Kinase antagonists

Abstract

The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.

What is claimed is: 
     
         1 . A compound of formula (I) 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein: 
         a) R 1  is unsubstituted alkyl; 
         b) R 2  is substituted aryl, or substituted or unsubstituted heteroaryl; 
         c) R 3  is hydrogen; 
         d) Y is —NH 2 . 
       
     
     
         2 . The compound of  claim 1 , wherein R 1  is unsubstituted C 1 -C 10  alkyl. 
     
     
         3 . The compound of  claim 1 , wherein R 1  is unsubstituted C 1 -C 4  alkyl. 
     
     
         4 . The compound of  claim 1 , wherein R 1  is unsubstituted C 1 -C 3  alkyl. 
     
     
         5 . The compound of  claim 1 , wherein R 1  is methyl, ethyl, n-propyl, or isopropyl. 
     
     
         6 . The compound of  claim 1 , wherein R 2  has a fused ring structure. 
     
     
         7 . The compound of  claim 1 , wherein R 2  is phenyl having the substitution pattern, 
       
         
           
           
               
               
           
         
         wherein the R 2  phenyl is fused at R 4 -R 5 , R 5 -R 6 , R 6 -R 7  or R 7 -R 8  by a substituted or unsubstituted heteroaryl group or a 6-membered heterocyclyl group. 
       
     
     
         8 . The compound of  claim 1 , wherein R 2  is phenyl having the substitution pattern, 
       
         
           
           
               
               
           
         
         wherein the R 2  phenyl is fused at R 4 -R 5 , R 5 -R 6 , R 6 -R 7  or R 7 -R 8  by a substituted or unsubstituted heteroaryl group or a 6-membered heterocyclyl group; and wherein any R 4 -R 8  group that is not part of the fused ring structure is hydrogen. 
       
     
     
         9 . The compound of  claim 7 , wherein the R 2  phenyl is fused at R 5 -R 6  by a substituted or unsubstituted heteroaryl group or a 6-membered heterocyclyl group. 
     
     
         10 . The compound of  claim 7 , wherein the R 2  phenyl is fused at R 5 -R 6  by a substituted or unsubstituted five-membered heteroaryl group. 
     
     
         11 . The compound of  claim 7 , wherein the R 2  phenyl is fused at R 4 -R 5 , R 5 R 6 , R 6 -R 7  or R 7 -R 8  by a heteroaryl group substituted by one or more of hydroxyl, cyano, unsubstituted alkyl, or amino. 
     
     
         12 . The compound of  claim 1 , wherein R 2  is substituted or unsubstituted indolyl, or substituted or unsubstituted benzodioxanyl. 
     
     
         13 . The compound of  claim 1 , wherein R 2  comprises 5-indolyl or 5-benzothiazolyl. 
     
     
         14 . A pharmaceutical composition comprising the compound of  claim 1  or a pharmaceutically acceptable salt thereof. 
     
     
         15 . A compound of formula (I) 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein: 
         a) X is N; 
         b) R 1  is unsubstituted alkyl; 
         c) R 2  is substituted or substituted aryl, or substituted or unsubstituted heteroaryl; and 
         d) R 23  is NH 2 . 
       
     
     
         16 . The compound of  claim 15 , wherein R 1  is unsubstituted C 1 -C 10  alkyl. 
     
     
         17 . The compound of  claim 15 , wherein R 1  is unsubstituted C 1 -C 4  alkyl. 
     
     
         18 . The compound of  claim 15 , wherein R 1  is unsubstituted C 1 -C 3  alkyl. 
     
     
         19 . The compound of  claim 15 , wherein R 1  is methyl, ethyl, n-propyl, or 2 isopropyl. 
     
     
         20 . The compound of  claim 15 , wherein R 2  has a fused ring structure. 
     
     
         21 . The compound of  claim 15 , wherein R 2  is R 4 -substituted aryl, wherein R 4  is unsubstituted heterocycloalkyl. 
     
     
         22 . The compound of  claim 15 , wherein R 2  is substituted or unsubstituted indolyl, or substituted or unsubstituted benzodioxanyl, wherein when indolyl or benzodioxanyl are substituted, the substituent is selected from CN, OR 10  wherein R 10  is hydrogen, unsubstituted alkyl, and NR 12 R 13 , wherein R 12  and R 13  are independently hydrogen or unsubstituted alkyl. 
     
     
         23 . The compound of  claim 15 , wherein R 2  comprises 5-indolyl or 5-benzothiazolyl. 
     
     
         24 . A pharmaceutical composition comprising the compound of  claim 15  or a pharmaceutically acceptable salt thereof.