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Medical use of 5-benzylaminosalicylic acid derivatives or salts thereof

A technology of benzylaminosalicylic acid and aminosalicylic acid is applied in the fields of depression, treatment or prevention of stress disorder and anxiety disorder, and can solve the problems of anticholinergic side effects, suicidal thoughts and extrapyramidal side effects, etc.

Active Publication Date: 2012-01-11
NEUROTECH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tricyclic antidepressants, although very effective, have CNS side effects such as sedation, confusion, delusions, obsessive-compulsive disorder, headache, sleep disturbance and cardiovascular side effects such as orthostatic hypotension, tachycardia, and anticholinergics Potential side effects are a concern
[0006] However, these SSRIs have also been associated with headaches, vomiting, decreased appetite, sexual dysfunction, sleep disturbance, fatigue, weight changes, suicidal thoughts, and extrapyramidal side effects

Method used

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  • Medical use of 5-benzylaminosalicylic acid derivatives or salts thereof
  • Medical use of 5-benzylaminosalicylic acid derivatives or salts thereof
  • Medical use of 5-benzylaminosalicylic acid derivatives or salts thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The antidepressant effect of compound 2 was evaluated by tail suspension test (TST).

[0054] Compound efficacy was evaluated using the tail suspension assay as an in vivo assay for depression. In this experiment, the immobility time of the animal, usually between 5-10 minutes, is recorded using manual or automated equipment. Mice whose tails were suspended showed alternating periods of activity (moving) and immobility, and drugs with antidepressant effects usually reduce immobility time in this experiment.

[0055] Male ICR mice weighing 28-30 g were used in the experiments. Experimental animals were kept in an animal breeding room with a 12-hour dark / 12-hour light cycle, and 8 mice were raised per cage, with free supply of feed and water. Mice consisting of 8 animals per group were randomly assigned to treatment groups.

[0056] Compound 2 was suspended in 10% lutrol solution, and all suspension solutions were orally administered to mice twice a day with a volume ...

Embodiment 2

[0066] Effect of compound 2 in stress model

[0067] 2-1. Induction of water immersion restraint stress (WIRS)

[0068] Sprague-Dawley (SD) rats weighing 200 g were fasted for 24 hours prior to administration of test compounds. After 1 hour, rats were housed in stress cages, and WIRS was induced by placing the cages in water for 10 hours at 24°C.

[0069] 2-2. Effect of compound 2 on gastric injury in stress model

[0070] SD rats with a body weight of 200 g were fasted for 24 hours, and then given 30 mg / kg of compound 2. After 1 hour, the rats were put into a stress cage, and the cage was placed in water for 10 hours. Ten hours after WIRS, the rats were sacrificed under ether anesthesia. Each stomach was excised, soaked and fixed in 10ml 2% formalin solution for 10 minutes, and then cut along the greater curvature of the stomach. After opening the stomach, confirm the hemorrhagic injury caused by stress with the naked eye, and the results are shown in figure 2 .

[0071...

Embodiment 3

[0072] Utilize open field experiment to evaluate the impact of compound 2 on locomotor activity

[0073] Locomotor activity was measured by open field experiments to determine the effect of drug treatment on animal mobility.

[0074] Experimental animals were kept in an animal breeding room with a 12-hour dark / 12-hour light cycle, and 8 mice were raised per cage, with free supply of feed and water. Mice consisting of 8 animals per group were randomly assigned to treatment groups.

[0075] Compound 2 was suspended in 10% lutrol solution, and all suspension solutions were orally administered to mice twice a day with a volume of 5 ml / kg. The control group was treated with only 10% lutrol solution in the same manner. Animals were given all drug or vehicle treatments (n=8 / group) 1 hour before testing.

[0076] 1. Control 1 (medium, 10% lutrol)

[0077] 2. Compound 2, 1.25 mg / kg (twice a day, orally administered)

[0078] 3. Compound 2, 2.5 mg / kg (twice a day, orally administe...

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Abstract

The present invention relates to a pharmaceutical composition useful for the treatment or prevention of stress-related disorders, depression, and anxiety disorders, containing 5-benzylaminosalicylic acid derivatives and / or pharmaceutically acceptable salts thereof as active ingredients. In addition, the present invention relates to a method for treating or preventing stress-related disorders, depression, and anxiety disorders, wherein the method comprises a step for administrating 5-benzylaminosalicylic acid derivatives and / or pharmaceutically acceptable salts thereof to a subject required for treatment.

Description

technical field [0001] The present invention relates to a pharmaceutical composition containing 5-benzylaminosalicylic acid derivatives or pharmaceutically acceptable salts thereof for treating or preventing stress disorder, depression and anxiety disorder. The present invention relates to a method for treating or preventing stress disorder, depression and anxiety disorder, which comprises 5-benzylaminosalicylic acid derivative or a pharmaceutically acceptable salt thereof. Background technique [0002] Stress occurs when a person does not respond appropriately to an emotional or physical threat, and is often accompanied by symptoms such as tissue damage, bleeding, infection, hypoglycemia, pain, and more. And overstress is a cause of mental illnesses such as depression or anxiety disorders. [0003] Depression is a stress-related mental illness with frequent relapses, a tendency to become chronic and serious consequences such as suicide. The main symptoms of depression are...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P25/24A61P25/22A61P25/00
CPCA61K31/167A61K31/192A61K31/196A61P25/00A61P25/18A61P25/22A61P25/24A61K2121/00
Inventor 郭秉周孙善珠卢载成申真熙
Owner NEUROTECH PHARMA
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