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    Substituted pyrazolo[3,4-D]pyrimidines as kinase antagonists
    1.
    发明授权
    Substituted pyrazolo[3,4-D]pyrimidines as kinase antagonists 有权
    取代的吡唑并[3,4-D]嘧啶作为激酶拮抗剂

    公开(公告)号：US07585868B2

    公开(公告)日：2009-09-08

    申请号：US11732856

    申请日：2007-04-04

    申请人： Zachary A. Knight ,  Beth Apsel ,  Kevan M. Shokat

    发明人： Zachary A. Knight ,  Beth Apsel ,  Kevan M. Shokat

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P35/02

    CPC分类号： C07D487/04

    摘要： The present invention provides novel compounds that can be used as antagonists of a lipid kinase such as a PI3 kinase, protein tyrosine kinase, and/or protein serine-threonine kinases such as mTOR. The present invention also provides methods of using the compounds for treating various disease conditions. The compounds include those having the formula: wherein the R1, R2 and R36 are as defined herein.

    摘要翻译： 本发明提供可用作脂质激酶如PI3激酶，蛋白酪氨酸激酶和/或蛋白丝氨酸 - 苏氨酸激酶（如mTOR）的拮抗剂的新型化合物。 本发明还提供了使用该化合物治疗各种疾病状况的方法。 化合物包括具有下式的化合物：其中R 1，R 2和R 36如本文所定义。

    Methods for identifying cellular responses attributable to signaling molecule inhibition and inhibitors thereof
    4.
    发明授权
    Methods for identifying cellular responses attributable to signaling molecule inhibition and inhibitors thereof 失效
    用于鉴定归因于信号分子抑制的细胞应答的方法及其抑制剂

    公开(公告)号：US06610483B1

    公开(公告)日：2003-08-26

    申请号：US09621293

    申请日：2000-07-20

    申请人： Kevan M. Shokat ,  Anthony Bishop

    发明人： Kevan M. Shokat ,  Anthony Bishop

    IPC分类号： C12Q168

    CPC分类号： C07D487/04 ,  C12Q1/485

    摘要： The present invention provides a method for the identification of a pattern of changes in cellular responses induced by the selective inhibition of a signaling molecule, by determining the specific effects of a selective inhibitor on a mutant form of a signaling molecule on cellular responses. The pattern of alterations in cellular responses resulting from the inhibition by a selective mutant inhibitor of the mutant signaling molecule are characteristic of the cellular response alterations that a specific inhibitor of the wild-type signaling molecule will produce. After determining the pattern of cellular responses of the mutant cells with the mutant molecule, compounds may be identified capable of inhibiting the wild-type molecule by producing a pattern of cellular responses in wild-type cells matching or having similarity to that of the inhibition of the mutant molecule.

    摘要翻译： 本发明提供了通过确定选择性抑制剂对细胞反应的信号分子的突变形式的特异性作用来鉴定通过选择性抑制信号分子诱导的细胞反应变化模式的方法。 由突变型信号分子的选择性突变抑制剂的抑制引起的细胞反应改变的模式是野生型信号分子的特异性抑制剂将产生的细胞应答改变的特征。 在用突变分子确定突变细胞的细胞反应模式之后，可以鉴定化合物能够通过与野生型分子的抑制相匹配或具有相似性的野生型细胞中产生细胞反应的模式来抑制野生型分子 突变分子。

    Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
    5.
    发明授权
    Engineered protein kinases which can utilize modified nucleotide triphosphate substrates 有权
    可以利用修饰的三磷酸核苷酸底物的工程蛋白激酶

    公开(公告)号：US06390821B1

    公开(公告)日：2002-05-21

    申请号：US09367065

    申请日：1999-11-17

    申请人： Kevan M. Shokat

    发明人： Kevan M. Shokat

    IPC分类号： G09B100

    CPC分类号： G01N33/5008 ,  A01K2217/05 ,  A01K2217/075 ,  A61K38/00 ,  C07K2319/00 ,  C07K2319/23 ,  C12N9/1205 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5026 ,  G01N33/5041 ,  G01N33/5091

    摘要： Engineered protein kinases which can utilize modified nucleotide triphosphate substrates that are not as readily utilized by the wild-type forms of those enzymes, and methods of making and using them. Modified nucleotide triphosphate substrates and methods of making and using them. Methods for using such engineered kinases and such modified substrates to identify which protein substrates the kinases act upon, to measure the extent of such action, and to determine if test compounds can modulate such action. Also engineered forms of multi-substrate enzymes which covalently attach part or all of at least one (donor) substrate to at least one other (recipient) substrate, which engineered forms will accept modified substrates that are not as readily utilized by the wild-type forms of those enzymes. Methods for making and using such engineered enzymes. Modified substrates and methods of making and using them. Methods for using such engineered enzymes and such modified substrates to identify the recipient substrates the enzymes act upon, to measure the extent of such action, and to measure whether test compounds modulate such action.

    摘要翻译： 可以使用不被野生型形式的那些酶所容易利用的修饰的三磷酸核苷酸底物的工程化蛋白激酶，以及制备和使用它们的方法。 修饰的三磷酸核苷底物及其制备和使用方法。 使用这种工程化的激酶和这种修饰的底物以鉴定激酶作用于哪种蛋白质底物的方法，以测量这种作用的程度，以及确定测试化合物是否可以调节这种作用。 同样工程化的多底物酶的形式，其将至少一种（供体）底物的部分或全部共价连接至至少一种其它（受体）底物，其工程化形式将接受改性底物，其不被野生型 这些酶的形式。 制备和使用这些工程化酶的方法。 改性底物及其制备和使用方法。 使用这种工程化酶和这种修饰的底物以鉴定酶作用于受体底物的方法，以测量这种作用的程度，以及测量测试化合物是否调节这种作用。