摘要 |
A 7H-2,7,9a-triaza-benzo[cd]azulen-6-one or 2H- [1,4]diazepine[6,7,1-hi]indol-1-one derivative or a pharmaceutically acceptable derivative thereof has the formula (I) or (II) wherein: X is O or S; Z is O or S; Y is N or CR3; R3 is H, halogen, cyano, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group or -C(W)-R20 or -CR29=N-R30; R1 is cyano, substituted alkyl, or optionally substituted alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group or C(O)R12, OR13, S(O)nR16 or NR17R18; R2 is H or alkyl; R4 is H, halogen, or alkyl; R5, R6, R7, and R8 are independently H, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group or -C(O)-R50; R9 is H or alkyl and R12, R13, R16 to R18, R50, W, R20, R29 and R30 are as defined in the specification; provided in formula (I) when Y is CR3 then R1 to R8 are not all H and in formula (II) R9 is not H when R5 or R6 is alkyl. The compounds are useful for inhibiting PARP activity of an enzyme such as poly (ADP-ribose) polymerase or tankyrase or for inhibiting PARP enzyme activity. |
申请人 |
AGOURON PHARMACEUTICALS, INC |
发明人 |
WEBBER, STEPHEN EVAN;SKALITZKY, DONALD JAMES;TIKHE,JAYASHREE GIRISH;KUMPF, ROBERT ARNOLD;MARAKOVITS, JOSEPHTIMOTHY;EASTMAN, BRIAN WALTER |