ATM inhibitors
    14.
    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。

    Dna-Pk Inhibitors
    15.
    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。

    DNA-PK inhibitors
    16.
    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。

    Phthalazinone derivatives
    18.
    发明申请

    公开(公告)号:US20060142293A1

    公开(公告)日:2006-06-29

    申请号:US11352178

    申请日:2006-02-10

    IPC分类号: A61K31/502

    摘要: A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.