Novel oxazolidinone derivatives

Abstract

The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

1 .- 21 . (canceled) 
     
     
         22 . A compound having the formula: 
       
         
           
           
               
               
           
         
       
     
     
         23 . A pharmaceutical composition comprising the compound of  claim 22 . 
     
     
         24 . A method of treating a bacterial infection in a subject, comprising administering to the subject the compound of  claim 22 . 
     
     
         25 . The method of  claim 24 , wherein the bacterial infection results from a Gram-positive bacterium. 
     
     
         26 . The method of  claim 24 , wherein the bacterial infection results from a bacterium selected from  Staphylococcus, Enterococcus, Streptococcus, Bacteroides, Clostridium,  and  Mycobacterium.    
     
     
         27 . The method of  claim 24 , wherein the bacterial infection results from a bacterium selected from  Staphylococcus, Enterococcus,  and  Streptococcus.