Pharmaceutical formulations of substituted azaindoleoxoacetic piperazine derivatives with protease inhibitors

Abstract

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

1 . A pharmaceutical formulation which comprises an antiviral effective amount of a compound selected from the group of 
       
         
           
           
               
               
           
         
         including pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier, wherein said compound in said formulation is administered to humans in a dosage range of 1 to 100 mg/kg body weight, and further wherein said formulation comprises another HIV treatment agent selected from the group consisting of protease inhibitors. 
       
     
     
         2 . The formulation of  claim 1 , wherein said compound is administered to humans in a dosage range of 1 to 20 mg/kg body weight. 
     
     
         3 . The formulation of  claim 2 , wherein said compound is administered to humans in a dosage range of 1 to 10 mg/kg body weight. 
     
     
         4 . The formulation of  claim 1 , wherein said formulation is orally administered. 
     
     
         5 . The formulation of  claim 1 , wherein said formulation is administered in divided doses. 
     
     
         6 . The formulation of  claim 4 , wherein said formulation is in the form of a suspension or tablet. 
     
     
         7 . A method of treating HIV infection, which comprises administering to a human in need thereof the compound 
       
         
           
           
               
               
           
         
         in an oral or parenteral formulation, together with another HIV treatment agent selected from the group consisting of protease inhibitors. 
       
     
     
         8 . A method of treating HIV infection, which comprises administering to a human in need thereof the compound 
       
         
           
           
               
               
           
         
         in an oral or parenteral formulation, together with another HIV treatment agent selected from the group consisting of protease inhibitors.