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A kind of salicylic acid-based fumarate derivative and its application in the treatment of Parkinson's disease and other neurodegenerative diseases

A technology of salicylic acid-based fumarate and derivatives, which is applied in the field of salicylic acid-based fumarate derivatives to treat Parkinson's disease, and can solve the problems of reducing lymphocyte count and increasing infection in patients taking medicine, etc. achieve good activity

Active Publication Date: 2020-05-15
CHONGQING NEUROPARK BIRSCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, according to the US FDA, DMF can reduce lymphocyte counts, but there is no evidence of increased infections in patients taking the drug

Method used

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  • A kind of salicylic acid-based fumarate derivative and its application in the treatment of Parkinson's disease and other neurodegenerative diseases
  • A kind of salicylic acid-based fumarate derivative and its application in the treatment of Parkinson's disease and other neurodegenerative diseases
  • A kind of salicylic acid-based fumarate derivative and its application in the treatment of Parkinson's disease and other neurodegenerative diseases

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation of embodiment 1 salicylic acid base fumarate derivative

[0049] 1. Protect the carboxyl group on salicylic acid

[0050] Dissolve salicylic acid (45g, 795.9nmol, 1 equivalent) in dimethylformamide (DMF) (450ml), and add N'N-carbonyldiimidazole (63.5g ), stirred at room temperature for 1h, and slowly added DBU (58.5ml) and tert-butanol (63ml) dropwise, then stirred at room temperature for 2h, and the reaction was completed and detected by LC-MS (the product spectrum is as attached figure 1 shown). The reactant was introduced into water (500ml) and extracted three times with ethyl acetate (3*800ml). The organic layers were combined, washed three times with water (3*800ml) and once with brine (1000ml), washed with anhydrous Na 2 SO 4 Drying, filtration, the filtrate was concentrated to no organic solvent, and the concentrate was purified by silica gel column chromatography (petroleum ether: ethyl acetate=100:1 as mobile phase) to obtain the product (52...

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Abstract

The brand-new compound provided by the applicant is a salicylic acid-based fumarate derivative, and its general structural formula (A) is: wherein, in the general structural formula (A), R1 is H + 、Na + 、K + or NH4 + One of the R 2 For the esterification of fumaric acid. It has a general structural formula in which salicylic acid and fumaric acid are combined through an esterification reaction, which is verified by the applicant through experiments. It is proved that the compound has good activity in treating neurodegenerative diseases.

Description

technical field [0001] The invention provides a class of novel compounds, more specifically relates to a salicylic acid-based fumarate derivative and its application in treating Parkinson's disease. [0002] technical background [0003] Neurodegenerative disease is a disease state in which cells and neurons of the brain and spinal cord are lost. The brain and spinal cord are made up of neurons that have different functions, such as controlling movement, processing sensory information, and making decisions. Cells in the brain and spinal cord generally do not regenerate, so excessive damage can be devastating and irreversible. Neurodegenerative diseases are caused by the loss of neurons or their myelin sheath, which worsens over time to lead to dysfunction. Neurodegenerative diseases are phenotypically divided into two groups: those affecting movement, such as cerebellar ataxias, and those affecting memory and associated dementias. [0004] As the population ages, the preva...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C67/29C07C69/60A61K31/222A61P25/16A61P25/00
CPCC07C69/60C07C67/29
Inventor 杨立川鲍比托马斯郭明跃
Owner CHONGQING NEUROPARK BIRSCI CO LTD