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    Cdc42 INHIBITOR AND USES THEREOF
    3.
    发明申请
    Cdc42 INHIBITOR AND USES THEREOF 审中-公开

    公开(公告)号：US20170334863A1

    公开(公告)日：2017-11-23

    申请号：US15671388

    申请日：2017-08-08

    申请人： Qun Lu ,  Huchen Zhou ,  Yanhua Chen ,  Amy Friesland

    发明人： Qun Lu ,  Huchen Zhou ,  Yanhua Chen ,  Amy Friesland

    IPC分类号： C07D239/42 ,  C07D239/69 ,  C07C335/12

    CPC分类号： C07D239/42 ,  C07C335/12 ,  C07D239/69

    摘要： Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.

    Cdc42 inhibitor and uses thereof
    4.
    发明授权
    Cdc42 inhibitor and uses thereof 有权

    公开(公告)号：US09725417B2

    公开(公告)日：2017-08-08

    申请号：US14807386

    申请日：2015-07-23

    申请人： Qun Lu ,  Huchen Zhou ,  Yanhua Chen ,  Amy Friesland

    发明人： Qun Lu ,  Huchen Zhou ,  Yanhua Chen ,  Amy Friesland

    IPC分类号： C07D239/42 ,  C07D239/69 ,  C07C335/12

    CPC分类号： C07D239/42 ,  C07C335/12 ,  C07D239/69

    摘要： Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyzes of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.

    Method of treating proliferative disorders and other pathological conditions mediated by Bcr-Abl, c-Kit, DDR1, DDR2 or PDGF-R kinase activity
    6.
    发明授权
    Method of treating proliferative disorders and other pathological conditions mediated by Bcr-Abl, c-Kit, DDR1, DDR2 or PDGF-R kinase activity 有权
    治疗由Bcr-Abl，c-Kit，DDR1，DDR2或PDGF-R激酶活性介导的增殖性疾病和其他病理状态的方法

    公开(公告)号：US09061029B2

    公开(公告)日：2015-06-23

    申请号：US13509626

    申请日：2010-11-17

    申请人： Neil Gallagher ,  Ophelia Yin

    发明人： Neil Gallagher ,  Ophelia Yin

    IPC分类号： A61K31/506 ,  C07D239/69 ,  A61K9/00

    CPC分类号： A61K31/506 ,  A61K9/0095 ,  C07D239/69

    摘要： The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I wherein the radicals as defined herein, or of a pharmaceutically acceptable salt thereof, for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity, wherein the pyrimidylaminobenzamide of formula I and, optionally, pharmaceutically acceptable carriers, are dispersed in a fruit preparation.

    摘要翻译： 本发明涉及用于施用式I嘧啶基氨基苯甲酰胺的方案，其中本文所定义的基团或其药学上可接受的盐用于治疗增殖性疾病，特别是固体和液体肿瘤，以及由其介导的其它病理学病症 Bcr-Abl癌蛋白，细胞跨膜酪氨酸激酶受体c-Kit，DDR1（盘状蛋白结构域受体1），DDR2（盘状蛋白结构域受体2）或PDGF-R（血小板衍生生长因子受体）激酶活性，其中式 I和任选的药学上可接受的载体分散在水果制剂中。