Benzimidazole and derivative thereof, and medicinal composition and application thereof in preparation of antidepressant medicaments

A technology of benzimidazole and derivatives, applied in the preparation of antidepressant drugs and functional foods, in the field of antidepressant drugs, benzimidazole and its derivatives, which can solve the inconvenience of simulation research and cannot fully explain depression Mechanism of action of antidepressants and other issues

Active Publication Date: 2013-05-29
泸州天演生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These studies put forward different hypotheses, trying to explain the mechanism of depression, so as to find a suitable way to cure the disease. However, due to the complexity of depression symptoms, various causes, guilt and suicidal tendencies and other characteristics are not convenient for simulation research, each hypothesis Neither fully explains the cases of depression nor the mechanism of action of antidepressants

Method used

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  • Benzimidazole and derivative thereof, and medicinal composition and application thereof in preparation of antidepressant medicaments
  • Benzimidazole and derivative thereof, and medicinal composition and application thereof in preparation of antidepressant medicaments
  • Benzimidazole and derivative thereof, and medicinal composition and application thereof in preparation of antidepressant medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Compounds of the present invention can be prepared as shown in the following schemes (with R 1 For tumouramine as an example):

[0055] .

[0056] The synthesis of benzimidazole and its derivatives of the present invention:

[0057] Add the benzimidazole compound into the microwave reaction tube, add the magnetron, add the solvent isoamyl alcohol to dissolve it, and finally add the substituted amine, stir evenly, and heat the reaction in the microwave reactor. The microwave reaction conditions are as follows: rise to 150° C. for 5 minutes and maintain for 150 minutes. After the reaction is finished, a series of conventional treatments can be carried out.

[0058] Specific implementation examples and descriptions of experiments:

[0059] Compound M084 (wherein R 1 is n-butylamino, R 2， R 3， R 4， R 5， R 6， is H, X is a compound of chlorine)

[0060]

[0061] The preparation process is as follows:

[0062] Add 2-chlorobenzimidazole compounds into a microwa...

Embodiment 2

[0162] According to the method of Example 1, benzimidazole and its derivatives are first prepared, and water for injection is added as usual, finely filtered, potted and sterilized to make an injection.

Embodiment 3

[0164] According to the method of Example 1, benzimidazole and its derivatives were first prepared, dissolved in sterile water for injection, stirred to dissolve, filtered with a sterile suction filter funnel, then sterile fine filtered, and packed in 2 ampoules , freeze-dried at a low temperature and then sterilized and melted to obtain a powder injection.

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PUM

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Abstract

The invention provides benzimidazole and derivative thereof, an antidepressant medicament which contains the benzimidazole and derivative thereof and a pharmaceutical carrier and excipient, and application thereof in preparation of antidepressant medicaments and preparation of functional foods. The benzimidazole and derivative thereof provided by the invention can be prepared into pharmaceutical preparations of various forms, including oral administration, injection, lung inhalation and transdermal preparations, and specifically including injections, oral liquids, tablets, capsules, granules, aerosols, dry powder inhalers, sprays, plasters and the like.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular relates to benzimidazoles and derivatives thereof, antidepressant medicines using the benzimidazoles as active ingredients, and their application in preparing antidepressant medicines and functional foods. technical background: [0002] Depression is a high-incidence mental illness, and patients are characterized by persistent low mood and cognitive impairment. Depression seriously plagues the life and work of patients, and brings a heavy burden to families and society. A joint study by the World Health Organization, the World Bank and Harvard University shows that depression has become the second largest disease in China's disease burden. Depression is highly prevalent, affecting more than 20% of people worldwide. Depression is also the disease with the highest suicide rate in the psychiatric department. The pain it causes to patients and their families, and the loss to soc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/30C07D401/12C07D401/04A61K31/4709A61K31/454A61K31/4439A61K31/4184A61P25/24A23L1/30
Inventor 罗怀容洪学传邓子新吴桂生杨丽萍朱进妹刘磊
Owner 泸州天演生物医药科技有限公司
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