Patent ID: 7247633

Claim:
A compound of the formula (I): wherein Y and Z represent both nitrogen and X represents CH, forming a pyrimidine derivative, and wherein R 1 and R 2 are each, independently, selected from a group A consisting of or from a group B, consisting of aryl-C 1 -C 6 -alkyl, aryl-C 1 -C 6 -alkoxy, heteroaryl-C 1 -C 6 -alkoxy, aryloxy-C 2 -C 6 -alkoxy, heteroaryloxy-C 2 -C 6 -alkoxy, 1-indanyloxy, 2-indanyloxy, aryloxy, heteroaryloxy, arylthio, heteroarylthio, C 5 -C 6 -cycloalkylthio, C 5 -C 8 -alkoxy, C 5 -C 8 -alkylthio, C 3 -C 6 -alkynyloxy, C 3 -C 6 -alkenyloxy, fluoro-C 2 -C 4 -alkoxy, C 4 -C 8 -cycloalkyloxy, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkoxy, aryl-C 1 -C 4 -alkylthio, heteroaryl-C 1 -C 4 -alkylthio, aryl-C 1 -C 4 -alkylamino, heteroaryl-C 1 -C 4 -alkylamino, heteroaryl and aryl; with the proviso that: (i) R 1 and R 2 are different and are not both selected from group A or group B at the same time; (iii) when X is CH and Z and Y both are nitrogen in formula (I), forming a pyrirnidine derivative, and R 2 is 1-piperazinyl, then R 1 is other than phenoxy, phenyl or phenyl substituted by bromo, and C 5 -C 8 alkoxy; and when R 2 is 4-methylpiperazin-1-yl or 4-(2-hydroxyethyl)piperazin-1-yl, then R 1 is other than 5-nitro-2-furyl; (iv) when X is CH and Z and Y both are nitrogen in formula (I), forming a pyrimidine derivative, and R 1 is 1-piperazinyl, then R 2 is other than C 5 -C 8 alkoxy; and where R 3 is H or C 1-4 -alkyl, allyl, 2-hydroxyethyl, 2-cyanoethyl, or a nitrogen protecting group; R 4 is hydrogen, or C 1-4 alkyl; and wherein any aryl or heteroaryl residue, alone or as part of another group, in R 1 or R 2 may be independently substituted in one or more positions, by C 1-4 -alkyl, C 1-4 -alkoxy, C 1-4 -alkylthio, C 2-4 -acyl, C 1-4 -alkylsulphonyl, cyano, nitro, hydroxy, C 2-6 -alkenyl, C 2-6 -alkynyl, fluoromethyl, trifluoromethyl, trifluoromethoxy, halogen, —N(R 5 )(R 6 ), aryl, aryloxy, arylthio, aryl-C 1-4 -alkyl, aryl-C 2-4 -alkenyl, aryl-C 2-4 -alkynyl, heteroaryl, heteroaryloxy, heteroarylthio or heteroaryl-C 1-4 -alkyl, aryl-C 1-4 -alkoxy, aryloxy-C 1-4 -alkyl, dimethylamino-C 2-4 -alkoxy; and wherein any aryl or heteroaryl residue as substituents on aryl or heteroaryl, alone or as part of another group, in R 1 or R 2 in turn may be substituted in one or more postions, independently of each other by C 1-4 -alkyl, C 1-4 -alkoxy, halogen, trifluoromethyl, cyano, hydroxy or dimethylamino; and R 5 and R 6 independently of each other are hydrogen, methyl or ethyl, or together with the nitrogen atom to which they are bound form a pyrrolidine, piperazine, morpholine, thiomorpholine or a piperidine ring; or a pharmaceutically acceptable salt, geometrical isomer, tautomer, optical isomer, or N-oxide form thereof.