Technology Development Co., Ltd.; batyl alcohol was produced by Jiangsu Pengyao Pharmaceutical Co., Ltd.; cyclophosphamide for injection was purchased from Jiangsu Hengrui Medicine Co., Ltd. production.

[0169] experimental method:

[0170] 1. Modeling method: Animals were randomly divided into 6 groups. Except for the normal control group, mice in other groups were given intraperitoneal injection of cyclophosphamide 100 mg / kg, once a day, for 3 consecutive days to form a leukopenia model.

[...

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Abstract

The invention discloses a compound shown by formula I, or usage of salt or ester which can be acceptable thereby on pharmacology, namely, a composition used for preparing medicine that can control and treat leukocytopenia. The invention also discloses the usage on controlling and treating immunological suppression.

Description

technical field [0001] The invention belongs to the field of pharmacy, and more specifically, the invention relates to a compound with the effect of raising white blood cells and a new application of the composition thereof. Background technique [0002] The white blood cell count in human peripheral blood is continuously lower than the normal value (4x10 9 / L) is called leukopenia and is most commonly caused by neutropenia. Patients may be asymptomatic or have nonspecific symptoms such as fatigue, anorexia, decreased energy, and a predisposition to infection. Whether co-infected neutropenia decreased degree. The most common sites of infection are the lungs, urinary tract, and skin. Leukopenia can be divided into two types: hereditary and acquired, among which acquired is the majority. Drugs, radiation, infection, toxins, etc. can all reduce leukocytes, and drugs are the most common. During treatment, the cause of leukopenia should be carefully searched, and appropriate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P7/00
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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