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Medicine for treating facial nerve injury and preparation method thereof

A drug and pharmaceutical technology, applied in the field of medicine, can solve the problems of less clinical trials and fewer drugs, and achieve excellent protective activity

Inactive Publication Date: 2020-03-27
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although many compounds for the treatment or prevention of neurodegenerative diseases have been described in the prior art, few actually enter clinical trials, and even fewer drugs are approved for marketing

Method used

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  • Medicine for treating facial nerve injury and preparation method thereof
  • Medicine for treating facial nerve injury and preparation method thereof
  • Medicine for treating facial nerve injury and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1: (E)-3-(6-(3,4-dimethyl-1H-pyrazol-5-yloxy)benzo[d]thiazol-2-yl)-N-hydroxyacrylamide (compound 1)

[0056]

[0057] Step 1: Under the protection of argon, 2-bromobenzo[d]thiazol-2-ol (4.56g), methyl acrylate 1ml, potassium acetate 3.9g, bis(triphenylphosphino)palladium dichloride 0.1 g was dissolved in 100ml of DMF, and reacted under reflux for 6h, and the reaction was complete as detected by TLC. Add 200ml of water and stir for 10min, extract with DCM, wash with saturated brine three times, dry over anhydrous sodium sulfate, evaporate the solvent under reduced pressure to obtain white solid (E)-3-(6-hydroxybenzo[d]thiazol-2-yl)acetic acid Methyl ester 3.83g, yield 81.2%.

[0058] Step 2: Add 2.35g of (E)-3-(6-hydroxybenzo[d]thiazol-2-yl)methyl acetate, 3.8g of HATU and 0.69g of hydroxylamine hydrochloride to 500ml of DCM under the protection of argon. , the reaction mixture was stirred at 20 °C for 5 h. The mixture was poured into water, diluted with D...

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Abstract

The invention provides benzothiazole compounds having a structure represented by the formula (I). The provided compounds have an excellent protective effect on nerves, can be used to treat diseases related with nerve damages, such as facial nerve damage, peripheral nerve damage caused by body damage or diseases (diabetes, eg.), neurological disorders (Parkinson's disease, Alzheimer disease, amyotrophic lateral sclerosis, etc.) caused by neural degeneration, and the like, and is preferentially used to treat facial nerve damage.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a medicine for treating nerve damage, and the medicine can treat nerve diseases related to nerve damage, such as facial nerve damage. Background technique [0002] Facial nerve injury is a kind of neurological disease, can be divided into traumatic facial nerve injury (such as physical injury such as traffic accident, fall injury, gunshot wound, stab wound, electric burn injury) and iatrogenic trauma according to the etiology. Among them, the mode of external force can be divided into exposure, pulling, extrusion, pressing, sharp instrument cutting injury and blunt instrument friction injury and other types. Neurological diseases are associated with the death or damage of neuronal cells. Typical treatments for neurological diseases involve drugs that inhibit neuronal cell death. More recent approaches involve promoting nerve regeneration by promoting neuronal growt...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/12A61K31/428A61P25/00A61P25/16A61P25/28A61P21/00
CPCC07D417/12
Inventor 赵有志范景辉关富龙张忠民庄亚严
Owner MUDANJIANG MEDICAL UNIV
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