Use of tetrahydropyridines in the treatment of sodium channel related disease and disorders

Abstract

The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorised as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.

1 . A method of treating one or more sodium channel related diseases or disorders in an individual, comprising administering to the individual a composition comprising a compound in an amount effective to treat the diseases or disorders, wherein the compound has the following structure (1): 
       
         
           
           
               
               
           
         
       
       its diastereomer, enantiomer, racemic mixture, salts or a combination thereof, wherein R is selected from a group comprising hydrogen, alkyl, alkenyl, alkoxy, halo, nitro, cyano, keto, amino, carboxylate, substituted or unsubstituted phenyls, adjacent rings which share a side with the R-bearing group, or a combination thereof. 
     
     
         2 . The method according to  claim 1 , wherein the R-bearing group is mono-, di-, or tri-substituted. 
     
     
         3 . The method according to  claim 1 , wherein the compound is a threo-diastereomer, a erythro-diastereomer or a mixture of the threo-diastereomer and the erythro-diastereomer. 
     
     
         4 . The method according to  claim 1 , wherein R is one or more substituents selected from the group consisting of hydrogen, halogens, substituted or unsubstituted phenyls, and adjacent rings which share a side with the R-bearing group. 
     
     
         5 . The method according to  claim 1 , wherein R consists of chlorine substituents at positions 3 and 4. 
     
     
         6 . The method according to  claim 1 , wherein R is a p-bromo. 
     
     
         7 . The method according to  claim 1 , wherein R is a p-chloro. 
     
     
         8 . The method according to  claim 1 , wherein R is a p-2-naphthyl. 
     
     
         9 . The method according to  claim 1 , wherein R is an unsubstituted p-phenyl. 
     
     
         10 . The method according to  claim 6 , wherein the compound has the following structure (2): 
       
         
           
           
               
               
           
         
       
     
     
         11 . The method according to  claim 6 , wherein the compound has the following structure (3): 
       
         
           
           
               
               
           
         
       
     
     
         12 . The method according to  claim 6 , wherein the compound comprises mixture of structures (2) and (3). 
     
     
         13 . The method according to  claim 1 , wherein the compound is capable of inhibiting sodium channel conductance. 
     
     
         14 . The method according to  claim 13 , wherein the sodium channels are voltage gated sodium channels. 
     
     
         15 . The method according to  claim 1 , wherein the compound is capable of inhibiting serotonin receptors and reducing the activity of serotonin receptors. 
     
     
         16 . The method according to  claim 1 , wherein the compound is administered orally, parenterally, intramuscularly, intravenously, mucosally or transdermally. 
     
     
         17 . The method according to  claim 1 , wherein the one or more sodium channel related diseases or disorders is selected from the group consisting of hyperactivity related, muscular, bladder, immune system or neurological disorders. 
     
     
         18 . The method according to  claim 17 , wherein the one or more sodium channel related diseases or disorders is selected from the group consisting of autism spectrum disorder (ASD), attention deficit hyperactivity disorder (ADHD), schizophrenia-related hyperactivity, bronchospasm, oesophageal spasm, irritable bowel syndrome (IBS), urinary incontinence, schizophrenia, epilepsy, migraine, and multiple sclerosis. 
     
     
         19 - 22 . (canceled) 
     
     
         23 . The method according to  claim 1 , wherein the one or more sodium channel related diseases or disorders is cancer. 
     
     
         24 . The method according to  claim 1 , wherein the method further includes alleviating one or more symptoms of the one or more sodium channel related diseases or disorders, wherein the symptoms include pain, convulsion and inflammation. 
     
     
         25 - 80 . (canceled)