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Coumarether compound and use of its composition

A technology of coumarin and compounds, which is applied in the field of coumarin compounds, and can solve the problems of weak drug efficacy, poor bioavailability, and many side effects

Active Publication Date: 2009-12-09
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not a bronchodilator, nor is it anti-inflammatory or anti-allergic, only for prevention
(5) Anticholinergic drugs, such as Propylene, can resist the spasm effect of the vagus nerve on the bronchi, but these drugs have poor bioavailability, weak efficacy, and many side effects, so they are rarely used in general asthma patients
[0022] In summary, there is still a lack of drugs with rapid onset of action and few side effects on the market.

Method used

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  • Coumarether compound and use of its composition
  • Coumarether compound and use of its composition
  • Coumarether compound and use of its composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1 Eclipta alba (Eclipta alba) extract compound wedelolide

[0089] (1) soaking and filtering

[0090] Eclipta whole grass 300kg, fully immersed in 0.75 tons of ethanol (concentration 95%)→soak overnight (10 hours)→coarse filtration, thereby removing the whole grass residue (retention)→net filtration (suction filtration) or high-speed centrifugation (10000rpm, 10 minutes), thereby removing dust and fine residue → green clarified filtrate.

[0091] (2) Ethanol recovery

[0092] Recover ethanol by distillation, the temperature does not exceed 60 degrees Celsius → every 2 hours of back distillation, remove the extract in the reaction kettle to the collection bucket (the extract is dark dark green, slightly viscous) → repeat the above steps until all ethanol is recovered .

[0093] (3) Second soaking and back distillation

[0094] Recover 0.75 tons of ethanol, re-soak the whole herb residue → soak overnight, the requirements for coarse filtration, net filtration ...

Embodiment 2

[0105] Embodiment 2 chemically synthesizes the compound of the present invention

[0106] Compounds 1 to 6 were synthesized according to the synthesis method in the literature (Wong et.al. "Wedelolactone and coumestan derivatives as new antihepatotic and antiphlogistic principles. Arzneimittelforschung. 1998 May38(5): 661-5;).

[0107]

[0108] Among them, compound 1: R 1 =R 2 = H, R 3 =R 4 =OH;

[0109] Compound 2: R 1 =OH, R 2 =CH 3 , R 3 =R 4 =OH;

[0110] Compound 3: R 1 =OH, R 2 =CH 3 , R 3 = Cl, R 4 =OH;

[0111] Compound 4: R 1 =OCH 3 , R 2 = H, R 3 = Cl, R 4 = H;

[0112] Compound 5: R 1 = H, R 2 =(CH 2 ) 2 CH 3 , R 3 =OCH 3 , R 4 = Cl;

[0113] Compound 6: R 1 =OH, R 2 =CH 3 , R 3 = H, R 4 =OH.

Embodiment 3

[0114] The preparation of embodiment 3 tablet

[0115] Utilize conventional technique, mix following component, then directly compress tablet, prepare the pharmaceutical composition of tablet form, its formula is as follows:

[0116] Element

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PUM

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Abstract

The present invention discloses one kind of coumar ether compound extracted from feverfew or its pharmaceutically acceptable salt, and the application of the coumar ether compound or its pharmaceutically acceptable salt, the extract containing the coumar ether compound or its pharmaceutically acceptable salt and their medicine composition in treating bronchial asthma, bronchitis and emphysema. Animal experiment shows that the coumar ether compound extracted from feverfew can treating bronchial asthma, bronchitis and emphysema effectively.

Description

technical field [0001] The invention relates to a coumarin compound extracted from Compositae plants, and the application of the pharmaceutical composition or health food containing the compound in the treatment of bronchial asthma, chronic bronchitis and emphysema. Background technique [0002] Coumarin compounds (as shown in formula I) can be extracted from plants or obtained by chemical synthesis, semi-synthesis, or biotransformation, for example, from Compositae plants Eclipta prostrata Linn, Wedelia chinensis, or Extracted from plants such as Eclipta alba. The extraction part of the compound in Compositae plants is the branch, leaf or fruit part of the plant, especially the leaf part. [0003] [0004] In the formula, [0005] R 1 Represents hydrogen atom, hydroxyl group and methoxy group; [0006] R 2 Represents hydrogen atom, C 1 -C 8 alkyl; [0007] R 3 and R 4 each independently selected from a hydrogen atom, a halogen atom, a hydroxyl group, and a meth...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/366A61P11/00A23L1/30C07D307/00C07D311/00A23L33/105
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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