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    DNA-PK inhibitors
    3.
    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。

    Dna-Pk Inhibitors
    4.
    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。

    PHTHALAZINONE DERIVATIVES
    8.
    发明申请
    PHTHALAZINONE DERIVATIVES 失效

    公开(公告)号：US20070093489A1

    公开(公告)日：2007-04-26

    申请号：US11550004

    申请日：2006-10-17

    申请人： Muhammad Javaid ,  Keith Menear ,  Sylvie Gomez ,  Marc Hummersone ,  Niall Martin ,  Graeme Smith ,  Xiao-Ling Cockcroft

    发明人： Muhammad Javaid ,  Keith Menear ,  Sylvie Gomez ,  Marc Hummersone ,  Niall Martin ,  Graeme Smith ,  Xiao-Ling Cockcroft

    IPC分类号： A61K31/53

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i)  where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii)  and where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

    ATM inhibitors
    9.
    发明申请
    ATM inhibitors 失效
    ATM抑制剂

    公开(公告)号：US20060178361A1

    公开(公告)日：2006-08-10

    申请号：US11351052

    申请日：2006-02-09

    申请人： Marc Hummersone ,  Keith Menear ,  Laurent Rigoreau ,  Graeme Smith ,  Niall Martin ,  Roger Griffin

    发明人： Marc Hummersone ,  Keith Menear ,  Laurent Rigoreau ,  Graeme Smith ,  Niall Martin ,  Roger Griffin

    IPC分类号： A61K31/55 ,  A61K31/453 ,  C07D409/14

    CPC分类号： 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 together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms; and R3 is selected from hydroxy and —NRN1RN2, where RN1 and RN2 are independently selected from hydrogen, optionally substituted C1-7 alkyl groups, optionally substituted C3-20 heterocyclyl groups and optionally substituted C5-20 aryl groups, or together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms, and its use in inhibiting ATM.

    摘要翻译： 式I化合物及其异构体，盐，溶剂化物，化学保护形式及其前药，其中：R 1和R 2一起与氮原子一起形成 它们所连接的是具有4-8个环原子的任选取代的含氮杂环; R 3和R 3选自羟基和-NR N 1 N 2 N 2，其中R 11和R 10独立地选自氢， N 2独立地选自氢，任选取代的C 1-7烷基，任选取代的C 3-20杂环基和任选取代的C 5 -20个芳基，或者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含氮杂环，以及其在抑制ATM中的用途。

    Compounds
    10.
    发明申请
    Compounds 失效

    公开(公告)号：US20060199804A1

    公开(公告)日：2006-09-07

    申请号：US11361599

    申请日：2006-02-24

    申请人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Graeme Smith

    发明人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Graeme Smith

    IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/53 ,  A61K31/506 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D251/54 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/04 ,  C07D471/04

    摘要： Compounds of formula I: A-B-C  (I)and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of:  where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is: RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is:  where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from:  which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of: