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    DNA-PK inhibitors
    2.
    发明授权
    DNA-PK inhibitors 失效
    DNA-PK抑制剂

    公开(公告)号：US07402607B2

    公开(公告)日：2008-07-22

    申请号：US11231041

    申请日：2005-09-20

    申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

    发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

    IPC分类号： A61K31/381 ,  C07D333/76

    CPC分类号： C07D413/14 ,  C07D409/04 ,  C07D409/14

    摘要： A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(═O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(═O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R6 and R7 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and if Q is —NH—C(═O)—, —Y—X may additionally be selected from C1-7 alkyl.

    摘要翻译： 式I化合物及其异构体，盐，溶剂合物，化学保护形式及其前药，其中：R 1和R 2独立地选自氢，任选地 取代的C 1-7烷基，C 3-20杂环基或C 5-20-20芳基，或者可以一起形成 与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; Q是-NH-C（-O） - 或-O-; Y是任选取代的C 1-5亚烷基; X选自SR 3或NR 4 R 5，其中R 3，R 3，R 3， 4和R 5独立地选自氢，任选取代的C 1-7 - 烷基，C 5-20-20芳基，或 C 3-20杂环基或R 4和R 5可以一起与它们所连接的氮原子一起形成一个 具有4至8个环原子的任选取代的杂环; 如果Q是-O-，X另外选自-C（-O）-NR 6 R 7，其中R 6和R 独立地选自氢，任选取代的C 1-7 - 烷基，C 5-20-20芳基或C 3-20 或者R 6和R 7可以与它们所连接的氮原子一起形成任选取代的杂环，其具有4个 至8个环原子; 并且如果Q是-NH-C（-O） - ，-Y-X可另外选自C 1-7烷基。

    Method of improving the effectiveness of a cytotoxic drug or radiotherapy using a quinazolinone compound
    9.
    发明授权
    Method of improving the effectiveness of a cytotoxic drug or radiotherapy using a quinazolinone compound 失效
    使用喹唑啉酮化合物改善细胞毒性药物或放射疗法的有效性的方法

    公开(公告)号：US06316455B1

    公开(公告)日：2001-11-13

    申请号：US09448485

    申请日：1999-11-24

    申请人： Roger John Griffin ,  Alan Hilary Calvert ,  Nicola Jane Curtin ,  David Richard Newell ,  Bernard Thomas Golding

    发明人： Roger John Griffin ,  Alan Hilary Calvert ,  Nicola Jane Curtin ,  David Richard Newell ,  Bernard Thomas Golding

    IPC分类号： A61K31513

    CPC分类号： C07D263/56 ,  C07C235/46 ,  C07C247/16 ,  C07C255/54 ,  C07D239/91 ,  C07D263/57 ,  C07D317/68 ,  C07D473/34 ,  C07D473/40

    摘要： A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The coumpounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride —X—Y— that represents the grouping (a), (b) or (c) wherein R5 is H, alkyl, aryl or aralkyl.

    摘要翻译： 公开了一系列3-氧基苯甲酰胺化合物和相关的喹唑啉酮化合物，其可以作为DNA修复酶聚（ADP-核糖）聚合酶或PARP酶（EC 2.4.2.30）的有效抑制剂，由此可以为 与DNA损伤性细胞毒性药物或放射治疗联合使用以增强后者的作用。 公开的专利文献包括3-苄氧基苯甲酰胺，其中5个或更多个亚甲基的链终止于卤素原子或嘌呤-9-基部分的某些苯并恶唑-4-甲酰胺化合物和某些喹唑啉酮化合物的3-氧代苯甲酰胺。 式X和Y一起可以形成代表（a），（b）或（c）的组合的新娘-X-Y-，其中R 5是H，烷基，芳基或芳烷基。