Drug for treatment of cerebral concussion and preparation method thereof

A concussion and drug technology, applied in drug combinations, nervous system diseases, organic chemistry, etc., can solve the problems of professional boxers such as chronic brain atrophy damage, poor brain rehabilitation, and nervous system diseases, and improve the integrity of the blood-brain barrier Sexuality, reduction in the number of damaged neurons, and excellent therapeutic effects

Inactive Publication Date: 2017-07-11
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Most concussions show transient neurological changes, but without timely and effective treatment, repeated and long-term concussions, the pathological changes in the brain tissue are particularly significant, which can cause serious sequelae, and some people die due to concussions. Cases and boxers suffer from chronic brain atrophy and even some serious neurological diseases after

Method used

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  • Drug for treatment of cerebral concussion and preparation method thereof
  • Drug for treatment of cerebral concussion and preparation method thereof
  • Drug for treatment of cerebral concussion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: N-(5,6-dimethyl-2-(1-methyl-1H-pyrazol-4-yl)-3H-imidazol[4,5-b]pyridin-7-yl)- 1,6-dioxohexahydropyrrole[1,2-a]pyrazine-2(1H)-carboxamide (Compound 1)

[0051]

[0052] Step 1: Mix potassium carbonate (2.74g, 20mmol) and 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolane under nitrogen protection -2-yl)-1H-pyrazole (2.23 g, 11 mmol) was added to a round bottom flask. 2-Chloro-5,6-dimethyl-3H-imidazol[4,5-b]pyridin-7-amine (1.96g, 10mmol) was dissolved in 1,4-dioxane (40ml) and water (2ml) and added in aliquots. Nitrogen gas was bubbled through the resulting suspension for about 2 minutes. Then tetrakis(triphenylphosphine)palladium (1.17g, 1mmol) was added in one portion, heated to reflux, and reacted for 10 hours under stirring. The reaction was partitioned between water (200ml) and ethyl acetate (200ml). The aqueous layer was further extracted with ethyl acetate (2×100ml), the combined organic matter was washed with brine (100ml), dried over anhydrou...

Embodiment 2

[0057] Example 2: N-(5-difluoromethyl-2-(1-isopropyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-7-yl)- 1,6-dioxohexahydropyrrole[1,2-a]pyrazine-2(1H)-carboxamide (Compound 2)

[0058]

[0059] Step 1: Under nitrogen protection, potassium carbonate (2.74g, 20mmol) and 1-isopropyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborol Alk-2-yl)-1H-pyrazole (2.59 g, 11 mmol) was added to the round bottom flask. 2-Chloro-5-difluoromethyl-3H-imidazol[4,5-b]pyridin-7-amine (2.18 g, 10 mmol) was dissolved in 1,4-dioxane (40 ml) and water (2ml) and added in aliquots. Nitrogen gas was bubbled through the resulting suspension for about 2 minutes. Then tetrakis(triphenylphosphine)palladium (1.17g, 1mmol) was added in one portion, heated to reflux, and reacted for 10 hours under stirring. The reaction was partitioned between water (200ml) and ethyl acetate (200ml). The aqueous layer was further extracted with ethyl acetate (2×100ml), the combined organics were washed with brine (100ml), dried ove...

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PUM

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Abstract

The invention relates to the technical field of medicine, and in particular, relates to a drug for treatment of cerebral concussion; the drug has the structure represented by the formula I described in the specification. The compound can greatly reduce the EBA content of rats with cerebral concussion, improves the integrity of blood-brain barrier, can reduce the number of damaged neurons and decreases the water content of brain tissues, so the compound has excellent therapeutic effect on cerebral concussion, and can be used for treatment of cerebral concussion.

Description

technical field [0001] The invention relates to a medicine for treating concussion, and also relates to a preparation method of the medicine. Background technique [0002] Concussion is a syndrome in which the head is injured due to external violent blows, falling from a height, or tumbling, which reduces the function of the brainstem reticular structure and affects the function of the spinal cord, resulting in decreased consciousness, muscle tension, and brain reflexes. It is the mildest type of brain injury, and most of it can be cured after treatment. It can occur alone or in combination with other craniocerebral injuries such as intracranial hematoma. The clinical manifestations are disturbance of consciousness: the degree is mild and the time is short, which can be as short as a few seconds or minutes, but not more than half an hour; amnesia of recent events: after waking up, the situation and the injury process can not be recalled, but the things before the injury can ...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/4985A61P25/00
CPCC07D519/00
Inventor 梁绍栋孟祥慧初金玉张万里刘英伟
Owner MUDANJIANG MEDICAL UNIV
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