Use of structurally enhanced fatty acids containing sulphur for preventing and or treating non alcoholic steatohepatitis

Abstract

The present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (II): wherein R 1 , R2, R3, X and Y are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt. More particularly, the present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (I): wherein R2, R 3 , and X, are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt. Further, the present invention relates to a compound of Formula (I) for preventing and/or treating non-alcoholic steatohepatitis, wherein R 2 , R 3 and X are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt.

1 . A compound of Formula (I) 
       
         
           
           
               
               
           
         
         wherein 
         R 2  and R 3  are independently chosen from the group of a hydrogen atom and linear, branched and/or cyclic C 1 -C 6  alkyl groups, with the proviso that R 2  and R 3  are not both hydrogen; 
         X is a carboxylic acid or a derivative thereof, wherein the derivative is a carboxylic ester, a glyceride or a phospholipid; 
         or a pharmaceutically acceptable salt, solvate, or solvate of such salt thereof, 
         for preventing and/or treating non-alcoholic steatohepatitis. 
       
     
     
         2 . The compound according to  claim 1  for use according to  claim 1 , wherein R 2  and R 3  are independently chosen from a hydrogen atom, a methyl group, an ethyl group, a n-propyl group and an isopropyl group. 
     
     
         3 . The compound according to  claim 1 , wherein R 2  and R 3  are independently chosen from C 1 -C 6  alkyl groups. 
     
     
         4 . The compound according to  claim 1 , wherein R 2  and R 3  are ethyl groups. 
     
     
         5 . The compound according to  claim 1 , wherein X is a carboxylic acid. 
     
     
         6 . The compound according to  claim 1 , wherein X is a C 1 -C 6  alkyl ester. 
     
     
         7 . The compound according to  claim 1 , wherein X is chosen from the group of a methyl ester, an ethyl ester, an isopropyl ester, a n-butyl ester and a tert-butyl ester. 
     
     
         8 . The compound according to  claim 1 , wherein X is selected from a methyl ester and an ethyl ester. 
     
     
         9 . The compound according to  claim 1 , wherein X is a glyceride chosen from a triglyceride, a 1,2-diglyceride, a 1,3-diglyceride, a 1-monoglyceride and 2-monoglyceride. 
     
     
         10 . The compound according to  claim 1 , wherein the compound is present in the form of an enantiomer, a diastereomer or a mixture thereof. 
     
     
         11 . The compound according to  claim 1 , wherein the compound is present in its R form, in its S form or in racemic form. 
     
     
         12 . The compound according to  claim 1 , wherein R 2  and R 3  are ethyl groups and X is a carboxylic acid. 
     
     
         13 . The compound according to  claim 1 , wherein said compound is administered in a dose of between about 5 mg to about 2 g per dose. 
     
     
         14 . The compound according to  claim 1 , wherein said compound is administered in a dose of between about 200 mg to about 800 mg per dose. 
     
     
         15 . The compound according to  claim 1 , wherein said compound is administered once daily. 
     
     
         16 . The compound according to  claim 1 , wherein said compound is formulated as a pharmaceutical composition for oral administration. 
     
     
         17 . The compound according to  claim 1 , wherein the pharmaceutical composition is in the form of a gelatin capsule or a tablet. 
     
     
         18 . The compound according to  claim 1 , wherein the pharmaceutical composition further comprises at least one binder, excipient, diluent, or any combinations thereof. 
     
     
         19 . The compound according to  claim 16 , wherein the pharmaceutical composition further comprises an antioxidant. 
     
     
         20 . The compound according to  claim 19 , wherein the antioxidant is chosen from tocopherol, BHA, and BHT, or mixtures thereof. 
     
     
         21 . 2-ethyl-2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenylthio)butanoic acid 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or ester thereof, for preventing and/or treating non-alcoholic steatohepatitis. 
       
     
     
         22 . The compound according to  claim 21 , wherein this is administered in a dose of between about 200 mg to about 800 mg per dose. 
     
     
         23 . A method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (I): 
       
         
           
           
               
               
           
         
         wherein R 2  and R 3  are independently chosen from the group of a hydrogen atom and linear, branched and/or cyclic C 1 -C 6  alkyl groups, with the proviso that R 2  and R 3  are not both hydrogen; X is a carboxylic acid or a derivative thereof, wherein the derivative is a carboxylic ester, a glyceride, or a phospholipid; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt. 
       
     
     
         24 . The method according to  claim 23 , wherein R 2  and R 3  are ethyl groups and X is a carboxylic acid.