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Egonol type benzofuran and novel use in pharmacy of glycosides thereof

A kind of technology of benzofuran and oleanol, applied in a new application field of a compound of general formula

Inactive Publication Date: 2009-08-12
CHENGDU DIAO JIUHONG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no literature records or research reports on the use of oleanol-type benzofuran and its glycosides as ACAT inhibitors for the above diseases

Method used

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  • Egonol type benzofuran and novel use in pharmacy of glycosides thereof
  • Egonol type benzofuran and novel use in pharmacy of glycosides thereof
  • Egonol type benzofuran and novel use in pharmacy of glycosides thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Extraction, separation and structure confirmation of oleanol-type benzofuran and its glycosides A, B, C, D, E, F, G, H, I, J

[0052] Extraction and separation: Take 2.2kg (dry weight) of the fruit of Styrax perkinsiae (Styrax perkinsiae, collected from Yongde County, Yunnan Province), grind it, and extract it with 80-90% industrial alcohol 25L at room temperature for 3 times, each time for 7 days . The extract was concentrated in vacuo to obtain 550g of total extract, which was suspended in 5L of hot water, extracted 5 times with petroleum ether, chloroform and n-butanol in sequence, each time with 5L of solvent, and the extract was concentrated respectively to obtain extract: Petroleum The ether fraction was 16 g, the chloroform fraction was 200 g, and the n-butanol fraction was 120 g. Samples were taken for in vitro activity screening, and both the chloroform and n-butanol fractions showed estrogen-promoting activity. Put the chloroform part on a silica ...

Embodiment 2

[0085] The preparation of embodiment 2 tablet

[0086] Tablet composition: Compound A 300mg

[0087] HPMC LV10028.7g

[0088] Lactose 70g

[0089] Magnesium Stearate 1g

[0090] (1000 pieces made in total)

[0091] Take Compound A, HPMC, and lactose, mix them evenly, use 75% ethanol as a binder to make wet granules, pass through a 22-mesh sieve, dry at 50°C for 3 hours, granulate with a 22-mesh sieve, add magnesium stearate, mix evenly, and press into tablets. Tablet weight 100mg, for patients with atherosclerosis or hyperlipidemia, orally, twice a day, 1 tablet each time, one month as a course of treatment.

Embodiment 3

[0092] The preparation of embodiment 3 capsules

[0093] Capsule Composition: Compound B 300mg

[0094] Starch 98.8g

[0095] Magnesium Stearate 1g

[0096] (1000 capsules in total)

[0097] Take compound B, starch, and magnesium stearate, mix well, and install a rubber sleeve. 100mg per capsule, for patients with atherosclerosis or hyperlipidemia, orally, twice a day, 1 tablet each time, one month as a course of treatment.

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PUM

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Abstract

The invention discloses the application of egonol-type benzofuran and glycosides thereof in the preparation of an ACAT (Acyl-CoA:Cholesterol Acyltransferase) inhibitor, provides the application of egonol-type benzofuran as shown in general formula I and glycosides thereof in the preparation of the ACAT inhibitor, and further provides the drug combination of the ACAT inhibitor, which contains egonol-type benzofuran and glycosides thereof with the active component being shown in the general formula I. The egonol-type benzofuran and the glycosides thereof can be prepared into various forms of drug, such as tablets, capsules and the like, because of the significant effect of the ACAT inhibitor thereof. The invention is suitable for preventing and treating diseases, such as angina, myocardial infarction, cerebral infarction, Alzheimer's disease, acute coronary syndromes (ACS), percutaneous transluminal coronary angioplasty (PTCA) or post-stenting coronary restenosis; and the invention, as a therapeutic agent for regulating the sebaceous gland function and inhibiting the excessive production of sebum, is also suitable for curing diseases, such as oily skin, acne, seborrhea, acne-like lesion caused by corticosteroid and the like.

Description

technical field [0001] The present invention relates to a new application of a compound of general formula, specifically, the present invention relates to the preparation of oleanol-type benzofuran and its glycosides for the prevention and / or treatment of angina pectoris, myocardial infarction, cerebral infarction, cerebral apoplexy, and ear Use in drugs for Alzheimer's disease, acute coronary syndrome, coronary artery restenosis after PTCA or stent placement, and oily skin, acne, seborrhea, and acne-like lesions caused by corticosteroids. Background technique [0002] The accumulation of cholesteryl ester in a large area of ​​blood vessels will cause atherosclerotic lesions and form fat-rich plaques. The destruction of fat-rich plaques will form thrombus and block the coronary lumen, which will lead to acute coronary syndrome, angina pectoris, and myocardial infarction. and other diseases. The formation of plaques formed by atherosclerotic lesions in the carotid arteries a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/36A61K31/7048A61P43/00A61P9/10A61P3/06A61P25/28A61P17/08
Inventor 晏菊芳李麒麟颜永红孙建王晓琴陈欣
Owner CHENGDU DIAO JIUHONG PHARMA FACTORY
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