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Prophylactic or therapeutic agent for optic nerve disorders comprising 4,6-dichloro-1h-indole-2-carboxylic acid derivative or salt thereof as active ingredient

A technology for optic nerve damage and active ingredients, applied in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc., can solve problems such as the prevention or treatment of optic nerve damage without clear and specific records

Inactive Publication Date: 2012-02-08
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, there is no clear and specific description in any of the patent documents on the preventive or therapeutic effects of 4,6-dichloro-1H-indole-2-carboxylic acid derivatives or salts thereof on optic nerve damage

Method used

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  • Prophylactic or therapeutic agent for optic nerve disorders comprising 4,6-dichloro-1h-indole-2-carboxylic acid derivative or salt thereof as active ingredient
  • Prophylactic or therapeutic agent for optic nerve disorders comprising 4,6-dichloro-1h-indole-2-carboxylic acid derivative or salt thereof as active ingredient
  • Prophylactic or therapeutic agent for optic nerve disorders comprising 4,6-dichloro-1h-indole-2-carboxylic acid derivative or salt thereof as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] 1. Experiment using NMDA-induced retinal damage model in rats

[0094] (Evaluation of retinal sections by oral administration of test compound)

[0095] The usefulness (retinal nerve cell death inhibitory effect) of the present compound was evaluated using an NMDA-induced rat retinal injury model (Invest.

[0096] (Preparation method of NMDA induced rat retinal damage model)

[0097] Vaporize 3-4% (V / V) isoflurane, make the rat [Slc: SD, male, about 7 weeks old] inhale the vaporized gas at 1-1.5L air / min, and perform general anesthesia , maintain anesthesia under the conditions of 2-3% (V / V) isoflurane. Thereafter, NMDA (manufactured by Sigma, [product number: M3262]) was dissolved in phosphate buffer solution (hereinafter also referred to as "PBS") to 2 mmol / L, and 5 μL (10 nmol as NMDA) of the resulting solution was dissolved in Administered in the vitreous.

[0098] (Preparation and evaluation method of retinal slices)

[0099] For rats after intravitreal admini...

Embodiment 2

[0125] 2. Experiments using NMDA-induced retinal damage model in rats

[0126] (Quantitative polymerase chain reaction (hereinafter also referred to as "PCR") evaluation after intravitreal administration of test compound)

[0127] (evaluation method of quantitative PCR)

[0128] In the NMDA-induced retinal damage model in rats, the expression level of neurofilament light chain (hereinafter also referred to as "NFL"), which is a major component of optic nerve axons and is important for maintaining the shape of axons, in retinal tissues was used as an index , to evaluate the effectiveness of the test compound.

[0129] (Evaluation method)

[0130]One day after the intravitreal administration of NMDA, 100 mg / kg of pentobarbital sodium injection was intraperitoneally administered to the rats. After general anesthesia, the eyeballs were enucleated and the retina was separated. Homogenize the isolated retina, extract total RNA using QIAzol Lysis Reagent (manufactured by QIAGEN [p...

Embodiment 3

[0156] 1) Tablets (in 150mg)

[0157]

[0158]

[0159] The tablet of the above prescription is coated with 3 mg of a coating agent (for example, coating agents such as hydroxypropylmethylcellulose, polyethylene glycol, talc, titanium oxide, and silicone resin), and the target tablet can be obtained . In addition, desired tablets can also be obtained by appropriately changing the types and / or amounts of the present compound and additives.

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Abstract

Disclosed is a compound useful as a prophylactic or therapeutic agent for optic nerve disorders, an inhibitor of retinal ganglion cell death or an agent for restoring the expression level of a neurofilament light chain, particularly a compound capable of exhibiting the above-mentioned pharmacological activities when administered orally. A 4,6-dichloro-1H-indole-2-carboxylic acid derivative or a salt thereof can significantly inhibit the decrease in the number of cells in a retinal ganglion cell layer of an NMDA-induced rat retinal disorder model when administered to the model orally, and can also restore the decrease in the expression level of a neurofilament light chain in a retina of the model when administered to the model intravitreally (intraocular local administration). Therefore, the compound or a salt thereof is useful as a prophylactic or therapeutic agent for optic nerve disorders, an inhibitor of retinal ganglion cell death or an agent for restoring the expression level of a neurofilament light chain.

Description

technical field [0001] The present invention relates to a preventive or therapeutic agent for optic nerve damage and an inhibitor of retinal nerve cell death comprising at least one of 4,6-dichloro-1H-indole-2-carboxylic acid derivatives or salts thereof as an active ingredient agent, or the expression level restorer of neurofilament light chain. Background technique [0002] The retina is composed of 10 layers including inner limiting membrane, nerve fiber layer, ganglion cell layer, inner plexiform layer, inner granular layer, outer plexiform layer, outer granular layer, outer limiting membrane, photoreceptor cell layer and retinal pigment epithelium, A tissue with a thickness of 0.1 to 0.5 mm, in which there are retinal nerve cells such as visual cells, bipolar cells, ganglion cells, horizontal cells, and amacrine cells. [0003] Retinal nerve cells play an important role in converting light stimuli into electrical signals, receiving and transmitting visual information t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/42A61K31/405A61P27/02C07D403/06
CPCA61K31/405C07D209/42C07D403/06A61P27/02A61P27/06
Inventor 笹冈正显梅本朋子清家寿之景山正明
Owner SANTEN PHARMA CO LTD
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