Intermediate compounds for making dihydropteridinones useful as pharmaceutical compositions

Abstract

Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R 1 -R 5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

1 ) A Compound of formula (II),  
       
         
           
           
               
               
           
         
       
       wherein 
 R 1 , R 2  which are identical or different, denote hydrogen or optionally substituted C 1 -C 6 -alkyl, or  
 R 1  and R 2  together denote a 2- to 5-membered alkyl bridge which optionally contain 1 to 2 heteroatoms,  
 R 3  denotes hydrogen or a group selected from among optionally substituted C 1 -C 12 -alkyl, C 2 -C 12 -alkenyl, C 2 -C 12 -alkynyl and C 6 -C 14 -aryl, or a group selected from among optionally substituted and/or bridged C 3 -C 12 -cycloalkyl, C 3 -C 12 -cycloalkenyl, C 7 -C 12 -polycycloalkyl, C 7 -C 12 -polycycloalkenyl, C 5 -C 12 -spirocycloalkyl, C 3 -C 12 -heterocycloalkyl which contains 1 to 2 heteroatoms, and C 3 -C 12 -heterocycloalkenyl which contains 1 to 2 heteroatoms, or  
 R 1  and R 3  or R 2  and R 3  together denote a saturated or unsaturated C 3 -C 4 -alkyl bridge which optionally contain 1 heteroatom,  
 and A is a leaving group chosen from: -o-methyl, —SCN, chlorine, bromine, iodine, methanesulphonyl, trifluoromethanesulphonyl and p-toluenesulphonyl.  
 
     
     
         2 ) The Compound according to  claim 1 , wherein 
 R 1 , R 2  which are identical or different, denote a group selected from among hydrogen, Me, Et, Pr, or    R 1  and R 2  together form a C 2 -C 4 -alkyl bridge.    
     
     
         3 ) The Compound according to  claim 1 , wherein 
 R 3  denotes a group selected from among optionally substituted C 1 -C 10 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 6 -heterocycloalkyl and C 6 -C 14 -aryl or    R 1  and R 3  or R 2  and R 3  together denote a saturated or unsaturated C 3 -C 4 -alkyl bridge which optionally contain 1 to 2 heteroatoms.