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    COMPOUNDS FOR INHIBITING WIP1, PRODRUGS AND COMPOSITIONS THEREOF, AND RELATED METHODS
    2.
    发明申请
    COMPOUNDS FOR INHIBITING WIP1, PRODRUGS AND COMPOSITIONS THEREOF, AND RELATED METHODS 审中-公开
    用于抑制WIP1，PRODRUGS及其组合物的化合物及相关方法

    公开(公告)号：WO2009029844A1

    公开(公告)日：2009-03-05

    申请号：PCT/US2008/074864

    申请日：2008-08-29

    Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  APPELLA, Ettore ,  APPELLA, Daniel ,  DURELL, Stewart R. ,  BANG, Jeong ,  YAMAGUCHI, Hiroshi ,  XU, Qun

    Inventor： APPELLA, Ettore ,  APPELLA, Daniel ,  DURELL, Stewart R. ,  BANG, Jeong ,  YAMAGUCHI, Hiroshi ,  XU, Qun

    IPC: C07F9/572 ,  A61K31/6615 ,  A61K31/675 ,  A61P35/00

    CPC classification number: C07F9/5722 ,  A61K31/6615 ,  A61K31/675

    Abstract: The invention provides compounds useful in inhibiting the activity of a Wip1 protein in a cell as well as prodrugs thereof, related methods of use and compositions which include the aforesaid compounds and prodrugs thereof. The compounds comprise a ring structure having at least five functional groups bonded thereto, wherein each functional group is bonded to a different ring atom, and wherein the at least five functional groups comprise: (a) first (R 1 ) and second (R 3 ) moieties each comprising a phosphate group wherein these first and second moieties are separated by at least one ring atom; (b) first (R 2 ) and second (R 4 ) hydrophobic groups, wherein the first and second hydrophobic groups are separated by at least one ring atom, and wherein the first hydrophobic group is bonded to a ring atom located between the ring atoms to which the first (R 1 ) and second (R 2 ) moieties are bonded; and an amide or carboxylic acid (R 5 ).

    Abstract translation: 本发明提供了可用于抑制细胞中Wip1蛋白的活性的化合物及其前药，相关使用方法和包含上述化合物及其前药的组合物。 化合物包括具有键合至少五个官能团的环结构，其中每个官能团键合到不同的环原子上，其中至少五个官能团包括：（a）第一（R1）和第二（R3）部分 每个包含磷酸基团，其中这些第一和第二部分被至少一个环原子分开; （b）第一（R2）和第二（R4）疏水基团，其中所述第一和第二疏水基团被至少一个环原子隔开，并且其中所述第一疏水基团与位于所述环原子之间的环原子键合， 第一（R1）和第二（R2）部分键合; 和酰胺或羧酸（R5）。

    MATERIALS AND METHODS FOR INHIBITING WIP-1
    5.
    发明申请
    MATERIALS AND METHODS FOR INHIBITING WIP-1 审中-公开
    用于抑制WIP-1的材料和方法

    公开(公告)号：WO2003083103A1

    公开(公告)日：2003-10-09

    申请号：PCT/US2003/008997

    申请日：2003-03-21

    Applicant: THE GOVERNMENT OF THE UNITED STATES OF AMERICA, asrepresented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  BULAVIN, Dmitry ,  APPELLA, Ettore ,  FORNACE, Albert, J., Jr. ,  KALLIONIEMI, Anne

    Inventor： BULAVIN, Dmitry ,  APPELLA, Ettore ,  FORNACE, Albert, J., Jr. ,  KALLIONIEMI, Anne

    IPC: C12N9/16

    CPC classification number: C07K14/82

    Abstract: Isolated or purified oligonucleotides and isolated or purified morpholino oligomers; a method of detecting cancer or a predisposition to cancer in a mammal, comprising comparing the level of expression of Wip1 in the mammal to a control; a method of treating cancer in a mammal that expresses the same or a higher level of Wip1 as compared to a mammal of the same species that does not have cancer, comprising administering to the mammal a cancer-treating effective amount of a Wip1 inhibitor; a method of screening an oligonucleotide or morpholino oligomer for the ability to inhibit the expression of Wip1; a method of determining the efficacy with which a test oligonucleotide or morpholino oligomer inhibits Wip1 expression; a method of screening a compound for Wip1-inhibiting activity; and a method of determining the efficacy with which a test compound inhibits Wip1.

    Abstract translation: 分离或纯化的寡核苷酸和分离或纯化的吗啉代低聚物; 一种检测哺乳动物癌症或易患癌症的方法，包括将哺乳动物中Wip1的表达水平与对照组进行比较; 与不具有癌症的同一物种的哺乳动物相比，治疗哺乳动物中表达相同或更高水平的Wip1的癌症的方法，包括给予哺乳动物癌症治疗有效量的Wip1抑制剂; 筛选寡核苷酸或吗啉代低聚物以抑制Wip1表达的能力的方法; 确定测试寡核苷酸或吗啉代低聚物抑制Wip1表达的功效的方法; 筛选化合物的Wip1抑制活性的方法; 以及测定化合物抑制Wip1的功效的方法。

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