US2016207927A1PendingUtilityA1

Pyrimidine substituted purine compounds as kinase (s) inhibitors

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Assignee: VERASTEM INCPriority: Apr 3, 2009Filed: Aug 18, 2015Published: Jul 21, 2016
Est. expiryApr 3, 2029(~2.7 yrs left)· nominal 20-yr term from priority
A61P 3/10A61P 35/04A61P 9/00A61P 37/08A61P 5/14A61P 37/06A61P 43/00A61P 37/02A61P 7/04A61P 35/00A61P 9/10A61P 7/06A61P 37/00A61P 7/00A61P 35/02A61P 27/02A61P 25/00A61P 29/00C12N 9/1205C07D 487/04A61P 11/06C12Y 207/01137A61P 11/00A61P 21/04A61P 1/16A61P 15/00C07D 473/32A61P 11/02A61P 17/14C12Y 207/11001A61P 17/04C12N 9/12A61P 1/00A61P 19/02A61P 13/08A61P 17/00A61K 31/5377A61P 1/04A61P 13/12A61P 17/06Y02A50/30
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Claims

Abstract

The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure: or a pharmaceutically acceptable salt thereof

Claims

exact text as granted — not AI-modified
1 - 46 . (canceled) 
     
     
         47 . A method of making a compound of Formula (I), the method comprising 
       
         
           
           
               
               
           
         
         reacting a compound of Formula (II) 
       
       
         
           
           
               
               
           
         
         with dimethyl zinc, 
         thereby providing the compound of Formula (I). 
       
     
     
         48 . The method of  claim 47 , wherein the reaction is performed in the presence of a palladium complex. 
     
     
         49 . The method of  claim 48 , wherein the palladium complex is Pd(dppf)Cl 2 . 
     
     
         50 . The method of  claim 47 , wherein the reaction is performed in the presence of a solvent. 
     
     
         51 . The method of  claim 50 , wherein the solvent is dioxane. 
     
     
         52 . The method of  claim 47 , wherein the temperature is about 65° C. 
     
     
         53 . A method of making a compound of the Formula (II), the method comprising 
       
         
           
           
               
               
           
         
         reacting a compound of the Formula (III) with N-Bromosuccinimide, 
         thereby providing the compound of Formula (II). 
       
     
     
         54 . The method of  claim 53 , wherein the reaction is performed in the presence of a solvent. 
     
     
         55 . The method of  claim 54 , wherein the solvent is chloroform. 
     
     
         56 . The method of  claim 53 , wherein the temperature is about 5° C. 
     
     
         57 . A method of making a compound of the Formula (III), the method comprising 
       
         
           
           
               
               
           
         
         reacting a compound of the Formula (IV) with morpholine, 
         thereby providing the compound of Formula (III). 
       
     
     
         58 . The method of  claim 57 , wherein the reaction is performed in the presence of a solvent. 
     
     
         59 . The method of  claim 58 , wherein the solvent is dimethyl acetamide. 
     
     
         60 . The method of  claim 57 , wherein the temperature is around 94° C. 
     
     
         61 . A method of making a compound of the Formula (IV), the method comprising 
       
         
           
           
               
               
           
         
         reacting a compound of the Formula (V) with a compound of the Formula (VI), 
       
       
         
           
           
               
               
           
         
         thereby providing the compound of Formula (IV). 
       
     
     
         62 . The method of  claim 61 , wherein the reaction is performed in the presence of a solvent. 
     
     
         63 . The method of  claim 62 , wherein the solvent is dichloromethane. 
     
     
         64 . The method of  claim 61 , wherein the reaction is performed in the presence of a palladium complex. 
     
     
         65 . The method of  claim 64 , wherein the palladium complex is 1,1′-bis(diphenylphosphino) ferrocene palladium (II) chloride. 
     
     
         66 . The method of  claim 61 , wherein the reaction is performed in the presence of a base. 
     
     
         67 . The method of  claim 61 , wherein the temperature is about 80° C.

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