Deferasirox-tacrine metal ion chelating agent and pharmaceutical use thereof

A metal ion, tacrine technology, applied in the field of medicine and chemical industry, can solve the problems of metal ion loss and redistribution, danger, enzyme activity inhibition, etc., and achieve the effect of improving utilization efficiency and therapeutic effect

Inactive Publication Date: 2015-08-05
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term treatment with such metal chelators has risks, such as depletion and redistrib...

Method used

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  • Deferasirox-tacrine metal ion chelating agent and pharmaceutical use thereof
  • Deferasirox-tacrine metal ion chelating agent and pharmaceutical use thereof
  • Deferasirox-tacrine metal ion chelating agent and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0037] Example 1-1 Preparation of 9-chloro-1,2,3,4-tetrahydroacridine (compound 3)

[0038] Anthranilic acid (3.2g, 23mmol) and cyclohexanone (2.26mL, 23mmol) were placed in an ice bath, and 69mmol of POCl was slowly added dropwise with a constant pressure dropping funnel 3 into the above mixture, stirring as you add. After the dropwise addition, the ice bath was removed, the above solution was heated to reflux, reacted for 3h, then cooled to room temperature, and unreacted POCl was distilled off under reduced pressure. 3 , the residue was diluted with ethyl acetate, neutralized with anhydrous potassium carbonate, washed with brine (3*100 mL). The organic layer was dried over anhydrous sodium sulfate, evaporated to dryness, and column chromatography gave 4.6 g of light yellow solid 3 with a yield of 91%. Mp 67–69°C.

Embodiment 1-2

[0039] Example 1-2 Preparation of 9-chloro-1,2,3,4-tetrahydroacridine (compound 3)

[0040] Anthranilic acid (3.2g, 23mmol) and cyclohexanone (2.26mL, 23mmol) were placed in an ice bath, and 92mmol of POCl was slowly added dropwise with a constant pressure dropping funnel 3 into the above mixture, stirring as you add. After the dropwise addition, the ice bath was removed, the above solution was heated to reflux, reacted for 2h, then cooled to room temperature, and unreacted POCl was distilled off under reduced pressure. 3 , the residue was diluted with ethyl acetate, neutralized with anhydrous potassium carbonate, washed with brine (3*100 mL). The organic layer was dried over anhydrous sodium sulfate, evaporated to dryness, and column chromatography gave 3 as a pale yellow solid. Mp 67–69°C.

Embodiment 1-3

[0041] Example 1-3 Preparation of 9-chloro-1,2,3,4-tetrahydroacridine (compound 3)

[0042] Anthranilic acid (3.2g, 23mmol) and cyclohexanone (2.26mL, 23mmol) were placed in an ice bath, and 115mmol of POCl was slowly added dropwise with a constant pressure dropping funnel 3 into the above mixture, stirring as you add. After the dropwise addition, the ice bath was removed, the above solution was heated to reflux, reacted for 4h, then cooled to room temperature, and unreacted POCl was distilled off under reduced pressure. 3 , the residue was diluted with ethyl acetate, neutralized with anhydrous potassium carbonate, washed with brine (3*100 mL). The organic layer was dried over anhydrous sodium sulfate, evaporated to dryness, and column chromatography gave a light yellow solid. Mp 67–69°C.

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PUM

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Abstract

The invention provides a deferasirox-tacrine metal ion chelating agent, the structural formula of which is shown as formula I. The invention also provides a preparation method of the deferasirox-tacrine metal ion chelating agent and application of the chelating agent in preparation of drugs treating Alzheimer's disease. According to the invention, deferasirox and tacrine are connected together through carbon chains of different lengths, the metal-chelating properties and antioxidant properties of deferasirox are reserved, and the connected tacrine matrix retains the original acetylcholine esterase inhibitory activity. The obtained novel ion chelating agent has multiple functions and can act on multiple target points. (formula I).

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a deferasino-tacrine metal ion chelating agent and its medicinal application. Background technique [0002] The latest census shows that there are 130 million elderly people over the age of 60 in my country, and my country has entered an aging society ahead of schedule, while Alzheimer's Disease (AD) and Parkinson's Disease (Parkinson's Disease, PD) The number of sick people has reached more than 15 million. By 2050, my country's elderly population will reach 439 million, accounting for 1 / 4 of the total population. Population aging and neurodegenerative diseases create enormous stress and challenges for society, families and the medical community. Currently, AD is a common but incurable neurodegenerative disease that affects a considerable proportion of the elderly. In people over 65 years old, the incidence of AD is 5%; in people over 80 years old, the...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61P25/28
CPCC07D401/12
Inventor 吉民杨悦蔡进张入仁陈峻青
Owner SOUTHEAST UNIV
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