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Lipoic acid prodrug

A technology of medicine and composition, applied in the field of lipoic acid prodrugs, can solve the problems of reduced lens elasticity, difficulty in adjusting lens thickness and the like

Pending Publication Date: 2021-11-26
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when the function of the ciliary muscle decreases due to aging or the elasticity (or viscoelasticity) of the lens decreases, that is, the lens hardens, it becomes difficult to adjust the thickness of the lens, and it becomes difficult to focus well when viewing objects.

Method used

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  • Lipoic acid prodrug
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Experimental program
Comparison scheme
Effect test

Embodiment

[0344] The synthesis of compounds, and the results of pharmacological tests, dynamic tests, and safety tests are shown below, but these are for better understanding of the present invention and do not limit the scope of the present invention.

[0345] [Synthesis of Compound]

[0346] Intermediate 1

[0347] 2-(4-(2-((tert-butyldimethylsilyl)oxy)ethyl)piperazin-1-yl)ethan-1-ol (intermediate 1)

[0348] To a solution of 1,4-bis(2-hydroxyethyl)piperazine (CAS No. 122-96-3, 5.00 g, 28.7 mmol) in chloroform (500 mL) was added tert-butyldimethyl at room temperature under nitrogen atmosphere Chlorosilane (4.33g, 28.7mmol) and triethylamine (4.0mL, 28.7mmol), stirred overnight. The reaction solution was concentrated, and the residue was purified twice by silica gel column chromatography (chloroform / methanol=100 / 1 to 5 / 1) to obtain the title intermediate 1 (1.71 g, 21%) as a colorless oily substance .

[0349]

[0350] Intermediate 2

[0351] (R)-5-(1,2-Dithiolan-3-yl)pentanoic...

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Abstract

The present disclosure provides a therapeutic or prophylactic agent for an ophthalmic disease such as presbyopia, said agent comprising, as an active ingredient, a lipoic acid prodrug having a specific structure.

Description

technical field [0001] The present invention relates to a lipoic acid prodrug and an agent for treating or preventing eye diseases such as presbyopia containing the lipoic acid prodrug as an active ingredient. Background technique [0002] Presbyopia is one of the aging phenomena of the eyes that begins around the age of 40. It is also commonly known as presbyopia. According to Non-Patent Document 1, it is defined as a pathological condition in which the adjustment range decreases with age (Age-Related Loss of Accommodation) disease. In order to see near objects, far objects and focus, the light entering the eye needs to be properly refracted when passing through the lens. Therefore, the eye has the function of adjusting the thickness of the lens, such as the contraction of the ciliary muscle located near the lens. The ocular tissues involved in the near-far accommodation response include the lens, Qin's zonules, lens capsule, and ciliary muscle. However, when the function...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P27/02A61P27/10C07D339/04A61K9/06A61K9/08A61K31/385A61K31/496A61K31/5377
CPCA61K9/08A61K31/496A61K31/5377A61P27/02A61P27/10C07D339/04A61K9/0048C07D491/056A61K31/381A61K31/385A61K31/436A61K9/06
Inventor 加藤雅智小田知子高冈慎治本田崇宏畑龙也
Owner SANTEN PHARMA CO LTD