Substituted benzazinones as antibacterial compounds

Abstract

corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.

What is claimed is: 
     
         1 . A method of treating a bacterial infection comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the structure 
       
         
           
           
               
               
           
         
       
       a prodrug thereof, or a pharmaceutically acceptable salt thereof. 
     
     
         2 . The method according to  claim 1 , wherein the bacterial infection is caused by Gram negative bacteria. 
     
     
         3 . The method according to  claim 1 , wherein the bacterial infection is an airway infection, urinary system infection, resipiratory system infection, intra-abdominal infection, sepsis infection, skin infection, nephritis, cholecystitis, oral cavity infection, endocarditis, pneumonia, bone marrow membrane myelitis, otitis media, enteritis, empyema, wound infection or an opportunistic infection. 
     
     
         4 . The method according to  claim 2 , wherein the Gram negative bacteria are selected from Gram negative bacteria of enterobacteria, Gram negative bacteria colonized in respiratory, Gram negative bacteria of glucose non fermentation, or drug resistant Gram negative bacteria. 
     
     
         5 . The method according to  claim 4 , wherein:
 the Gram negative bacteria of Enterobacteriaceae are selected from  Escherichia, Klebsiella, Serratia, Enterobacter, Citrobacter, Morganella, Salmonella, Shigella, Providencia , or  Proteus;      the Gram negative bacteria colonized in respiratory system are selected from  Haemophilus  or  Moraxella;      the Gram negative bacteria of glucose non fermentation are selected from  Pseudomonas aeruginosa, Pseudomonas  other than  P. aeruginosa, Stenotrophomonas, Burkholderia , or  Acinetobacter ; and   the drug resistant Gram negative bacteria are selected from Carbapenem-Resistant Enterobacteriaceae producing bacteria.   
     
     
         6 . A method for inhibiting activity of LpxC in bacteria comprising contacting the bacteria with an effective amount of a compound having the structure 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         7 . The method according to  claim 6 , wherein the bacteria are Gram negative bacteria. 
     
     
         8 . The method according to  claim 7 , wherein the Gram negative bacteria are selected from Gram negative bacteria of enterobacteria, Gram negative bacteria colonized in respiratory, Gram negative bacteria of glucose non fermentation, or drug resistant Gram negative bacteria. 
     
     
         9 . The method according to  claim 8 , wherein:
 the Gram negative bacteria of Enterobacteriaceae are selected from  Escherichia, Klebsiella, Serratia, Enterobacter, Citrobacter, Morganella, Salmonella, Shigella, Providencia , or  Proteus;      the Gram negative bacteria colonized in respiratory system are selected from  Haemophilus  or  Moraxella;      the Gram negative bacteria of glucose non fermentation are selected from  Pseudomonas aeruginosa, Pseudomonas  other than  P. aeruginosa, Stenotrophomonas, Burkholderia , or  Acinetobacter ; and   the drug resistant Gram negative bacteria are selected from Carbapenem-Resistant Enterobacteriaceae producing bacteria.