Therapeutic agent for meibomian gland dysfunction

a meibomian gland and therapeutic agent technology, applied in the field of meibomian gland dysfunction therapy agent, can solve the problems of lowering the quality of life of many patients, not knowing the effective treatment method of mgd, and not being clear for those skilled in the ar

Inactive Publication Date: 2016-01-28
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The compound described in this patent is useful for treating a condition called meibomian gland dysfunction. The compound has specific groups that make it effective in preventing or treating this condition.

Problems solved by technology

In Non-Patent Document 1, it has been disclosed that among the patients visiting ophthalmology who appeal symptoms such as ocular discomfort, as a main complaint, meibomian gland dysfunction (hereinafter also referred to as “MGD”) becomes a cause thereof in a significant proportion, and lowering in quality of life is caused in many patients.
However, it has never been known an effective treatment method of MGD, and yet, clear definition for MGD or diagnostic criteria itself has never been present in the first place.
However, in Patent Document 1, it has never been disclosed whether the mTOR inhibitor has a treatment effect on MGD or not.
In addition, it is also not clear for those skilled in the art whether or not a medicament which can treat dry eye or posterior blepharitis can prevent and / or treat MGD itself.

Method used

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  • Therapeutic agent for meibomian gland dysfunction
  • Therapeutic agent for meibomian gland dysfunction
  • Therapeutic agent for meibomian gland dysfunction

Examples

Experimental program
Comparison scheme
Effect test

examples

Test Using Complete Freund's Adjuvant Administered Rabbit

[0102]In a complete Freund's adjuvant administered rabbit, telangiectasia around the meibomian gland orifices, and obstruction at the meibomian gland orifices, which are similar to the signs / findings of MGD can be recognized. Effects of sirolimus which was a representative example of the present compound on the telangiectasia and obstruction were investigated (see JP 2014-024835A).

[0103](Sample Preparation)

[0104]0.1% (w / v) sirolimus suspension: it was prepared by suspending in 0.01% (w / v) hydroxypropylmethyl cellulose. Incidentally, with regard to sirolimus, that purchased from LKT Laboratories, Inc., (Catalog number: R0161) was used (which is the same in the following Examples).

[0105](Test Method)

[0106]10 μL of the complete Freund's adjuvant was administered to the right upper eyelid (3 portions) of about 2 kg of male Japanese white rabbits, respectively. After 4 days from provocation, around the meibomian gland orifices of t...

preparation examples

[0125]The drugs of the present invention are more specifically explained by referring to Preparation examples, but the present invention is not limited by these Preparation examples alone.

prescription example 1

Eye Drop (0.1% (w / v))

[0126]

In 100 mlSirolimus0.1gMedium chain fatty acid triglyceride (MCT)7.5gBenzalkonium chloride0.2gTyloxapol1.2gPoloxamer 1881gGlycerin22.5gSterile purified waterq.s.

[0127]To sterile purified water are added sirolimus and the above-mentioned components other than these, and the mixture is thoroughly mixed to prepare an eye drop. Characteristics of the present eye drop is an emulsion. By changing the formulation amount of the sirolimus, eye drops with the concentration of the sirolimus of 0.05% (w / v), 0.5% (w / v) or 1% (w / v) can be prepared.

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Abstract

A compound represented by the formula (1):wherein R1 represents a hydroxyl group, a dimethylphosphynoyloxy group, etc.; and R2 and R3 represent a methoxy group, etc.,or a pharmaceutically acceptable salt thereof can reduce a score of telangiectasia around the meibomian gland orifices and a number of obstruction at the orifices, so that it is useful as a prophylactic and / or therapeutic agent for meibomian gland dysfunction.

Description

TECHNICAL FIELD[0001]The present invention relates to a prophylactic and / or therapeutic agent for meibomian gland dysfunction containing a compound represented by the formula (1):wherein[0002]R1 represents a hydroxyl group, a methoxy group, a hydroxymethoxy group, an ethoxy group, a 1-hydroxyethoxy group, a 2-hydroxyethoxy group, a 2-methoxyethoxy group, a 2-ethoxyethoxy group, a formyloxy group, a carboxyoxy group, an acetoxy group, a hydroxyacetoxy group, a propionyloxy group, a 2-hydroxypropionyloxy group, a 3-hydroxypropionyloxy group, a 2-methylpropionyloxy group, a 2-(hydroxymethyl)-propionyloxy group, a 3-hydroxy-2-(hydroxymethyl)propionyloxy group, a 2,2-dimethylpropionyloxy group, a 2-(hydroxymethyl)-2-methylpropionyloxy group, a 2,2-bis(hydroxymethyl)propionyloxy group, a methylphosphynoyloxy group, a dimethylphosphynoyloxy group or a 1H-tetrazol-1-yl group;[0003]R2 represents a hydrogen atom, a hydroxyl group, a methoxy group, a mercapto group or a methylthio group;[0004]...

Claims

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Application Information

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IPC IPC(8): A61K31/436A61K9/00A61K31/675
CPCA61K31/436A61K9/0048A61K31/675A61P27/02A61P27/04A61P9/00A61P9/14A61P9/06A61K31/453A61K9/10A61K9/107
Inventor MIYAKE, HIDEKIODA, TOMOKOSHII, DAISUKE
Owner SANTEN PHARMA CO LTD
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