Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

Abstract

Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

1 - 123 . (canceled)  
     
     
         124 . An amino alcohol of the following formula:  
       
         
           
           
               
               
           
         
       
       where P 1  is hydrogen; 
 P 2  is selected from benzyl and an amino-protecting group;  
 R 2  is selected from alkyl, aryl, cycloalkyl, cycloalkylalkyl and aralkyl,  
 which are optionally substituted with a group selected from alkyl, halogen, nitro, cyano, trifluoromethyl, —OR 9  and —SR 9 , where R 9  is selected from hydrogen, alkyl and halogen and  
 R 3  is selected from hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl, heteroaralkyl, aminoalkyl and mono- and disubstituted aminoalkyl, wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl, or in the case of a disubstituted aminoalkyl, said substituents along with the nitrogen atom to which they are attached, from a heterocycloalkyl or a heteroaryl.  
 
     
     
         125 . The amino alcohol of  claim 124  wherein R 2  is selected from alkyl, aryl, cycloalkyl, cycloalkylalkyl and aralkyl, substituted with a group selected from alkyl, halogen, nitro, cyano, trifluoromethyl, —OR 9  and —SR 9 , where R 9  is selected from hydrogen, alkyl and halogen.  
     
     
         126 . The amino alcohol of  claim 125  wherein R 2  is an aralkyl substituted with a group selected from alkyl, halogen, nitro, cyano, trifluoromethyl, —OR 9  and —SR 9 , where R 9  is selected from hydrogen, alkyl and halogen.  
     
     
         127 . The amino alcohol of  claim 126  wherein R 2  is an aralkyl substituted with one or more halogens.  
     
     
         128 . The amino alcohol of  claim 127  wherein R 3  is selected from alkyl, haloalkyl, alkenyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl and heteroaralkyl.  
     
     
         129 . The amino alcohol of  claim 127  wherein the one or more halogens is fluorine.