Tricyclic tetrahydroquinoline antibacterial agents

Abstract

Described herein are antibacterial compounds of formula I, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.

1 . A compound of formula I: 
       
         
           
           
               
               
           
         
         wherein:
 R 1  is selected from the group consisting of: 
 
       
       
         
           
           
               
               
           
         
         which are optionally substituted with R 2 ;
 R 2  is C 1-6 alkyl or phenyl optionally substituted with halo; 
 X and Y are independently H, halo or C 1-6  alkyl; 
 
         or a salt, solvate, or a hydrate thereof;
 provided that when R 1  is moiety (b) and R 2  is phenyl, at least one of X and Y is halo. 
 
       
     
     
         2 . The compound of  claim 1  wherein X is H or F, Y is H or F or both X and Y are H or F. 
     
     
         3 . The compound of  claim 1  wherein R 2  is methyl or ethyl. 
     
     
         4 . The compound of  claim 1  having formula Ib: 
       
         
           
           
               
               
           
         
       
     
     
         5 . (canceled) 
     
     
         6 . (canceled) 
     
     
         7 . (canceled) 
     
     
         8 . A pharmaceutical composition comprising a compound of  claim 1  and a pharmaceutically acceptable carrier, diluent or excipient. 
     
     
         9 . A bacteriostatic or bactericidal use of a compound of  claim 1  comprising:
 (a) contacting a bacteria with a compound of  claim 1 . 
 
     
     
         10 . The use of  claim 9  wherein (a) occurs in vitro or in vivo. 
     
     
         11 . A use of a compound of  claim 1  or a composition of  claim 1  to treat a bacterial infection in a mammal which comprises: administering an effective amount of a compound of  claim 1  to the mammal. 
     
     
         12 . A use of a compound of  claim 1  to prevent a bacterial infection in a mammal which comprises: administering an effective amount of the compound of  claim 1  to the mammal. 
     
     
         13 . A bacteriostatic or bactericidal use of a composition of  claim 8  comprising:
 (a) contacting a bacteria with a composition of  claim 8 . 
 
     
     
         14 . The use of  claim 13  wherein (a) occurs in vitro or in vivo. 
     
     
         15 . A use of a composition of  claim 8  to treat a bacterial infection in a mammal which comprises: administering an effective amount of a composition of  claim 8  to the mammal. 
     
     
         16 . A use of a composition of  claim 8  to prevent a bacterial infection in a mammal which comprises: administering an effective amount of a composition of  claim 8  to the mammal.