Novel use of sesquiterpene derivative

Inactive Publication Date: 2019-09-26
KOOKMIN UNIV IND ACAD COOP FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to a food composition that can prevent or improve macular degeneration or macular edema caused by vascular leakage in the eye. The composition contains a specific compound (Chemical Formula 1) and its pharmaceutically acceptable salt as the active ingredient. This compound has been found to have beneficial effects on the eye, including reducing the risk of developing these eye conditions and improving their symptoms.

Problems solved by technology

For example, continued increase in blood pressure in in hypertensive patients causes breakdown of the blood-retinal barrier and the damage to the blood-retinal barrier causes retinal edema due to vascular leakage.
The macula lutea is often damaged by macula tumentia following the removal of the eye lens for treatment of cataract.
However, care should be taken to avoid the fovea when irradiating laser because it is extremely vulnerable.
If the fovea is damaged during the operation, the central vision may be impaired.
Also, more than one laser treatments are often necessary to remove the swelling.
Vitrectomy is employed when the laser treatment is ineffective, but this method is often associated with the high risk of tissue invasion which causes postoperative complications.
In addition, the intravitreal administration of steroids often cause postoperative complications.
The administration directly into the vitreous cavity also causes inconvenience of administration, pain and side effects.

Method used

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  • Novel use of sesquiterpene derivative
  • Novel use of sesquiterpene derivative
  • Novel use of sesquiterpene derivative

Examples

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examples

Preparation of methyl 3-[[(1R,2S,4aR,8aS)-1,2,4a,5-tetramethyl-2,3,4,7,8,8a-hexahydronaphthalen-1-yl]methyl]-4,5-dihydroxybenzoate

[0097]A Hyrtios sp. (38 g dry weight) sample preserved in EtOH was extracted completely using MeOH. After evaporating the MeOH extract in vacuo, the remaining residue (15.6 g) was fractionated using water and a CH2Cl2 solvent. The organic phase was evaporated in vacuo and a gum (5.32 g) was obtained. 2.37 g of the gum was subjected to flash chromatography using a Si gel column and using hexane and EtOAc of increasing concentrations as eluents. Some of the resulting fractions were subjected to flash chromatography using a Si gel column and using hexane / EtOAc (100:0 to 50:50). Two UV-positive fractions were obtained and further purified by HPLC (UV detection at 210 nm, eluent 90:10 MeOH / H2O) to obtain a compound of Preparation Example 1 (3 mg).

[0098]The obtained compound of Preparation Example 1 had the following physicochemical properties and was identifi...

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Abstract

The present disclosure relates to a novel use of a sesquiterpene derivative, more particularly to a composition for preventing, improving or treating macular degeneration or macular edema caused by vascular leakage in the eye, the composition containing a sesquiterpene derivative compound represented by Chemical Formula 1 of the present disclosure or a pharmaceutically acceptable salt thereof as an active ingredient. Whereas the intraocular disease-related treating agents available in the market should be injected directly into the vitreous cavity, thus causing pain and side effects, the sesquiterpene derivative compound of the present disclosure is delivered to the target tissue (eye) via different administration routes (oral, intraperitoneal, etc.) other than the intravitreal route. Accordingly, the sesquiterpene derivative compound provides excellent therapeutic effect without being restricted by the administration routes.

Description

TECHNICAL FIELD[0001]The present disclosure relates to a novel use of a sesquiterpene derivative, more particularly to a composition for preventing, improving or treating macular degeneration or macular edema caused by vascular leakage in the eye, the composition containing a sesquiterpene derivative compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.BACKGROUND ART[0002]Macular edema refers to the swelling of the macula lutea. The edema is caused by fluid leaking from the retinal blood vessel. Blood is leaked from weak blood vessel walls and flown into the macula lutea packed with retinal cones which sense color and are responsible for vision during the day. Then, images are blurred at the center or right side of the central region. The vision worsens gradually over several months. All age-related macular degeneration (AMD) is associated with macular edema. Vascular leakage in the eye occurs due to various causes. For exa...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A23L33/10A61P27/02A61K31/145A61K31/136A61K31/235A61K31/122A61K31/196
CPCA61K31/235A23L33/10A61K31/145A61K31/122A23V2002/00A61K31/136A61P27/02A61K31/4184A61K31/196A61K9/00A61K9/06A61K31/015A61K9/0019A61K9/0048A23V2200/30A61K31/423
Inventor OH, SANGTAEK
Owner KOOKMIN UNIV IND ACAD COOP FOUND
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