QUINAZOLINONE DERIVATIVES

摘要

A compound of formula (1), wherein: X is an oxygen or sulfur atom; R<1> is an aliphatic, cycloaliphatic or cycloalkyl-alkyl- group; R<2> is an optionally substituted heteroaromatic group or a -CN group; R<3> is a group -(Alk<1>)mL<1>(AIk<2>)nR<4> in which m and n, which may be the same or different, is each zero or the integer 1, Alk<1> and AIk<2>, which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L<1> is a covalent bond or a linker atom or group and R<4> is a hydrogen atom or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; A is an optionally substituted cycloaliphatic or heterocycloaliphatic group optionally fused to an optionally substituted aryl or heteroaryl group; R<5>, which may be attached to any available C or N atom present in the cycloaliphatic or heterocycloaliphatic, or where fused, aryl or heteroaryl group, is a group -(AIk<3>)tL<2>(AIk<4>)vR<6> in which t and v, which may be the same or different, is each zero or the integer 1, Alk<3> and AIk<4>, which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain, L<2> is a covalent bond or a linker atom or group and R<6> is a hydrogen or halogen atom or a -CN group or an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates, tautomers, isomers or N-oxides thereof. The compounds of the present invention are potent inhibitors of IMPDH.