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    Indolinone combinatorial libraries and related products and methods for the treatment of disease
    1.
    发明申请
    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：US20050197382A1

    公开(公告)日：2005-09-08

    申请号：US10784917

    申请日：2004-02-24

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

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

    IPC分类号： C07D209/34 ,  A61K31/404 ,  G01N33/53 ,  G01N33/543

    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。

    Tyrosine kinase inhibitors
    2.
    发明授权
    Tyrosine kinase inhibitors 失效
    酪氨酸激酶抑制剂

    公开(公告)号：US06987113B2

    公开(公告)日：2006-01-17

    申请号：US09096014

    申请日：1998-06-10

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

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

    IPC分类号： A61K31/505 ,  A61P7/00 ,  C07D487/00

    CPC分类号： C07D209/34

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

    摘要翻译： 本发明涉及预期调节蛋白酪氨酸激酶活性的新型3-杂芳基亚氨基二氢吡喃-2-酮化合物及其生理上可接受的盐和前药，因此可用于预防和治疗蛋白质酪氨酸激酶相关细胞 疾病如癌症。

    Azaindole tyrosine kinase inhibitors
    3.
    发明授权
    Azaindole tyrosine kinase inhibitors 失效
    阿魏酸酪氨酸激酶抑制剂

    公开(公告)号：US06849641B1

    公开(公告)日：2005-02-01

    申请号：US09191199

    申请日：1998-11-12

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

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

    IPC分类号： A61P35/00 ,  C07D209/34 ,  C07D471/02 ,  A61K31/44

    CPC分类号： C07D209/34

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

    摘要翻译： 本发明涉及预期调节蛋白酪氨酸激酶活性的新型3-杂芳基亚氨基二氢吡喃-2-酮化合物及其生理上可接受的盐和前药，因此可用于预防和治疗蛋白质酪氨酸激酶相关细胞 疾病如癌症。

    3-(cycloalkanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
    5.
    发明授权
    3-(cycloalkanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors 失效
    3-（环烷酰基杂芳基）-2-二氢吲哚酮蛋白酪氨酸激酶抑制剂

    公开(公告)号：US06350754B2

    公开(公告)日：2002-02-26

    申请号：US09482198

    申请日：2000-01-12

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

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

    IPC分类号： A61K31404

    CPC分类号： C07D405/06 ,  C07D209/34

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

    摘要翻译： 本发明涉及新的3-（环烷基 - 杂芳基烯基）-2-二氢吲哚酮化合物及其生理上可接受的盐和前体药物，其预期调节蛋白酪氨酸激酶的活性，因此可用于预防和治疗蛋白质酪氨酸激酶 相关的细胞病症如癌症。

    Bicyclic protein kinase inhibitors
    7.
    发明授权
    Bicyclic protein kinase inhibitors 失效
    双环蛋白激酶抑制剂

    公开(公告)号：US06316429B1

    公开(公告)日：2001-11-13

    申请号：US09074621

    申请日：1998-05-07

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

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

    IPC分类号： C07D48700

    CPC分类号： C07D471/04 ,  C07D209/34

    摘要： The present invention relates to novel 3-idene-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-异吲哚-2-酮吲哚酮化合物及其生理学上可接受的盐，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。

    3-heteroarylidenyl-2-azaindolinones active as protein tyrosine kinase inhibitors
    9.
    发明授权
    3-heteroarylidenyl-2-azaindolinones active as protein tyrosine kinase inhibitors 失效
    作为蛋白酪氨酸激酶抑制剂有活性的3-杂芳基-2-氮杂吲哚酮

    公开(公告)号：US06696463B2

    公开(公告)日：2004-02-24

    申请号：US09948106

    申请日：2001-09-07

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

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

    IPC分类号： C07D20942

    CPC分类号： C07D209/34

    摘要： The invention relates to 3-heteroarylidenyl-2-azaindolinone compounds of the formula: wherein, A is selected from the group consisting of nitrogen, oxygen and sulfur; only one of B, D, E, F or G is nitrogen; Z is selected from the group consisting of oxygen, sulfur and NR11; or physiologically acceptable salts thereof; and wherein the groups R1-R7 are defined herein. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention have improved hydrosolubility and are expected to modulate the activity of protein tyrosine kinases. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention should be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

    摘要翻译： 本发明涉及下式的3-杂芳基-2-氮杂吲哚酮化合物：其中A选自氮，氧和硫; B，D，E，F或G中只有一个是氮;选择Z 由氧，硫和NR 11组成的组; 其生理上可接受的盐;并且其中基团R 1 -R 7在本文中定义。 本发明优选实施方案的3-杂芳基-2-氮杂吲哚酮化合物具有改善的水溶性，并且预期调节蛋白酪氨酸激酶的活性。 本发明优选实施方案的3-杂芳基-2-氮杂吲哚酮化合物可用于预防和治疗蛋白质酪氨酸激酶相关细胞病症如癌症。

    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：US06683082B2

    公开(公告)日：2004-01-27

    申请号：US09819698

    申请日：2001-03-29

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

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

    IPC分类号： A61K31495

    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。