Positively charged aryl and heteroaryl acetate prodrugs with fast skin penetration

A technology of acetic acid and phenylacetic acid, applied in the field of positively charged aryl and heteroaryl acetic acid prodrugs with fast skin penetration rate, which can solve the problem of slow skin penetration rate

Active Publication Date: 2016-09-28
TECHFIELDS BIOCHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the slow rate of skin penetration of these drugs, it is difficult to achieve therapeutically effective plasma concentrations by means of formulations

Method used

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  • Positively charged aryl and heteroaryl acetate prodrugs with fast skin penetration
  • Positively charged aryl and heteroaryl acetate prodrugs with fast skin penetration
  • Positively charged aryl and heteroaryl acetate prodrugs with fast skin penetration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0063] Synthesis of 1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid diethylaminoethyl acetate

[0064] 28.6 g (0.1 mol) of 1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetyl chloride was dissolved in 100 ml of chloroform. The mixture was cooled to 0 °C. 15 ml of triethylamine and 8.9 g (0.1 mol) of diethylaminoethanol were added to the reaction mixture, and stirred at room temperature for 3 hours. The solvent was evaporated to dryness. The residue was dissolved in 300ml of methanol, 200ml of 5% sodium bicarbonate solution was added, and stirred for 3 hours. The mixture was evaporated to dryness. 300 ml of methanol were added to the residue with stirring. The solid was removed by filtration and washed with methanol. The filtrate was evaporated to dryness, and the residue was dissolved in 200 ml of chloroform. 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 acid was added to the re...

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Abstract

The invention relates to prodrug compounds disclosed as structural formula 1, a pharmaceutical composition and a preparation method thereof, and application of the compounds or composition thereof in preparing drugs for treating medicable states of non-steroid anti-inflammatory agents in humans or animals. The invention also discloses a transdermal therapy application system comprising the compounds or pharmaceutical composition thereof.

Description

[0001] Divisional statement [0002] This application is a divisional application of a Chinese patent application filed on August 8, 2006 with the application number 200680055559.8 and the invention title "Positively charged aryl and heteroaryl acetic acid prodrugs with fast skin penetration speed" . technical field [0003] The present invention relates to positively charged and water soluble prodrugs of aryl and heteroaryl acetates and their use in the treatment of any nonsteroidal anti-inflammatory drug (NSAIAs) treatable condition in humans or animals. Specifically, the present invention aims to overcome the side effects caused by non-steroidal anti-inflammatory drugs. These prodrugs can be administered orally or transdermally. technical background [0004] 1-Methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid (Tometine), 5-(4-chlorobenzoyl)-1,4-dimethyl-1H -Pyrrole-2-acetic acid (Zomenic acid), 1,8-Diethyl-1,3,4,9-tetrahydropyran-[3,4-b]indole-1-acetic acid (Etodolac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/337C07D209/28C07D491/052C07C219/10C07C317/44A61K31/40A61K31/405A61K31/407A61K31/216A61P29/00A61P35/00A61P1/08A61P25/00A61P27/02A61P27/06A61P27/16A61P19/02A61P19/10A61P17/00A61P25/06A61P11/06
CPCC07C219/10C07C317/44C07D207/337C07D209/28C07D491/052
Inventor 于崇曦徐丽娜
Owner TECHFIELDS BIOCHEM CO LTD
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