Coumarin dimer compound, pharmaceutical composition, preparation method and application thereof

A technology of coumarins and compounds, applied in the field of natural medicinal chemistry, can solve problems such as no therapeutic drugs, achieve the effect of increasing expression and improving nerve cell damage

Active Publication Date: 2021-04-02
CHINA RESOURCES SANJIU MEDICAL & PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Currently, there are no clinically effective treatments for

Method used

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  • Coumarin dimer compound, pharmaceutical composition, preparation method and application thereof
  • Coumarin dimer compound, pharmaceutical composition, preparation method and application thereof
  • Coumarin dimer compound, pharmaceutical composition, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0092]Embodiment 2 Characterization of Compounds of formula I

[0093]

[0094]UV (UV) showed strong absorption at 297 nm and 326 nm, indicating that the compound is a coumarin compound. High resolution mass spectrometry gives molecular formula C28Hide26O7[M + NA]+: 497.1566 (CALCD 497.1576)Figure 11 .

[0095]Compound (i)1H-NMR spectrum (seeFigure 12 ) The low field area shows the characteristics of a pair of coumarin skeletons [δH6.20 (1H, D, J = 9.4 Hz, H-3), 7.83 (1H, D, J = 9.4 Hz, H-4)], and a set of ABX systems hydrogen signal [δH7.54 (1H, D, J = 8.6 Hz, H-5), 7.09 (1H, DD, J = 8.6, 2.3Hz, H-6), 7.32 (1H, D, J = 2.3 Hz, H-8)] , And a pair of mutually coupled oxygen protocoms [δH 6.24 (1H, D, J = 2.3 Hz, H-9), 4.69 (1H, D, J = 2.9 Hz, H-10)]. At the same time, in13A total of 28 carbon signals in the C-NMR spectrum were displayed in two coumarins, respectively, see Table 1.

[0096]Compound (i)1H-1H Cosy spectrum (seeFigure 13 ), Can be observed that three groups of proton coupling systems...

preparation experiment example 1

[0100]Preparation Experimental Example 1 (Preparation of Injection)

[0101]The compound obtained from the above-described example 1 described above, adding 1000 ml of injection water, pH value to 7, stirred with sodium carbonate to 7, stirring, sterilization, potting, gasification, vapor by 100 ° C for 15 minutes Sterilization, which was prepared for injection for injection of 2 mg / 2 ml of compound I.

preparation experiment example 2

[0102]Preparation Experimental Example 2 (Preparation of Capsules)

[0103]

[0104]According to the weight weighing of the above formula, the compound, microcrystalline cellulose, carboxymethyl starch sodium, sodium dodecyl sulphate, sodium sulfate, and the roller pressure method are used to carry out dry granulation, and then hard Mixed magnesium fatty acid is mixed, filled into the 3 # hollow capsule, which is made of a particulate set of a capsule containing 100 mg / grain containing a compound of formula I.

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Abstract

The invention relates to the field of natural pharmaceutical chemistry, and particularly provides a coumarin dimer compound, a pharmaceutical composition and a preparation method and application of the coumarin dimer compound. The coumarin dimer compound has a structure shown as a formula I shown in the specification. The coumarin dimer compound can remarkably improve nerve cell damage of an A[beta]1-42 induced senile dementia model; moreover, can improve neurotrophic factor expression, has anti-inflammatory and antioxidant effects, and can be used for preventing and treating nervous system degenerative diseases such as vascular dementia, vascular cognitive impairment, senile dementia (also called Alzheimer's disease), cholinergic neurodegenerative change, learning and memory ability decline and the like.

Description

Technical field[0001]The present invention relates to the field of natural pharmaceutical chemistry, and more particularly to a coumarin dimeric compound, a pharmaceutical composition, and a method and use thereof.Background technique[0002]Alzheimer's disease (AD, senile dementia) is a central nervous system degenerative disease based on sexual cognitive impairment and memory damage, is a slow disease process, continuous nerves that have deteriorated over time Dysfunction, 60% -70% of the contract, now there is one of the largest threats in human health in the 21st century. Early clinical manifestations in AD are difficult to remember the recent events, sexual memory damage, cognitive dysfunction, behavioral or character, daily dysfunction, minor behavior ability, MBI, the favorite on weekdays What is done is losing interest, cold, anxiety, anxiety, uncontrollable, more aggressive, lose interest in food, do everything is suspicious, often suddenly suddenly anger. With the continuous...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/37A61P25/28A61P25/00
CPCA61P25/00A61P25/28C07D493/04
Inventor 刘晖晖张容容刘中秋章时杰韩正洲马庆魏伟锋张洪胜许雷曾烨李明辉黄煜权谢文波张赟魏民马鹏岗
Owner CHINA RESOURCES SANJIU MEDICAL & PHARMA
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