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    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity
    5.
    发明授权
    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity 失效
    用于抑制PARP活性的烷氧基取代的化合物，方法和组合物

    公开(公告)号：US06380211B1

    公开(公告)日：2002-04-30

    申请号：US09711953

    申请日：2000-11-15

    申请人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    发明人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    IPC分类号： A61K3147

    CPC分类号： C07D471/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/12 ,  C07D221/18 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D475/02 ,  C07D491/04 ,  C07F9/6561

    摘要： A compound, compositions, methods of use, and processes of making formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH—(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iii) —R2C═N—; (iv) —CR2(OH)—NR7—; or (v) —C(O)—NR7—.

    摘要翻译： 化合物，组合物，使用方法和制备式I的方法：或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物，其中：R 1当存在时为氢或低级烷基 或 - （CH 2）n - （CHOH）y（CH 2）mA，其中n为1-4，y为0或1，m为0-5，A为 是环烷基，环烯基，低级烷酰基，芳基，芳烷基，-NH 2，-NH-（低级烷基），Y表示形成芳族或非芳族和碳环或杂环的稠合5-至6-元环所必需的原子; Z 是（i）-CHR2CHR3-，其中R2和R3独立地是氢，烷基，芳基或芳烷基;（ii）-R6C = CR3-，其中R6和R3独立地是氢，低级烷基，芳基，芳烷基，氯，溴或-NR7R8 其中R 7和R 8独立地为氢或低级烷基，或者R 6和R 3一起形成芳族或非芳族和碳环或杂环的稠合5-至6-元环;（ⅲ）-R2C = N-; （iv ）-CR2（OH）-NR7-; 或（ⅴ）-C（O）-NR7-。