Pharmaceutical application of derivant of benzofuran-ketone

A technology of drugs and compounds, applied in the field of pharmaceuticals, can solve the problems of gastrointestinal irritation and side effects, weak analgesic effect, etc.

Inactive Publication Date: 2005-01-26
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the second class of drugs has relatively weak analgesic effects and side effects of gastrointestinal irritation

Method used

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  • Pharmaceutical application of derivant of benzofuran-ketone
  • Pharmaceutical application of derivant of benzofuran-ketone
  • Pharmaceutical application of derivant of benzofuran-ketone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Grind 10kg of the aerial part of Jenvoi grass, extract it with 95% diethyl ether at room temperature for 48 hours, and obtain 0.6kg of extract, extract the above extract with diethyl ether, chloroform, ethyl acetate, and n-butanol respectively, in which the chloroform parts are combined and concentrated , separated on a silica gel column. II Chloroform-acetone mixed solvent was eluted, and the eluents were combined and concentrated to obtain white needle crystals, britannilactone 3g, mp.175-177°C. 0.03%. 1-O-Acetylbritanniactone, mp. 124-126°C. 0.01%.

Embodiment 2

[0022] Pulverize the aboveground part of the golden Buddha grass, extract it with 95% ethanol at room temperature to obtain the extract, extract the above extract with ether, chloroform, ethyl acetate, and n-butanol respectively, wherein the chloroform part is combined and concentrated, and placed Separation on a silica gel column. Using gradient elution, the eluents of the same components were combined and concentrated to obtain white orthorhombic crystals, (I) (britannilactone, mp.175-177°C, 0.03%) and needle crystals (II) (1-O- Acetylbritanniactone, mp. 124-126°C, 0.01%).

[0023]

[0024] Therefore, we studied a series of compounds, all of which contain benzofuranone structure and have analgesic activity. The general structural formula of this series of compounds is as follows:

[0025]

[0026] Benzofuranone Derivatives

[0027] No. R 1 R 2 R 3

[0028] 1CH 3 CH 2 CO CH 3 -CH 3 or=CH 2

[0...

Embodiment 3

[0054] Take 10,000g of Golden Buddha Herb, add 10,000ml of 95% ethanol to soak overnight, heat and reflux for extraction for 2 hours, filter, discard the medicinal residues, concentrate, add an equal volume of water to the filtrate, stir well, and refrigerate overnight. Filtrate, concentrate under reduced pressure, concentrate the filtrate to about 1000g, add a suitable shaper to granulate, and obtain the granule.

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Abstract

A benzofuranone derivative and its medical application are disclosed. Said derivative can be modified to obtain 50 derivative S, while can be used as analgesic of both inflammatory pain and neurous pain. Its effective rate is 99% (50 cases of illness).

Description

technical field [0001] The present invention relates to the use of benzofuranone derivatives, in particular to the use in the field of pharmacy. technical background [0002] Pain is a protective and defensive function established by the body when it is subjected to some kind of harmful stimulus and causes the body to get rid of the further damage of this stimulus. Clinically, the nature, characteristics, location and time course of pain often become one of the important diagnostic indicators for certain diseases. However, pain itself and the accompanying series of physiological and biochemical reactions are harmful to the body to varying degrees. Chronic intractable pain can change people's personality, and the severe pain can even cause shock or life-threatening. The principle of pain treatment is to make a clear diagnosis and remove the cause as much as possible. However, after the etiology is clarified, drug pain relief is still the first choice of treatment. Analges...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/343A61P25/04A61P29/00C07D307/83
Inventor 张嫡群任雷鸣付焱袁志芳王志云张兰桐
Owner HEBEI MEDICAL UNIVERSITY
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