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L-tryptophan asiatic acid amide and applications thereof in preparation of antidepressant medicines

A technology of asiatic acid and asiaticoyl, which is applied to asiaticoyl-L-tryptophan and its application field in the preparation of antidepressant drugs, can solve problems such as adverse reactions, restricted widespread use, etc., and achieve high The effect of active, good development value

Active Publication Date: 2014-08-13
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But there are different degrees of adverse reactions, such as drowsiness, blurred vision, high blood pressure, convulsions and low libido, etc., which limits its wide use

Method used

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  • L-tryptophan asiatic acid amide and applications thereof in preparation of antidepressant medicines
  • L-tryptophan asiatic acid amide and applications thereof in preparation of antidepressant medicines
  • L-tryptophan asiatic acid amide and applications thereof in preparation of antidepressant medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: Preparation of asiatic acid derivative X4

[0022]

[0023] The synthesis method of asiatic acid derivative X4 (asiatic acid-L-tryptophan) was as follows: 200 mg of asiatic acid (JXCS) was dissolved in 10 mL of tetrahydrofuran, and 220 mg of PyBOP, 100 mg of DIEA and 120 mg of L -Tryptophan, after reacting at room temperature for 5 hours, the solvent was evaporated, and after column chromatography, 98 mg of the product was obtained. Purity: 96%. [M+H]+: 675.1. 1 H NMR (300 MHz, DMSO): δ 12.66 – 12.37 (m, 1H), 10.82 (s, 1H), 7.51 (d, J = 7.7 Hz, 1H), 7.28 (d, J = 8.3 Hz, 1H), 7.16 (s, 1H), 7.11 – 6.99 (m, 2H), 6.99 – 6.87 (m, 1H), 4.96 (s, 1H), 4.34 (d, J = 18.1 Hz, 2H), 4.12 (s, 2H) , 3.43 (s, 1H), 3.20 – 2.98 (m, 4H), 2.02 – 1.92 (m, 1H), 1.92 – 1.79 (m, 1H), 1.67 (d, J = 12.0 Hz, 5H), 1.26 (d , J = 17.5 Hz, 10H), 1.07 (s, 2H), 0.82 (dd, J = 41.7, 8.1 Hz, 15H), 0.64 (s, 3H), 0.52 (s, 3H).

Embodiment 2

[0024] Embodiment 2, the preparation of asiaticoyl-L-tryptophan tablet

[0025]

[0026] Process:

[0027] Take the prescription amount of asiaticoyl-L-tryptophan, crush it through a 100-mesh sieve, then crush the prescription amount of starch and lactose through a 100-mesh sieve, and mix well. Add asiaticoyl-L-tryptophan and sodium starch glycolate to the mixed starch and lactose, and mix well. Add an appropriate amount of 7% starch slurry, mix well, granulate through a 16-mesh wire mesh, dry below 60°C, granulate, add an appropriate amount of magnesium stearate, mix evenly, analyze the content, and then compress into tablets. It can be made into 1000 tablets each containing asiaticoyl-L-tryptophan 30mg.

Embodiment 3

[0028] Embodiment 3, the preparation of asiaticoyl-L-tryptophan capsules

[0029]

[0030] Process:

[0031] Take the prescribed amount of asiaticoyl-L-tryptophan, crush it through a 100-mesh sieve, add the prescribed amount of starch and starch silica gel, mix well, and directly put it into capsules to make 1000 capsules each containing asiaticoyl - Capsules of L-Tryptophan 30 mg.

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Abstract

The invention relates to L-tryptophan asiatic acid amide (X4) and applications thereof in preparation of antidepressant medicines, and also provide a pharmaceutical composition comprising the L-tryptophan asiatic acid amide. Experiments show that: the L-tryptophan asiatic acid amide and the pharmaceutical composition thereof are safe, efficient, stable and cheap medicines for preventing and treating depression, have high activity, are superior to asiatic acid and fluoxetine, and have high development value.

Description

technical field [0001] The present invention relates to the compound asiaticoyl-L-tryptophan and its application in the preparation of antidepressants. Background technique [0002] With the acceleration of people's life rhythm, the increase of social pressure, and the decrease of psychological endurance, the rate of suffering from depression continues unabated. According to the World Health Organization, patients with various types of depression account for 3% to 5% of the global population. Depression is expected to become the second most common disease worldwide by 2020. Therefore, there is an urgent need for safe, efficient and inexpensive antidepressants. [0003] Drugs currently used to treat depression mainly include: tricyclic antidepressants and monoamine oxidase inhibitors such as doxepin; selective monoamine oxidase inhibitors such as moclobemide; serotonin reuptake inhibitors such as fluoxetine; Sexual NE reuptake inhibitors such as reboxetine; dual 5-HT and n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/58A61P25/24
Inventor 张黎赵娜萍侯静李铁军张大志蔡瞻马建丽韩志鹏张姗姗朱鹏熹盛丹丹杨雪郝翀芮耀诚卫立辛刘厚佳
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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