| abstract |
The present invention relates to novel dihydropteridinones of the formula R 1 H, halogen, amino, -XH, or optionally halogenated alkyl; R 2 is H, formyl, -XH or -X-alkyl, or optionally substituted alkyl; R3 and R4 are H, halogen, optionally substituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, -NR8-aryl, -NR8-heteroaryl, -NR8-cycloalkyl, -NR8-heterocycloalkyl, - X-cycloalkyl, -X-heterocycloalkyl, -X-aryl, -X-heteroaryl, -COXR8, -CON (R8) 2, -COR8 and -XR8; or R3 and R4 together form an alkylene bridge containing one or two heteroatoms; R5 is H, optionally substituted alkyl, alkenyl, alkynyl, aryl, heteroaryl or cycloalkyl; or R 3 and R 5 or R 4 and R 5 together form an alkylene bridge containing one or two heteroatoms; R6 is optionally substituted aryl or heteroaryl; R7 is H or -CO-X-alkyl; X0 or S; and R 8 H, optionally substituted alkyl, alkenyl, alkynyl and phenyl and their isomers, acid addition salts, for use in the preparation thereof and in particular for use as an active ingredient in anti-proliferative drugs. HE |