NOVEL PARP INHIBITORS

摘要

Compounds represented by the general formula (Iota) and salts thereof; and medicinal compositions containing the same as the active ingredient: [wherein R<1> is H, halogeno, OH, amino, C1-4 alkyl which may be substituted with one to five halogen atoms, or C1-4 alkoxy; n is 0 to 2; R<2> and R<3> are each H, C1-6 alkyl, C2-4 alkenyl, or -L-Ar (wherein L is a bond or C1-6 alkylene; and Ar is a group derived from a saturated or unsaturated 5- or 6-membered ring which may contain one to three atoms selected from among N, S, and O or a saturated or unsaturated 8- to 12-membered fused-bicyclic hydrocarbon group), with the proviso that these groups may be substituted with one or more members selected from the group (A) consisting of halogeno, NO2, CN, OH, oxo, substituted and unsubstituted amino, and so on; X is -(CHR<4>)-, -(C=NOR<5>)-, or -C(O)-; R<4> is -NR<6>R<7> (wherein R<6> and R<7> are each H, C1-6 alkyl, C1-6 alkylcarbonyl, or the like); R<5> is H or C1-6 alkyl; Y is -NH- or methylene; and Z is methylene, ethylene, or vinylene, with the proviso that one or more hydrogen atoms constituting Y and/or Z may be replaced by halogeno, NO2, alkyl, or the like]. The compounds exhibit inhibitory activity against poly(ADP-ribose) polymerase (PARP) and are extremely safe and pharmaceutically excellent.