Dioxolane analogues of uridine for the treatment of cancer

Abstract

The invention provides compounds of the formula: R 1 is OR 11 , or NR 5 R 5 ′; R 2 is H or F; R 5 is H, C 1 -C 6 alkyl, OH, C(═O)R 6 , O(C═O)R 6 or O(C═O)OR 6 ; R 5 ′ is H or C 1 -C 6 alkyl; R 6 is C 1 -C 6 or C 3 -C 7 cycloalkyl; R 13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R 22 ; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.

1 .- 22 . canceled 
     
     
         23 . A compound represented by formula Ia″: 
       
         
           
           
               
               
           
         
         wherein: 
       
       R 1  is NH 2 ; 
       R 2  is H; 
       R 13  is phenyl optionally substituted in 4 position with halo or C 3 -C 4 -cycloalkyl, or naphthyl; 
       R 15  is methyl; and 
       R 161  and R 162  are the same or different C 1 -C 3 -alkyl; 
       or a pharmaceutically acceptable salt or solvate thereof. 
     
     
         24 . A compound according to claim  1 , wherein R 163  is propyl and R 164  is propyl. 
     
     
         25 . A compound according to claim  1 , wherein R 163  is ethyl and R 164  is ethyl. 
     
     
         26 . A compound according to claim  1 , wherein R 13  is phenyl substituted in the 4 position with bromo or cyclopropyl. 
     
     
         27 . A compound according to claim  1 , which is: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or solvate thereof. 
       
     
     
         28 . A compound according to claim  1 , which is: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or solvate thereof. 
       
     
     
         29 . A compound according to claim  1 , which is: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt or solvate thereof. 
       
     
     
         30 . A pharmaceutical composition comprising the compound according to any one of claims  1  to  7  or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier therefor.