(2r)-1-(3-chloro-2-pyrazinyl)-2-methylpiperazine and salts thereof

Abstract

The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R 1 -R 4 are each independently selected from the group consisting of hydrogen, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, and di-C 1 -C 6 -alkylamino-C 2 -C 6 -alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.

1 - 34 . (canceled) 
     
     
         35 . A method for treating or preventing a serotonin-related disorder in a mammal comprising administering to the mammal a therapeutically effective amount of a pharmaceutical composition comprising a compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein R 1 -R 4  are hydrogen and HA is L-malic acid; 
         and a pharmaceutically acceptable carrier. 
       
     
     
         36 . The method of  claim 35 , wherein the serotonin-related disorder is a 5-HT2C-receptor related disorder. 
     
     
         37 . The method of  claim 35 , wherein the serotonin-related disorder is obesity or type II diabetes. 
     
     
         38 . The method of  claim 35 , wherein the mammal is a human. 
     
     
         39 . The method of  claim 35 , wherein treating the serotonin-related disorder comprises alleviating at least one symptom of the serotonin-related disorder. 
     
     
         40 . The method of  claim 35 , wherein the pharmaceutical composition is administered orally. 
     
     
         41 . The method of  claim 35 , wherein the pharmaceutical composition is administered parenterally. 
     
     
         42 . A method of treating obesity in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein R 1 -R 4  are hydrogen and HA is L-malic acid; 
         and a pharmaceutically acceptable carrier. 
       
     
     
         43 . The method of  claim 42 , wherein the pharmaceutical composition is administered orally. 
     
     
         44 . The method of  claim 42 , wherein the subject is a human. 
     
     
         45 . A method of treating type II diabetes in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein R 1 -R 4  are hydrogen and HA is L-malic acid; 
         and a pharmaceutieally acceptable carrier. 
       
     
     
         46 . The method of  claim 45 , wherein the pharmaceutical composition is administered orally. 
     
     
         47 . The method of  claim 45 , wherein the pharmaceutical composition is administered parenterally. 
     
     
         48 . The method of  claim 45 , wherein the subject is a human.