Substituted 4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one derivatives as poly (ADP-ribose) polymerase-1 inhibitors

摘要

Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly(ADP-ribose)polymerase-1 inhibitors (PARP-1 inhibitors).;

主权项

1. A compound of formula (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof: wherein, R1 is independently selected from hydrogen, halo, nitro, cyano, or an unsubstituted or substituted group selected from (C1-C12)alkyl, haloalkyl, cycloalkyl, alkylthio or OS(O)2alkyl, where substituents are selected from a member of the group consisting of hydroxy, oxo, halo, thio, nitro, amino, alkyl, alkoxy, haloalkyl and haloalkoxy; n is 1, 2 or 3; X is selected from —O—, —S—, —S(O)2—, —SO—, or —NH—; and R2 is an unsubstituted or substituted group selected from aryl, heteroaryl or heterocyclyl, where (i) substituents on the aryl group are selected from a member of the group consisting of halo, alkyl, alkoxy, hydroxy, haloalkyl, haloalkoxy, cyano, thioalkyl and cycloalkyl, and (ii) substituents on the heteroaryl group or heterocyclyl group are selected from a member of the group consisting of halo, alkyl, alkoxy, hydroxy, haloalkyl, haloalkoxy, aryl, aralkyl, cyano, alkylthio and thioalkyl.