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Platelet activation factor resisting compound

An activating factor and anti-platelet technology, which can be used in anti-inflammatory agents, organic chemistry, drug combinations, etc., to solve problems such as the limitation of full efficacy of drugs, affecting clinical application effects, and poor bioavailability.

Active Publication Date: 2006-03-22
JIANGSU CAREFREE PHARM CO LTD
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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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0041]

[0042] Wherein, X is a linking skeleton containing 1-8 carbon atoms, and R1 and R2 are H or a hydrocarbon group with 1-8 carbon atoms. In order to further improve water solubility, increase bioavailability, and enhance curative effect, this embodiment can The above-mentioned ginkgolide B modified with a nitrogen-containing group is salted, that is: the drug compound is an organic acid salt of ginkgolide B with a nitrogen-containing group connected 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 connected to the 10-hydroxyl group, and the inorganic acid salt is sulfate or hydrochloride...

Embodiment 2、1

[0043] The preparation process of embodiment 2, 10-O-(dimethylaminoethyl) ginkgolide B and its hydrochloride

[0044]

[0045] After a novelty search by the Shanghai Science and Technology Novelty Search Consulting Center of the Chinese Academy of Sciences, the report stated that within the scope and time limit of the retrieved literature, no structure identical to the compound 10-O-(dimethylaminoethyl) ginkgolide B was found. The substance report proves that the compound is novel, and the structure of the compound is 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 platelet activation factor resisting compounds in the shown structure and their salts of organic acid or inorganic acid. Structurally, the compounds have various nitrogen-containing radicals connected to the hydroxyl radical in the tenth place of bilobalide B. The compounds of the present invention have the advantages of high water solubility, high bioavailability, full playing of the medicine effect, etc.

Description

technical field [0001] The present invention relates to a class of drugs with platelet activating factor (PAF) antagonism, in particular to a drug compound against platelet activating factor. Background technique [0002] Ginkgo biloba has been used as a medicinal plant for a long time. Around 1000 AD, Chinese folks used ginkgo leaves to treat asthma and bronchitis. With the standardization of drug extraction process and the in-depth study of pharmacological activity, countries all over the world, especially European countries such as Germany and France, have widely used Ginkgo biloba extract (GBE) to treat respiratory system, cardiovascular and cerebrovascular system and other diseases. Ginkgolides are a series of diterpenoid compounds present in Ginkgo biloba leaves and rhizomes, and their chemical properties are quite stable. Ginkgolide is a strong antagonist of platelet-activating factor (PAF), which is a strong physiological regulator and plays an important role in man...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61K31/366A61P9/10A61P29/00A61P11/06C07D311/00C07D307/00
Inventor 秦引林夏鹏张倩陈瑛何龙其
Owner JIANGSU CAREFREE PHARM CO LTD
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