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Water-soluble positive-charge prodrugs high in skin penetration speed for prostaglandins and compounds of prostaglandins

A prostaglandin and prostacyclin technology, which is applied in the field of prodrugs of positively charged water-soluble prostaglandins and related compounds with fast skin penetration speed, can solve problems such as destruction, inactivation, and pain

Active Publication Date: 2016-05-11
TECHFIELDS BIOCHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Prostaglandins, when administered by injection, are painful and in many cases require frequent and expensive doctor visits to treat chronic disease states, and most prostaglandins, prostacyclins and related compounds do not reach their intended site of action Destroyed and inactivated in the blood and liver

Method used

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  • Water-soluble positive-charge prodrugs high in skin penetration speed for prostaglandins and compounds of prostaglandins
  • Water-soluble positive-charge prodrugs high in skin penetration speed for prostaglandins and compounds of prostaglandins
  • Water-soluble positive-charge prodrugs high in skin penetration speed for prostaglandins and compounds of prostaglandins

Examples

Experimental program
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Effect test

Embodiment approach

[0060] N, the preparation method of N-diethylaminoethyl 11,15-diacetoxy-9-ketone-5,13-prostadienoic acid-1-amide acetate

[0061] 43.7 g (0.1 mol) of 11,15-diacetoxy-9-keto-5,13-prostadienoic acid were dissolved in 300 ml of chloroform. To the reaction mixture was added 20.6 g of N,N'-dicyclohexylcarboimide. To the reaction mixture was added 11.7 g of N,N-diethylaminoethylamine hydrogen bromide. The mixture was stirred at room temperature for 3 hours. The solids were removed by filtration. The chloroform solution was washed twice with 5% aqueous sodium bicarbonate, 100 ml each time, and washed three times with water, 100 ml each time. The organic layer was dried over anhydrous sodium sulfate. Sodium sulfate was removed by filtration. 6 g of acetic acid was added to the reaction mixture with stirring. 200ml of hexane was added. The solid product was collected by filtration. After drying, 45 g of the hygroscopic target product was obtained with a yield of 85.8%. Solubil...

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Abstract

The invention relates to design and synthesis of positive-charge prodrugs, with a structure shown as 'structural formula 2' of general formula (2), for prostaglandins, prostacyclins and relevant compounds. A compound shown as the 'structural formula 2' of the general formula (2) can be obtained by reacting of the prostaglandins, the prostacyclins and the relevant compounds under protection with proper alcohol, mercaptan or amine and coupling agents. The prodrugs can be used for treating any states of people or animals, which can be treated by any of the prostaglandins, the prostacyclins and the relevant compounds. The concentration of the prostaglandins, the prostacyclins and the relevant compounds in blood can be stabilized at the optimum treatment concentration through controlled-release transdermal drug delivery systems of the prodrugs, so that curative effect is enhanced and side effects of the prostaglandins, the prostacyclins and the relevant compounds are reduced. Through transdermal drug delivery of the prodrugs, drug delivery for people, particularly for children, is facilitated substantially.

Description

technical field [0001] The present invention relates to positively charged water-soluble prodrugs of prostaglandins, prostacyclins and related compounds and their use in the treatment of any prostaglandin, prostacyclin and related compounds treatable state in humans or animals. Specifically, the present invention is directed to the rapid penetration of the skin by prostaglandins, prostacyclins and related compounds. Background technique [0002] Natural prostaglandins and prostacyclins are eicosanoid-like compounds that are self-active substances derived from biomembrane phospholipids. They can be found almost anywhere on the body. The basic structure of prostaglandins is shown in structural formula 1. [0003] [0004] All natural prostaglandins have a 15α-hydroxyl group and a C-13 trans double bond (William O. Foye, et al. Principles of Medicinal Chemistry, fourth edition, Williams & Wilkins, 1995, pg538). Chains containing carboxyl groups are called alpha-chains and...

Claims

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Application Information

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IPC IPC(8): C07C405/00A61P27/02A61P27/06A61P15/10A61P15/00A61P9/12A61P15/04A61P9/00A61P7/02A61P11/00A61P1/00
Inventor 于崇曦徐丽娜
Owner TECHFIELDS BIOCHEM CO LTD
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