PHTHALAZINONE DERIVATIVES AS INHIBITORS OF PARP-1.

摘要

A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NR^X or CR^XR^Y; if X = NR^X then n is 1 or 2 and if X = CR^XR^Y then n is 1; if X = NR^X, then R^X is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X = CR^XR^Y then R^x is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and Rgamma is selected from H, hydroxy, optionally substituted amino, or R^x and R^gamma may together form an optionally substituted spiro-C3-7 cycloalkyl or heterocyclyl group; R^C1 and R^C2 are both hydrogen, or when X is CR^XR^Y, R^C1, R^C2, R^x and R^y, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R¹is selected from H and halo. The compounds act as inhibitors of poly(APD-ribose)synthase, PARP-1.