Substituted pyrimidin-2-ones and the salts thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 239/36 (2006.01) C07D 239/38 (2006.01)

Patent

CA 1180710

Abstract Substituted pyrimidin-2-ones and the salts thereof Compounds of the general formula:- Image I (wherein X represents a halogen atom or a trifluoromethyl group; R1 and R2 independently represent a hydrogen atom or a lower alkyl group; Z is -O-, -S-, -SO-, -SO2- or the group -NR4- wherein R4 is as defined for R hereinafter or represents the group COR5 in which R5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group; R represents a C6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group ?NR4, the group -ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and R3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C7-16 aralkyl or C6-10 aryl group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation. The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

393785

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