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Coumarin dimer compound, pharmaceutical composition, and preparation method and application of the coumarin dimer compound

A technology of coumarins and compounds, which is applied in the field of natural medicinal chemistry, can solve the problem of lack of therapeutic drugs, and achieve the effects of improving expression and nerve cell damage.

Active Publication Date: 2020-04-28
CHINA RESOURCES SANJIU MEDICAL & PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This new chemical entity called Coumaline Dimers improves how neurons are protected from amyloids that cause spongiform encephalopathies or other brain disorders like Parkinson's Disease. It also enhances neural growth factor production which helps with motor functioning at work better than previous drugs without causing side effectes on their own body.

Problems solved by technology

This patents discusses different aspects related to Amyopectina syndrome: genetic factors play crucial roles during childhood learning; environmental conditions affect brain function and mental performance. There may be other risk factors associated with this condition like smoking cigarettage use, alcohol consumption, excess weight gain due to lack of exercise, obstructed eatings, sleep disorders caused by stressors, abnormal behaviors, and social interactions involving older individuals. Current treatments focus primarily on symptom reduction but they can cause side effects.

Method used

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  • Coumarin dimer compound, pharmaceutical composition, and preparation method and application of the coumarin dimer compound
  • Coumarin dimer compound, pharmaceutical composition, and preparation method and application of the coumarin dimer compound
  • Coumarin dimer compound, pharmaceutical composition, and preparation method and application of the coumarin dimer compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0092] The characterization of embodiment 2 formula I compound

[0093]

[0094] Ultraviolet spectrum (UV) shows strong absorption at 297nm and 326nm, indicating that the compound is a coumarin compound. High resolution mass spectrometry gave the molecular formula C 28 h 26 o 7 , [M+Na] + :497.1566(calcd 497.1576), see Figure 11 .

[0095] Compound (I) in 1 H-NMR spectrum (see Figure 12 ) low-field region showing characteristic hydrogen signals on a pair of coumarin backbones [δ H 6.20(1H, d, J=9.4Hz, H-3), 7.83(1H, d, J=9.4Hz, H-4)], and a set of hydrogen signals of the ABX system [δ H 7.54(1H,d,J=8.6Hz,H-5),7.09(1H,dd,J=8.6,2.3Hz,H-6),7.32(1H,d,J=2.3Hz,H-8)] , and a pair of coupled oxygen-proton signals [δ H 6.24 (1H, d, J=2.3Hz, H-9), 4.69 (1H,d, J=2.9Hz, H-10)]. At the same time, in 13 The C-NMR spectrum shows a total of 28 carbon signals, which are respectively assigned to two coumarin units, as shown in Table 1.

[0096] Compound (I) in 1 H- 1 In the...

preparation experiment example 1

[0100] Preparation experiment example 1 (preparation of injection)

[0101] Take 1000 mg of the compound represented by formula I obtained in Example 1 above, add 1000 ml of water for injection, adjust the pH value to 7 with sodium carbonate, stir to dissolve, sterilize and filter, pot, and circulate steam at 100 ° C for 15 minutes Sterilize, and make each injection containing 2mg / 2ml of the compound of formula I for injection.

preparation experiment example 2

[0102] Preparation experiment example 2 (preparation of capsules)

[0103]

[0104] Weigh the compound shown in formula I obtained in Example 1 according to the weight of the above formula, microcrystalline cellulose, sodium carboxymethyl starch, sodium lauryl sulfate, mix, adopt the roller compaction method to carry out dry granulation, and then mix with hard Magnesium fatty acid is mixed, filled into 3# hollow capsules, and made into capsules containing formula I compound 100mg / grain for oral use.

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PUM

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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

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Claims

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Application Information

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Owner CHINA RESOURCES SANJIU MEDICAL & PHARMA
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