Use of 3-substituted phthalide and the analogue

The technology of an analogue, phthalide, is applied in the field of preparation of medicines for the prevention and treatment of Alzheimer's disease and other neurological diseases, and can solve the problems of no effective treatment and the like

Inactive Publication Date: 2009-06-17
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are currently no treatments that specifically treat or reverse disease progression

Method used

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  • Use of 3-substituted phthalide and the analogue
  • Use of 3-substituted phthalide and the analogue
  • Use of 3-substituted phthalide and the analogue

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Preparation of 3-substituted phthalides:

[0023] The novel 3-substituted phthalide compounds involved in the present invention can be prepared according to the following two methods, wherein method one is used to prepare chiral novel 3-substituted phthalide compounds, and method two is used to prepare racemic Novel 3-substituted phthalides.

[0024] Method 1: From room temperature to 80°C, with a substrate concentration of 0.5-1.25 mol / L, in 2-5 equivalents of reducing agent formate, chiral diamine ligand and (p-methylisopropyl)phenyl dichloride Under the catalysis of the complex catalyst of ruthenium dimer, the number of moles of the substrate and the number of moles of the catalyst are 100-500:1, react for 4-24 hours, and purify by column chromatography with a certain yield and a certain optical purity to obtain Product; General reaction formula is as follows:

[0025]

[0026] Among them, the main configuration of the product is determined by the conf...

Embodiment 2

[0038] Example 2 biological test

[0039] 1. Drosophila training and learning index measurement operation of olfactory short-term memory deficit test:

[0040]About 100 fruit flies were placed in an automatic training device for training. During the training, two gases 1.5‰ octanol and 1‰ methylcyclohexanol were introduced successively, one with electric shock CS+ and the other without electric shock CS-, 1 Their memory was tested immediately after the period training ended. During the detection, the fruit flies were placed in the center of two opposite smells, and allowed to choose freely for 120 seconds, and the learning index was calculated according to the number of fruit flies that chose each smell.

[0041] 2. Drosophila training and learning index measurement operation of the olfactory long-term memory deficit test:

[0042] About 100 fruit flies were trained in an automatic training device. During the training, two gases 1.5‰ octanol and 1‰ methylcyclohexanol were in...

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PUM

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Abstract

The present invention relates to the use of 3-sbustituted phthalide or analogue for preparing the medicine for treating Alzheimer disease or other neurotic disease. The structural formula is shown in the right formula. Filtering is executed through a high-effective living model which integrates gene technique and biological technique. The research shows that most compounds have a certain function that the defective individual recovers learning capacity, wherein a plurality of specific compounds represent better activity. The learning capacity of deflective individual can be recovered for above 85%. Furthermore a stable treating effect can be shown in a plurality of tests.

Description

technical field [0001] The invention relates to the use of a series of 3-substituted phthalide compounds and their analogues, especially the use as a medicine for the prevention and treatment of Alzheimer's disease and other neurological diseases. Background technique [0002] Alzheimer's disease, also known as Alzheimer's disease (Alzheimer's disease, AD) is a kind of primary degenerative brain disease that occurs in old age and early old age, and refers to a kind of persistent high-level neurological dysfunction, that is, in the Obstacles in memory, thinking, analysis and judgment, visuospatial recognition, emotions, etc. without disturbance of consciousness. Its characteristic pathological changes are atrophy of the cerebral cortex, accompanied by deposition of β-amyloid (β-AP), neurofibrillary tangles (neurofibrillary tangles, NFT), a large number of memory neurons decreased, and The formation of senile plaques (senileplaque, SP). There are currently no therapeutic dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K31/366A61K31/381A61K31/4709A61K31/403A61K31/437A61P25/28
Inventor 林国强张波陈雯雯孙兴文李榕徐明华
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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