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    Therapeutic compounds
    1.
    发明授权
    Therapeutic compounds 有权
    治疗化合物

    公开(公告)号：US07531530B2

    公开(公告)日：2009-05-12

    申请号：US10565308

    申请日：2004-07-23

    申请人： Thomas Helleday ,  Nicola Curtin

    发明人： Thomas Helleday ,  Nicola Curtin

    IPC分类号： A61P35/00

    CPC分类号： C07D487/06 ,  A61K31/5517 ,  A61K38/005 ,  C12N15/1137 ,  C12N2310/14 ,  C12Y204/0203

    摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

    摘要翻译： 本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。 本发明还涉及这些化合物在制备药物中的用途。

    Therapeutic compounds
    2.
    发明授权
    Therapeutic compounds 有权
    治疗化合物

    公开(公告)号：US07351701B2

    公开(公告)日：2008-04-01

    申请号：US10898653

    申请日：2004-07-23

    申请人： Thomas Helleday ,  Nicola Curtin

    发明人： Thomas Helleday ,  Nicola Curtin

    IPC分类号： A61P35/00

    CPC分类号： C07D487/06 ,  A61K31/5517 ,  A61K38/005 ,  C12N15/1137 ,  C12N2310/14 ,  C12Y204/0203

    摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

    摘要翻译： 本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。 本发明还涉及这些化合物在制备药物中的用途。

    Dna-Pk Inhibitors
    5.
    发明申请
    Dna-Pk Inhibitors 审中-公开
    Dna-Pk抑制剂

    公开(公告)号：US20070238731A1

    公开(公告)日：2007-10-11

    申请号：US11575606

    申请日：2005-09-20

    申请人： Graeme Smith ,  Niall Martin ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  Kappusamy Saravanan ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Keith Menear ,  Marc Hummersone

    发明人： Graeme Smith ,  Niall Martin ,  Roger Griffin ,  Bernard Golding ,  Ian Hardcastle ,  Kappusamy Saravanan ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Keith Menear ,  Marc Hummersone

    IPC分类号： A61K31/5355 ,  C07D413/14

    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, C3-20heterocyclyl 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或R 4 R 5和R 5独立地选自氢，任选取代的C 1-7 - 烷基，C 5-20芳基或C 3-20个杂环基或R 4和R 5可以一起与它们所连接的氮原子一起形成任选地 具有4至8个环原子的取代杂环; 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。

    DNA-PK inhibitors
    7.
    发明申请
    DNA-PK inhibitors 失效
    DNA-PK抑制剂

    公开(公告)号：US20060106025A1

    公开(公告)日：2006-05-18

    申请号：US11231041

    申请日：2005-09-20

    申请人： Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Laurent Rigoreau ,  Roger Griffin ,  Bernard Golding ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Ian Hardcastle ,  Kappusamy Saravanan

    发明人： Graeme Smith ,  Niall Martin ,  Keith Menear ,  Marc Hummersone ,  Laurent Rigoreau ,  Roger Griffin ,  Bernard Golding ,  David Newell ,  Hilary Calvert ,  Nicola Curtin ,  Ian Hardcastle ,  Kappusamy Saravanan

    IPC分类号： A61K31/496 ,  C07D409/14

    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。