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Prodrugs of positively charged water-soluble diflunisal and related compounds

A compound and composition technology, applied in the field of prodrugs of positively charged water-soluble diflunisal and related compounds, can solve problems such as the treatment level of difficult diflunisal

Active Publication Date: 2019-07-23
TECHFIELDS BIOCHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is difficult to achieve therapeutically effective plasma concentrations of diflunisal by means of formulations

Method used

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  • Prodrugs of positively charged water-soluble diflunisal and related compounds
  • Prodrugs of positively charged water-soluble diflunisal and related compounds
  • Prodrugs of positively charged water-soluble diflunisal and related compounds

Examples

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Embodiment approach

[0067] 1. the synthetic method of diethylaminoethyl salicylate salicylate acetate

[0068] 31.8 g (0.1 mol) of acetylsalicyloyl salicylic acid chloride were dissolved in 100 ml of chloroform. The mixture was cooled to 0 °C. To the reaction mixture were added 15 ml of triethylamine and 8.9 g (0.1 mol) of dimethylaminoethanol. The mixture was stirred at room temperature for 3 hours. The reaction solvent was distilled off. The residue was dissolved in 300 ml of methanol, and 200 ml of 5% aqueous sodium bicarbonate was added to the reaction mixture. The mixture was stirred for 3 hours. The mixture was evaporated to dryness, and 300 ml of methanol were added to the residue with stirring. The solid was removed by filtration and washed with methanol. The solution was evaporated to dryness, and 200 ml of chloroform was added to the residue. 6 g of acetic acid was added to the reaction mixture with stirring. The solids were removed by filtration. An additional 6 g of acetic ac...

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Abstract

The present invention relates to novel positively charged diflunisal, salicyl salicylic acid and prodrugs of salicylic acid shown in general formula (1) "structural formula 1" and general formula (2) "structural formula 2" design and synthesis. The compounds in the above general formula (1) "structural formula 1" and general formula (2) "structural formula 2" can be prepared by reacting diflunisal, salicyl salicylic acid or salicylic acid with appropriate alcohols, mercaptans, or amines have to. These prodrugs can be used medicinally in the treatment of any diflunisal, salicylsalicylic acid or salicylic acid treatable state in humans or animals, not only by oral administration but also by transdermal administration in the treatment, thereby avoiding the Most side effects of diflunisal, salicylsalicylic acid, or salicylic acid were eliminated. The controlled-release transdermal drug delivery system of the prodrug can stabilize the blood drug concentration of diflunisal, salicylsalicylic acid or salicylic acid at the optimal therapeutic level, thereby improving the curative effect and reducing diflunisal, salicylsalicylic acid or salicylic acid. Salicylic acid side effects.

Description

[0001] This application is a divisional application of the Chinese invention patent application No. 200680055458.0. The filing date of the original application was July 26, 2006, and the title of the invention was "Prodrugs of Positively Charged Water-Soluble Diflunisal and Related Compounds with Rapid Skin Penetration Speed". technical field [0002] The present invention relates to positively charged water-soluble prodrugs of 5-(2,4-difluorophenyl)salicylic acid (diflunisal), salicylsalicylic acid or other salicylic acid analogues and their use in the treatment of Any use of diflunisal, salicylsalicylic acid and salicylic acid in treating diseases in humans or animals. Specifically, the present invention is to overcome the side effects brought by the use of diflunisal, salicyl salicylate or salicylic acid. These prodrugs can be administered orally or transdermally. [0003] technical background [0004] Diflunisal and salicylsalicylic acid are two of the many salicylic ac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C219/14C07C229/12C07C327/30C07C213/06C07C227/18A61K31/255A61K31/235A61P29/00A61P27/02A61P27/06A61P27/16A61K9/70A61K9/72A61P11/06A61P17/00A61P17/10A61P35/00A61P25/06A61P19/00A61P15/00A61P19/02A61P1/08
Inventor 于崇曦徐丽娜
Owner TECHFIELDS BIOCHEM CO LTD
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