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    Kinase inhibitors, prodrug forms thereof and their use in therapy
    2.
    发明授权
    Kinase inhibitors, prodrug forms thereof and their use in therapy 有权
    激酶抑制剂，其前药形式及其在治疗中的用途

    公开(公告)号：US09101632B2

    公开(公告)日：2015-08-11

    申请号：US13390398

    申请日：2010-09-02

    申请人： Jeffrey Bruce Smaill ,  Adam Vorn Patterson ,  Guo-Liang Lu ,  Ho Huat Lee ,  Amir Ashoorzadeh ,  Robert Forbes Anderson ,  William Robert Wilson ,  William Alexander Denny ,  Huai-Ling Annie Hsu ,  Andrej Maroz ,  Stephen Michael Frazer Jamieson ,  Alexandra Marie Mowday ,  Kendall Marie Carlin

    发明人： Jeffrey Bruce Smaill ,  Adam Vorn Patterson ,  Guo-Liang Lu ,  Ho Huat Lee ,  Amir Ashoorzadeh ,  Robert Forbes Anderson ,  William Robert Wilson ,  William Alexander Denny ,  Huai-Ling Annie Hsu ,  Andrej Maroz ,  Stephen Michael Frazer Jamieson ,  Alexandra Marie Mowday ,  Kendall Marie Carlin

    IPC分类号： A61K31/519 ,  A61P35/00 ,  C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/519

    摘要： The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy-and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.

    摘要翻译： 本发明提供了式I的激酶抑制剂：其中：（1）R 1是H，和（a）R 2是（3-氯苄基）氧基，R 3是氯; （b）R2和R3与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; （c）R2是2-吡啶基甲氧基，R3是氯; （d）R2和R3均为氯; （e）R 2是氯，R 1是溴; （f）R2和R3都是溴; （g）R2是氟，R3是乙炔基; （h）R2是氯，R3是乙炔基; （i）R2是溴，R3是乙炔基; （j）除了当R 1与R 3结合在一起的3位时，在4-位上，R 2是溴并且R 3是氟; （k）R2是2-吡啶基甲氧基，R3是氟; 或（1）R 2是2-吡啶基甲氧基，R 1是溴; 或（2）R 1，R 2和R 3中的至少一个选自苄氧基，3-氯苄氧基和2-吡啶基甲氧基，当R 1，R 2和R 3中的至少一个不是苄氧基，3-氯苄氧基或2-吡啶基甲氧基时， 其余的独立地选自H，卤素和C 2 -C 4炔基，条件是当R 1，R 2和R 3中的一个是苄氧基或2-吡啶基甲氧基时，R 1，R 2和R 3中的另外两个不是H; 或（3）R 1，R 2和R 3中的两个与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; 另一个选自H，卤素和C 2 -C 4炔基。 还提供了还原前药，其包含如上定义的激酶抑制剂和直接或间接连接于激酶抑制剂的氮的还原性触发剂。 还提供了包含激酶抑制剂或前药的药物组合物，以及这些组合物在治疗中的用途，特别是用于治疗癌症。

    Pteridinones as kinase inhibitors
    9.
    发明授权
    Pteridinones as kinase inhibitors 失效
    蝶啶酮作为激酶抑制剂

    公开(公告)号：US07169778B2

    公开(公告)日：2007-01-30

    申请号：US10070530

    申请日：2000-06-21

    申请人： William Alexander Denny ,  Gordon William Rewcastle ,  Ellen Dobrusin ,  James Bernard Kramer ,  Dennis Joseph McNamara ,  Howard Daniel Hollis Showalter ,  Peter Laurence Toogood

    发明人： William Alexander Denny ,  Gordon William Rewcastle ,  Ellen Dobrusin ,  James Bernard Kramer ,  Dennis Joseph McNamara ,  Howard Daniel Hollis Showalter ,  Peter Laurence Toogood

    IPC分类号： A61K31/535 ,  C07D475/00

    CPC分类号： C07D475/00

    摘要： Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).

    摘要翻译： 公开了式（Ia），（Ib），（Ic），（Id）的化合物，其中：W是NH，S，SO或SO 2; R 2是（未）取代的芳基，（未）取代的杂芳基或（取代的）取代的碳环或杂环; Q是氢或低级烷基; R 4和R 6相同或不同，表示氢，卤素，低级烷基，低级烷氧基，（未）取代的芳基，（未）取代的杂芳基，（un ）取代的芳基烷基或（未）取代的杂芳基烷基; 和R 8是氢，低级烷基或含有3-7个成员的（未）取代的碳环，其中至多两个成员任选是选自氧和氮的杂原子; 或（R 8）是（un）取代的芳基，（未）取代的杂芳基，（未）取代的芳基烷基或（未）取代的杂芳基烷基。 这些化合物可用于治疗细胞增殖性疾病，如癌症和再狭窄。 这些化合物是细胞周期蛋白依赖性激酶（cdks）和生长因子介导的激酶的有效抑制剂。 本发明还提供了治疗细胞增殖性疾病的方法。 本发明还提供含有式（I）化合物的药学上可接受的组合物。