Inhibitors of hiv replication

Abstract

The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.

1 . A compound of formula (I) 
       
         
           
           
               
               
           
         
         wherein: 
         R 1  is CH 3 , CH 2 CH 3 , Cl, Br, CHF 2  or CF 3 ; 
         R 2  is H, OH or F; 
         X is CH 2  or O; 
         provided that when R 1  is CH 3  and R 2  is H, X is O; 
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         2 . A compound according to  claim 1  selected from: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         3 . A compound according to  claim 1  of formula (Ia) 
       
         
           
           
               
               
           
         
         wherein: 
         R 1  is CH 3 , CH 2 CH 3 , Cl, Br, CHF 2  or CF 3 ; 
         R 2  is H, OH or F; 
         X is CH 2  or O; 
         provided that when R 1  is CH 3  and R 2  is H, X is O; 
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         4 . A compound according to  claim 1  selected from: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         5 . A compound according to  claim 1  selected from: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         6 . A pharmaceutical composition comprising a compound as claimed in  claim 1  together with a pharmaceutically acceptable excipient. 
     
     
         7 . A method of treatment of a mammal, including a human being, to treat HIV infection, comprising administering to said mammal an effective amount of a compound as claimed in  claim 1 . 
     
     
         8 . A compound as claimed in  claim 1  in combination with one or more other pharmacologically active agents. 
     
     
         9 . A compound as claimed in  claim 1  in combination with one or more other agents which are useful for the treatment of HIV infection. 
     
     
         10 . A product comprising a compound as claimed in  claim 1  and one or more other pharmacologically active agents as a combined preparation for simultaneous, separate or sequential use in therapy. 
     
     
         11 . A kit comprising two or more pharmaceutical compositions, at least one of which comprises a compound as claimed in  claim 1  together with a pharmaceutically acceptable excipient, and means for separately retaining said compositions.