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    • 9. 发明申请
    • HETEROCYCLIC COMPOUNDS AND THEIR USE AS PARP INHIBITORS
    • 杂环化合物和它们作为PARP抑制剂
    • WO0157038A9
    • 2001-09-20
    • PCT/EP0100790
    • 2001-01-25
    • BASF AGLUBISCH WILFRIEDKOCK MICHAELHOEGER THOMASGRANDEL ROLANDMUELLER REINHOLDSCHULT SABINE
    • LUBISCH WILFRIEDKOCK MICHAELHOEGER THOMASGRANDEL ROLANDMUELLER REINHOLDSCHULT SABINE
    • C07D471/04A61K31/437A61P25/00
    • C07D471/04
    • The invention relates to compounds of formula (I), wherein; either A or A represents CONH2, and the other radical A or A represents hydrogen, chlorine, fluorine, bromine, iodine C1-C6 alkyl, OH, nitro, CF3, CN, NR R , NH-CO-R , O-C1-C4 alkyl; X can represent N and C-R ; X , independent of X , can represent N and C-R ; R can represent hydrogen, C1-C6 alkyl, C1-C4 alkyl-phenyl, phenyl; B can represent an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 15 carbon atoms, an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms or 0 to 2 sulfur atoms, which can each still be substituted with an R and a maximum of 3 of the same or different radicals R , and; R , R , R , R -R have the meanings as cited in Claim No. 1. The invention also relates to the tautomeric forms, and possible enantiomeric and diastereomeric forms of said compounds, to the prodrugs thereof and to their use as PARP inhibitors.
    • 本发明涉及式(I)化合物式中A <1>或A <2>是CONH 2,另一基团A <2>或A <1>为氢,氯,氟,溴,碘,C1-C6 烷基,OH,硝基,CF 3,CN,NR <11> - [R <12>,NH-CO-R <13>,O-C 1 -C 4烷基,并且X <1>可以是N和CR <2> 和X <2>可以是独立的X <1>,N和CR <2>和C 1 -C 4 - 烷基 - 苯基,R <2>是氢,C1-C6烷基的苯基,和B是不饱和,饱和或 部分不饱和的单 - ,最多15个碳原子,不饱和的二环或三环的环,饱和或部分不饱和的单 - ,具有最大14个碳原子和0至5个氮原子,0〜2个氧原子和0〜二环或三环环 可以指2个硫原子,每个的又带有R <4>和最多3组相同或不同的基团R <5>可以被取代,并且R <1>,R <4>,R <5>,R <11> - [R <13>的含义如权利要求1和互变异构形式在指示物, 可能的对映体和非对映形式,以及它们的前体药物,以及它们作为PARP抑制剂的用途。