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Coupling medicament for treating diabetes mellitus and medicinal application thereof

A technology of diabetes and drugs, which is applied in the field of coupled drugs for the treatment of diabetes and its medical application, and can solve the problems of diabetes and cardiovascular diseases that are not strong enough or fast enough

Inactive Publication Date: 2011-06-29
CHIFCON DRUG DISCOVERY SUZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the current natural medicines for treating diabetes and cardiovascular diseases are not strong enough and fast enough, and these weaknesses limit their further application

Method used

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  • Coupling medicament for treating diabetes mellitus and medicinal application thereof
  • Coupling medicament for treating diabetes mellitus and medicinal application thereof
  • Coupling medicament for treating diabetes mellitus and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Example 1: Coupling Compound XIV of Oleanolic Acid (OA) and Nitric Oxide Donor

[0101] The synthetic equation of this coupled compound XIV is:

[0102]

[0103] The chemical name of the coupled compound XIV is:

[0104] (Z)-2-(((6aS, 6bR, 10S, 12aR, 12bR)-10-hydroxy-2, 2, 6a, 6b, 9, 9, 12a-heptamethyl-1, 2, 3, 4, 4a, 5, 6, 6a, 6b, 7, 8, 8a, 9, 10, 11, 12, 12a, 12b, 13, 14b-icosahydropicene-4a-carbonyloxy)methoxy)-1-(pyrrolidin-1-yl)diazene oxide .

[0105] The preparation process of this coupling compound XIV is:

[0106] Compound OA (zidonolic acid, 84mmol) was dissolved in DMF (100ml), and 90mmol of Na was added 2 CO 3 And 10mmol of KI, after stirring for 15 minutes, add compound 1 (chemical name: (Z)-2-(chloromethoxy)-1-(pyrrolidin-1-yl) diazene oxide, known compound, self-made) (72mmol). The resulting mixture was stirred at a temperature of 100°C for 16 hours. After cooling, the solid was filtered off, 150ml of water was added, the product was extracted t...

Embodiment 2

[0112] Example 2: Coupling Compound XV of Oleanolic Acid (OA) and Nitric Oxide Donor

[0113] The synthetic equation of this coupling compound XV is:

[0114]

[0115] The chemical name of the coupled compound XV is:

[0116] 3-cyano-4-(((6aS, 6bR, 10S, 12aR, 12bR)-10-hydroxy-2, 2, 6a, 6b, 9, 9, 12a-heptamethyl-1, 2, 3, 4, 4a, 5, 6, 6a, 6b, 7, 8, 8a, 9, 10, 11, 12, 12a, 12b, 13, 14b-icosahydropicene-4a-carbonyloxy)methyl)-1,2,5-oxadiazole 2-oxide.

[0117] The preparation process of this coupling compound XV is:

[0118] Compound OA (zidonolic acid, 3mmol) was dissolved in DMF (30ml), and 3.6mmol of Na was added 2 CO 3 and 1 mmol of KI, after stirring for 15 minutes, compound 2 (chemical name: 4-(bromomethyl)-3-cyano-1,2,5-oxadiazole 2-oxide, known compound, self-made) (2.5 mmol) was added. The resulting mixture was stirred at room temperature for 16 hours. After the solid was removed by filtration, water (50ml) was added and the product was repeatedly extracted three...

Embodiment 3

[0123] Example Three: Rhein (Rh) and Nitric Oxide Donor Coupling Compound XVI

[0124] The chemical structural formula of this coupling compound XVI:

[0125]

[0126] The chemical name of the coupling compound XVI is:

[0127] 3-cyano-4-((4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carbonyloxy)methyl)-1,2,5-oxadiazole 2-oxide.

[0128] The preparation process of the coupling compound XVI is the same as that of Example 2, so it will not be repeated. The coupling compound XVI prepared by the above method is proved by means of nuclear magnetic resonance, mass spectrometry and element analysis, etc., that the coupling compound XVI does have the elemental composition and molecular structure described in the above molecular formula. The specific parameters are:

[0129] 300mz 1 H NMR (DMSO-d6) δ8.20-7.40 (m, 5H), 5.69 (2H);

[0130] 13 C NMR (DMSO-d6) δ191.10(C), 180.67(C), 163.06(C), 161.34(C), 160.87(C), 153.60(C), 137.59(CH), 137.69(C), 136.13 (C), 133.96(C), 133...

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Abstract

The invention discloses a natural coupling medicament for treating diabetes mellitus and other blood vascular diseases. The medicament has a chemical structure with a general formula (I), and is formed by coupling natural ingredients of active Chinese medicinal herbs and a nitric oxide donor. The coupling medicament can be used for preparing finished product medicaments for treating the diabetes mellitus, and has the effects of reducing blood sugar, blood pressure and blood fat, resisting platelet aggregation, resisting atherosclerosis and the like. After entering human bodies, the coupling medicament can be subjected to enzymolysis in vivo to release nitric oxide and natural medicinal ingredients, so the natural coupling medicament has the advantages of small toxic and side effect and lasting effect of natural medicaments and has the characteristic of quick and high activity of the nitric oxide, and has the wide application range in pharmaceutical science.

Description

technical field [0001] The present invention relates to a class of drugs for treating blood vessel diseases and their medical application, especially to a class of coupled drugs capable of enzymatically releasing nitric oxide free radicals in the body. At the same time, it can also be used to treat other cardiovascular diseases. Background technique [0002] Nitric oxide (hereinafter abbreviated as NO), as a free radical gas, is a low molecular weight and hydrophobic bioactive molecule in the human body, which can freely pass through the cell membrane and act on target molecules in the cell. In theory, nitric oxide can reach any part of cells and tissues, and can regulate various cell functions and produce a wide range of biological effects in vivo. Therefore, nitric oxide donors and regulators have important application value in the research and development of new drugs. [0003] As a biological effect molecule, NO participates in various important physiological effects in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61P3/10A61P3/06A61P9/12A61P9/10A61P7/02
Inventor 冯子侠刘晓东尚红鹰
Owner CHIFCON DRUG DISCOVERY SUZHOU
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