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    4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
    6.
    发明授权
    4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors 失效
    4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途

    公开(公告)号：US06610688B2

    公开(公告)日：2003-08-26

    申请号：US09741737

    申请日：2000-12-21

    申请人： Congxin Liang ,  Li Sun ,  Chung Chen Wei ,  Peng Cho Tang ,  Gerald McMahon ,  Klaus Peter Hirth ,  Jingrong Cui

    发明人： Congxin Liang ,  Li Sun ,  Chung Chen Wei ,  Peng Cho Tang ,  Gerald McMahon ,  Klaus Peter Hirth ,  Jingrong Cui

    IPC分类号： C07D48704

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.

    摘要翻译： 本发明涉及4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途。 本文公开的特定的4-取代的7-氮杂 - 二氢吲哚-2-酮是式1及其药学上可接受的盐，溶剂合物，包合物和前药，其中R1，R2，R3，R4，X，Y和Z如本文所定义。 本发明还涉及包含式1化合物的药物组合物和剂型，以及它们用于治疗和/或预防疾病例如但不限于癌症的方法。

    Indolinone combinatorial libraries and related products and methods for the treatment of disease
    7.
    发明授权
    Indolinone combinatorial libraries and related products and methods for the treatment of disease 有权
    吲哚酮组合文库及相关产品及治疗方法

    公开(公告)号：US07202265B2

    公开(公告)日：2007-04-10

    申请号：US10784917

    申请日：2004-02-24

    申请人： Peng Cho Tang ,  Connie Li Sun ,  Gerald McMahon ,  Klaus Peter Hirth ,  Laura Kay Shawver

    发明人： Peng Cho Tang ,  Connie Li Sun ,  Gerald McMahon ,  Klaus Peter Hirth ,  Laura Kay Shawver

    IPC分类号： A61K31/404 ,  C07D403/06

    CPC分类号： C07D209/34

    摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1′ position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.

    摘要翻译： 本发明涉及能够调节，调节和/或抑制蛋白激酶信号转导的有机分子。 这些化合物可用于治疗与未调节的蛋白激酶信号转导相关的疾病，包括细胞增殖性疾病如癌症，动脉粥样硬化，关节炎和再狭窄以及诸如糖尿病的代谢疾病。 本发明具有抑制蛋白激酶及相关产物和方法的吲哚啉酮化合物。 可以通过向3 - [（吲哚-3-基）亚甲基] -2-二氢吲哚酮，特别是在吲哚环的1'位置添加化学取代基来获得对FLK蛋白激酶特异性的抑制剂。 特异性抑制FLK和血小板衍生生长因子蛋白激酶的吲哚酮化合物可以含有四氢吲哚或环戊基-b-吡咯部分。 被取代基修饰的吲哚啉酮化合物，特别是在羟吲哚环的5位，可以有效地激活蛋白激酶。 本发明还具有酪氨酸激酶抑制剂和相关产物和方法的新型水溶性吲哚啉酮化合物。

    Indolinone combinatorial libraries and related products and methods for the treatment of disease
    9.
    发明授权
    Indolinone combinatorial libraries and related products and methods for the treatment of disease 失效

    公开(公告)号：US6147106A

    公开(公告)日：2000-11-14

    申请号：US915366

    申请日：1997-08-20

    申请人： Peng Cho Tang ,  Li Sun ,  Gerald McMahon ,  Klaus Peter Hirth ,  Laura Kay Shawver

    发明人： Peng Cho Tang ,  Li Sun ,  Gerald McMahon ,  Klaus Peter Hirth ,  Laura Kay Shawver

    IPC分类号： C07D209/34 ,  A61K31/404 ,  C07D403/06

    CPC分类号： C07D209/34

    摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.

    Bicyclic protein kinase inhibitors
    10.
    发明授权
    Bicyclic protein kinase inhibitors 失效
    双环蛋白激酶抑制剂

    公开(公告)号：US07189721B2

    公开(公告)日：2007-03-13

    申请号：US10725267

    申请日：2003-12-02

    申请人： Peng Cho Tang ,  Li Sun ,  Gerald McMahon

    发明人： Peng Cho Tang ,  Li Sun ,  Gerald McMahon

    IPC分类号： A61K31/519 ,  A61K31/503 ,  C07D487/02

    CPC分类号： C07D471/04 ,  C07D209/34

    摘要： The present invention relates to novel 3-hetero-arylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

    摘要翻译： 本发明涉及调节蛋白激酶活性的新型3-异亚烷基-2-二氢吲哚酮化合物及其生理上可接受的盐，因此预期可用于预防和治疗蛋白激酶相关的细胞病症例如癌症。