Patent ID: 6514983
Filing Date: 2003-02-04
Classification: A61K,A61P,C07D

Abstract:
A compound having an IC50 of 25 &mgr;M or lower for inhibiting poly(ADP-ribose)polymerase in vitro, said compound being a compound of formula I: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, whereinY is C1 alkylhalo, C1 alkyl-COâ€”G, a direct bond, C&boxH;O, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is O; R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; with the provisos that when Y is CR8 then R8 is halo, hydroxy, amino, alkylamino, nitro, nitroso, carboxy or aralkyl; and that when Y is CR8 and Z is O, then at least one of R1, R2, R3, R4, R5, R6, and R7, and R8 are selected from the group consisting of halo, aryl, amino, alkylamino, nitro, nitroso, carboxy or aralkyl, and R1, R2, R3, R4, R5, R6, R7 or R8 are not phenyl; and furtherwherein said alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl and aralkyl groups are independently substituted with one or more substituent(s) selected from the group consisting of C3-C8 cycloalkyl, C5-C7 cycloalkenyl, halo, hydroxyl, nitro, trifluoromethyl, C1-C6 straight or branched chain alkyl, C2-C6 straight or branched chain alkenyl, C1-C4 alkoxy, C2-C4 alkenyloxy, phenoxy, benzyloxy, and aryl having one or more substituent(s) independently selected from the group consisting of hydrogen, halo, hydroxyl, nitro, trifluoromethyl, C1-C6 straight or branched chain alkyl, C2-C6 straight or branched chain alkenyl, C1-C4 alkoxy or C2-C4 alkenyloxy, phenoxy, and benzyloxy; with the provisos that Y is not CR8 when there is a double bond between C1 and C2 and that when Z is oxygen and R1-R7 are hydrogen then Y is not a direct bond.