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Medicinal compound for resisting platelet activating factor

A technology of pharmaceutical compounds and activating factors, which is applied in the direction of drug combinations, antipyretics, anti-inflammatory agents, etc., can solve problems such as the limitation of drug efficacy, impact on clinical application effect, and poor bioavailability

Inactive Publication Date: 2007-01-24
秦引林
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, ginkgolide B is a diterpene compound with a hexacyclic cage structure. It has a rigid structure, is insoluble in water, and has poor bioavailability, which limits the full use of the drug effect and affects the clinical application effect.

Method used

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  • Medicinal compound for resisting platelet activating factor
  • Medicinal compound for resisting platelet activating factor
  • Medicinal compound for resisting platelet activating factor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] An anti-platelet activating factor drug compound, characterized in that the drug compound is connected with a nitrogen-containing group on the 10-position hydroxyl group of ginkgolide B, and its structural formula is as follows:

[0041]

[0042] Among them, X is a linking skeleton containing 1-8 carbon atoms, and R1 and R2 are H or a hydrocarbon group with a carbon number of 1-8. In order to further improve the water solubility, increase the bioavailability, and enhance the curative effect, this embodiment can The above-mentioned ginkgolide B modified with a nitrogen-containing group forms a salt, that is, the drug compound is an organic acid salt of ginkgolide B with a nitrogen-containing group attached to the 10-hydroxyl group, and the organic acid salt is citrate or Acetylsalicylate; the above-mentioned drug compound can also be an inorganic acid salt of ginkgolide B with a nitrogen-containing group attached to the 10-position hydroxyl group, and the inorganic acid sa...

Embodiment 2、1

[0043] Example 2, 10-O-(dimethylaminoethyl) ginkgolide B and the preparation process flow of its hydrochloride

[0044]

[0045] After a novelty search conducted by the Shanghai Sci-tech Novelty Search and Consultation Center of the Chinese Academy of Sciences, the report stated that: within the scope and time limit of the searched literature, there is no identical structure to the compound 10-O-(dimethylaminoethyl) ginkgolide B The material report proved that the compound is novel and the structure of the compound was discovered.

Embodiment 3

[0046] Example 3 10-O-(p-dimethylaminobenzyl) ginkgolide B and its preparation process

[0047]

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Abstract

The present invention discloses a kind of medicine compound antaonizing platelet activating factor. The medicine compound is bilobalide B with nitrogen-containing radical connected to the hydroxyl radial in the site 10 and has the structure as shown. The medicine compound of the present invention has high water solubility, high bioavailability and high curative effect, and its salt has greatly raised water solubility, bioavailability and curative effect.

Description

Technical field [0001] The present invention relates to a class of drugs with platelet activating factor (PAF) antagonism, in particular to a pharmaceutical compound against platelet activating factor (PAF). Background technique [0002] Ginkgo has been used as a medicinal plant for a long time. Around 1000 AD, the folks in my country used Ginkgo biloba to treat asthma and bronchitis. With the standardization of drug extraction technology and the in-depth study of pharmacological activity, countries around the world, especially European countries such as Germany and France, have widely used Ginkgo biloba extract (GBE) to treat diseases such as the respiratory system and the cardiovascular and cerebrovascular systems. Ginkgolides are a series of diterpenoids present in the leaves and rhizomes of Ginkgo biloba, and their chemical properties are quite stable. Ginkgolide is a strong antagonist of platelet-activating factor (PAF). Platelet-activating factor is a strong physiological r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61P9/10A61P37/08A61P11/06A61P29/00C07D307/00
Inventor 秦引林夏鹏张倩陈瑛何龙其
Owner 秦引林
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