DNA-PK inhibitors
    1.
    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

    IPC分类号: A61K31/496 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
    2.
    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

    IPC分类号: A61K31/5355 C07D413/14

    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。

    ATM inhibitors
    8.
    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

    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。

    PHTHALAZINONE DERIVATIVES
    10.
    发明申请

    公开(公告)号:US20070093489A1

    公开(公告)日:2007-04-26

    申请号:US11550004

    申请日:2006-10-17

    IPC分类号: A61K31/53

    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.