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Benzimidazole and derivative thereof, and medicinal composition and application thereof

A technology of benzimidazole and its derivatives, applied in the application of drugs and functional foods, in the field of pharmaceutical compositions for the prevention and treatment of neuropsychiatric diseases, can solve problems such as poor therapeutic effect, harm, and unknown etiology

Inactive Publication Date: 2013-05-29
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the treatment of epilepsy is still dominated by drugs. Due to its unknown etiology, unclear pathogenesis, difficult diagnosis, and poor treatment effect, about 20%-30% of epilepsy patients cannot be controlled by drugs, or cannot tolerate the side effects of drugs. Refractory epilepsy has gradually become one of the main diseases that endanger the public health of the Chinese population

Method used

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  • Benzimidazole and derivative thereof, and medicinal composition and application thereof
  • Benzimidazole and derivative thereof, and medicinal composition and application thereof
  • Benzimidazole and derivative thereof, and medicinal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Compounds of the present invention can be prepared as shown in the following schemes (with R 1 For tumouramine as an example):

[0061]

[0062] Synthesis of benzimidazole and its derivatives:

[0063] 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.

[0064] Concrete implementation example:

[0065] 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)

[0066]

[0067] The preparation process is as follows:

[0068] Add 2-chlorobenzimidazole compounds into a microwave reaction tube, add magnets, add solvent isoamyl alcohol to di...

Embodiment 2

[0168] 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

[0170] 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 a derivative thereof, a medicinal composition which contains the benzimidazole and derivative thereof as active components and is used for preventing and treating neurological and psychotic diseases, and application thereof in preparation of medicaments and functional foods for resisting senility, senile dementia and other neurological and psychotic diseases. 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 benzimidazole and derivatives thereof, pharmaceutical compositions for preventing and treating neuropsychiatric diseases containing benzimidazole and derivatives thereof as active ingredients, and their preparation for preventing and treating neuropsychiatric diseases and Applications in functional foods. technical background: [0002] Neuropsychiatric diseases are a group of diseases mainly manifested in nervous system lesions, behavior, and mental activity disorders. They are mainly divided into neurological diseases and mental diseases, such as Alzheimer's disease, epilepsy, vascular dementia, Parkinson's disease, memory impairment, brain injury, Spinal cord injury, stroke, mental retardation, schizophrenia, etc. [0003] Senile dementia (Alzheimer's disease, AD) is a progressive and fatal neurodegenerative disease. Psychiatric symptoms and behavioral disturb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/30C07D401/12C07D401/04A61K31/4709A61K31/454A61K31/4439A61K31/4184A61P25/28A61P25/08A61P25/16A61P25/00A61P25/18A23L1/30
Inventor 罗怀容洪学传邓子新吴桂生丁爱军朱进妹邹系胜
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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