Design, synthesis and methods of use of acyclic flexmier nucleoside analogues having anti-coronavirus activity

Abstract

The present invention is directed to compounds, methods and compositions for treating or preventing viral infections using nucleosides analogs. Specifically, the present invention provides for the design and synthesis of acyclic fleximer nucleoside analogues having increased flexibility and ability to alter their conformation structures to provide increased antiviral activity potential with the result of inhibiting several coronaviruses.

That which is claimed is: 
     
         1 . An acyclic fleximer nucleoside analogue having antiviral activity selected from the following compounds: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt, hydrate, prodrug or solvate thereof. 
     
     
         2 . The acyclic fleximer nucleoside analogue according to  claim 1 , for use as a medicine or antiviral medicine with antiviral activity that inhibits or reduces the effects of a coronavirus in a subject. 
     
     
         3 . The acyclic fleximer nucleoside analogue according to  claim 1 , in a composition further comprising a pharmaceutically acceptable carrier. 
     
     
         4 . A method of treating and/or reducing the effects of a coronavirus in a subject in need of such treatment, the method comprising administering a therapeutically effective amount of an acyclic fleximer nucleoside analogue selected from the group consisting of: 
       
         
           
           
               
               
           
         
       
       and a pharmaceutically acceptable salt, isomer, hydrate, prodrug or solvate thereof. 
     
     
         5 . The method of  claim 4 , wherein the acyclic fleximer nucleoside analogue is in a composition further comprising a pharmaceutically acceptable carrier. 
     
     
         6 . The method of  claim 4 , wherein the acyclic fleximer nucleoside analogue is in a composition further comprising an additional antiviral agent. 
     
     
         7 . The method of  claim 4 , wherein the therapeutically effective amount of the acyclic fleximer nucleoside analogue is from 0.05 to 50 mg per kilogram body weight of the subject per day.