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Ocular hypotensive agent comprising compound capable of inhibiting histone deacetylase as active ingredient

A deacetylase and inhibitory technology, applied in the field of ocular hypotensive agents, can solve unknown problems and achieve the effect of reducing intraocular pressure

Inactive Publication Date: 2010-02-10
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, the relationship between compounds having HDAC inhibitory activity and morphological changes of trabecular cells, and the relationship between compounds having HDAC inhibitory activity and intraocular pressure lowering effects are still unknown.

Method used

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  • Ocular hypotensive agent comprising compound capable of inhibiting histone deacetylase as active ingredient
  • Ocular hypotensive agent comprising compound capable of inhibiting histone deacetylase as active ingredient
  • Ocular hypotensive agent comprising compound capable of inhibiting histone deacetylase as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

reference example 1

[0256] tert-butyl 2-aminophenylcarbamate (reference compound 1-1)

[0257] Add a THF (50 mL) solution of di-tert-butyl dicarbonate (44 g, 200 mmol) dropwise into a THF (150 mL) solution of o-phenylenediamine (22 g, 200 mmol) and triethylamine (30 mL, 210 mmol), and stir at room temperature 15 hours. The reaction solution was concentrated, and the obtained solid was filtered out with ethyl acetate, and the solid was dried under reduced pressure to obtain 21 g of the title reference compound as a white solid. Separately, the solid obtained by concentrating the filtrate was filtered out with ethyl acetate and dried under reduced pressure to obtain 11 g of the title reference compound as a white solid (yield 76%).

[0258] [Table 1]

[0259]

reference example 2

[0261] N-(2-tert-butoxycarbonylaminophenyl)-5-methoxycarbonylpyridine-2-carboxamide (reference compound 2-1)

[0262] To tert-butyl 2-aminophenylcarbamate (reference compound 1-1, 10g, 50mmol), 5-methoxycarbonylpyridine-2-carboxylic acid (10g, 55mmol) and N-methylmorpholine (11mL, HATU (21 g, 55 mmol) was added to a solution of 100 mmol) in DMF (100 mL), and stirred at room temperature for 20 hours. Water (300 mL) was added and extracted 3 times with ethyl acetate (300 mL). The organic layer was washed with saturated brine (200 mL), and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the precipitated solid was collected by filtration to obtain 15 g of the title reference compound as a light brown solid (yield 79%).

[0263] [Table 2]

[0264]

reference example 3

[0266] N-(2-tert-butoxycarbonylaminophenyl)-5-hydroxymethylpyridine-2-carboxamide (reference compound 3-1)

[0267] Under ice cooling, add Lithium borohydride (2.1 g, 100 mmol), stirred for 3 hours. Water (200 mL) and 1.0 M hydrochloric acid (300 mL) were added under ice-cooling, extracted with ethyl acetate (300 mL), and the organic layer was washed with water (500 mL) and saturated brine (400 mL). After drying over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure. Ethyl acetate (20 mL) and hexane (30 mL) were added to the residue, and the precipitated solid was collected by filtration to obtain 18 g of the title reference compound as a white solid (yield 53%).

[0268] [table 3]

[0269]

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Abstract

The object is to find a novel pharmacological activity of a compound capable of inhibiting an HDAC. The compound capable of inhibiting a histone deacetylase has an excellent ability of changing the cytomorphology of a trabeculara cell and / or an excellent ocular hypotensive activity, and is therefore useful as a prophylactic and / or therapeutic agent for a disease associated with aqueous humor circulation and / or ocular tension, particularly a prophylactic and / or therapeutic agent for glaucoma, ocular hypertension or the like.

Description

technical field [0001] The present invention relates to an ocular hypotensive agent containing at least one compound having a histone deacetylase (hereinafter referred to as "HDAC") inhibitory activity as an active ingredient, which is useful as a medicine. The above compound has the effect of changing the cell morphology of trabecular cells and / or the effect of lowering intraocular pressure, and is useful as a preventive and / or therapeutic agent for diseases related to aqueous humor circulation and / or intraocular pressure. Background technique [0002] The aqueous humor circulation in the eye is closely related to the intraocular pressure, and if the aqueous humor circulation is damaged, the intraocular pressure will be greatly affected. Especially when the aqueous humor circulation is blocked, the intraocular pressure increases, causing glaucoma, ocular hypertension and other diseases related to the aqueous humor circulation or intraocular pressure. [0003] Normally, aqu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/44A61K31/443A61K31/4433A61K31/4436A61K31/4439A61K31/444A61K31/5377A61P27/02A61P43/00C07D213/81C07D401/12C07D405/12C07D405/14C07D409/12C07D417/12C07D413/12
CPCC07D211/32C07D405/12C07D409/12A61K31/5377C07D213/81C07D413/12A61K31/44C07D207/333C07D401/12A61K31/4439A61K31/4436C07D405/14A61K31/444C07D417/12A61K31/443A61K31/4433C07D401/04A61P27/00A61P27/02A61P27/06A61P43/00A61K31/165A61K31/40
Inventor 米田信次藤泽幸史渡边克彦藤河顺子岛崎敦桐原朋子田岛久嗣
Owner SANTEN PHARMA CO LTD
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