US2020048182A1PendingUtilityA1

A salicyl fumarate derivative and its application in the treatment of parkinson's disease and other neurodegenerative diseases

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Assignee: CHONGQING NEUROPARK BIOSCIENCE CO LTDPriority: Mar 28, 2017Filed: Mar 9, 2018Published: Feb 13, 2020
Est. expiryMar 28, 2037(~10.6 yrs left)· nominal 20-yr term from priority
Inventors:Lichuan YangBobby ThomasMingyue Guo
C07C 69/60C07C 67/29
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Claims

Abstract

A salicyl fumarate derivative, and its general structural formula (A) is: Wherein the structural formula (A), R 1 is one of H + , Na + , K + or NH4 + . R 2 is one of fumaric acid ester products. It has the general structural formula of the combination of salicylic acid and fumaric acid through esterification reaction. This category of compounds possesses good effects in treatment of neurodegenerative diseases.

Claims

exact text as granted — not AI-modified
1 . A salicyl fumarate derivative wherein: its general structural formula (A) is: 
       
         
           
           
               
               
           
         
         Within the structural formula (A), R 1  is one of H + , Na + , K +  or NH4 + , R 2  is one of fumaric acid ester products. 
       
     
     
         2 . The salicyl fumarate derivative according to  claim 1 , wherein: the esterification of the fumaric acid is one of: mono-methyl fumarate, mono-ethyl fumarate, mono-propyl fumarate, mono-isopropyl fumarate, mono-butyl fumarate, mono-tertbutyl fumarate as described. 
     
     
         3 . The salicyl fumarate derivative according to  claim 2 , wherein: the stated salicyl fumarate derivative is methyl salicyl fumarate, its structural formula is: 
       
         
           
           
               
               
           
         
       
     
     
         4 . The salicyl fumarate derivative according to  claim 2 , wherein: the stated salicyl fumarate derivative is ethyl salicyl fumarate, its structural formula is: 
       
         
           
           
               
               
           
         
       
     
     
         5 . The production method for the described salicyl fumarate derivative according to  claim 1 , wherein:
 1) The esterification reaction of tert-butyl alcohol and salicylic acid is carried out, protecting the carboxyl group of salicylic acid, obtaining intermediate product I;   2) The esterification of intermediate product I and the fumaric acid derivative is carried out, obtaining intermediate product II;   3) The tert-butanol in intermediate product II is removed under acidic condition, obtaining target product III.   The chemical reaction formula is as follows:   
       
         
           
           
               
               
           
         
       
     
     
         6 . A method comprising applying the salicyl fumarate derivative according to  claim 1  to drug production for the treatment of Parkinson's Disease. 
     
     
         7 . A method comprising applying the salicyl fumarate derivative according to  claim 2  to drug production for the treatment of Parkinson's Disease. 
     
     
         8 . A method comprising applying the salicyl fumarate derivative according to  claim 3  to drug production for the treatment of Parkinson's Disease. 
     
     
         9 . A method comprising applying the salicyl fumarate derivative according to  claim 4  to drug production for the treatment of Parkinson's Disease.

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