Inhibition of activated cdc42-associated kinase 1

Abstract

Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.

We claim: 
     
         1 . A compound of Formula I: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof,
 wherein each of R 1  and R 2  is selected from the group consisting of: R 4 —O—, H, 
 
       
         
           
           
               
               
           
         
       
       and
 R 3  is 
 
       
         
           
           
               
               
           
         
         wherein R 4  is a C 1 -C 6  alkyl or H;
 R 5  is a C 3 -C 8  cycloalkyl, benzyl, 
 
       
       
         
           
           
               
               
           
         
         and
 R 6  is F, Cl, or OMe; and 
 
         R 7  is a C 1 -C 3  alkyl, provided that when R 1  is H 3 CO— and R 2  is morpholino, R 5  is not cyclopropyl or 
       
       
         
           
           
               
               
           
         
       
       where R 7  is methyl, and provided that when R 1  and R 2  are each hydrogen, R 3  is not 
       
         
           
           
               
               
           
         
       
       where R 5  is benzyl. 
     
     
         2 . The compound of  claim 1 , wherein R 1  is H 3 CO—; R 2  is 
       
         
           
           
               
               
           
         
       
       and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         3 . The compound of  claim 1 , wherein R 1  is H 3 CO—; R 2  is 
       
         
           
           
               
               
           
         
       
       and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         4 . The compound of  claim 1 , wherein R 1  is H 3 CO—; R 2  is 
       
         
           
           
               
               
           
         
       
       and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         5 . The compound of  claim 1 , wherein R 1  is 
       
         
           
           
               
               
           
         
       
       R 2  is H 3 CO—; and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         6 . The compound of  claim 1 , wherein R 1  is H; R 2  is H; and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         7 . The compound of  claim 1 , wherein R 1  is H 3 CO—; R 2  is 
       
         
           
           
               
               
           
         
       
       and R 3  is 
       
         
           
           
               
               
           
         
       
     
     
         8 . A composition, comprising the compound of  claim 1  and a carrier. 
     
     
         9 . The composition of  claim 8 , wherein the carrier is a pharmaceutically acceptable carrier. 
     
     
         10 . A composition, comprising the compound of  claim 2  and a carrier. 
     
     
         11 . The composition of  claim 10 , wherein the carrier is a pharmaceutically acceptable carrier. 
     
     
         12 . A composition, comprising the compound of  claim 3  and a carrier. 
     
     
         13 . The composition of  claim 12 , wherein the carrier is a pharmaceutically acceptable carrier. 
     
     
         14 . A composition, comprising the compound of  claim 4  and a carrier. 
     
     
         15 . The composition of  claim 14 , wherein the carrier is a pharmaceutically acceptable carrier. 
     
     
         16 . A composition, comprising the compound of  claim 6  and a carrier. 
     
     
         17 . The composition of  claim 16 , wherein the carrier is a pharmaceutically acceptable carrier. 
     
     
         18 . A composition, comprising the compound of  claim 7  and a carrier. 
     
     
         19 . The composition of  claim 18 , wherein the carrier is a pharmaceutically acceptable carrier.