Methods and compositions for inhibition of adaptor protein/tyrosine
kinase interactions
    52.
    发明授权
    Methods and compositions for inhibition of adaptor protein/tyrosine kinase interactions 失效
    用于抑制衔接蛋白/酪氨酸激酶相互作用的方法和组合物

    公开(公告)号:US6090838A

    公开(公告)日:2000-07-18

    申请号:US90737

    申请日:1998-06-04

    摘要: The present invention relates to methods and compositions for the inhibition of adaptor protein/protein tyrosine kinase protein interactions, especially wherein those interactions involving a protein tyrosine kinase capable of complexing with a member of the SH2- and/or SH3-containing family of adaptor proteins are associated with a cell proliferative disorder. Specifically, the present invention relates to particular compounds, especially quinazoline derivative compounds, and methods utilizing such compounds.

    摘要翻译: 本发明涉及用于抑制衔接蛋白/蛋白酪氨酸激酶蛋白相互作用的方法和组合物,特别是其中涉及能够与适配蛋白家族的含SH2和/或SH3的成员复合的蛋白质酪氨酸激酶的那些相互作用 与细胞增殖性疾病相关。 具体地,本发明涉及具体的化合物,特别是喹唑啉衍生物化合物,以及利用这些化合物的方法。

    Quinoline compounds
    56.
    发明授权
    Quinoline compounds 失效
    喹啉化合物

    公开(公告)号:US5650415A

    公开(公告)日:1997-07-22

    申请号:US487090

    申请日:1995-06-07

    摘要: A method of inhibiting cell proliferation or differentiation by exposing a cell to a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. Q is selected from the group consisting of NH and S, n is 0 or 1; and R.sub.1-9 are independently selected from the group consisting of halo, trihalomethyl, alkyl, nitro, hydroxy, alkoxy, sulphoxy, sulphonyl, amide, sulfonamide, carboxamide, amino, and hydrogen. Also provided is a compound of the structure ##STR2##

    摘要翻译: 一种通过将细胞暴露于式IMA化合物或其药学上可接受的盐来抑制细胞增殖或分化的方法。 Q选自NH和S,n为0或1; 卤素,三卤代甲基,烷基,硝基,羟基,烷氧基,磺酰氧基,磺酰基,酰胺,磺酰胺,甲酰胺,氨基和氢。 还提供了结构的化合物

    Indolinone combinatorial libraries and related products and methods for the treatment of disease
    57.
    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

    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。

    Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds
    60.
    发明授权
    Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds 失效
    用5-氮杂喹喔啉类化合物调节丝氨酸/苏氨酸蛋白激酶功能的方法

    公开(公告)号:US06727252B1

    公开(公告)日:2004-04-27

    申请号:US09688199

    申请日:2000-10-16

    IPC分类号: A61K314985

    CPC分类号: C07D471/04 A61K31/4985

    摘要: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with 5-azaquinoxaline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to 5-azaquinoxaline compounds and pharmaceutical compositions comprising these compounds.

    摘要翻译: 本发明部分地涉及用5-氮杂喹喔啉类化合物调节丝氨酸/苏氨酸蛋白激酶的功能的方法。 该方法包括表达丝氨酸/苏氨酸蛋白激酶(例如RAF)的细胞。 此外,本发明描述了用本发明鉴定的化合物预防和治疗生物体中丝氨酸/苏氨酸蛋白激酶相关异常状况的方法。 此外,本发明涉及5-氮杂喹喔啉化合物和包含这些化合物的药物组合物。