Fibroblast activation protein inhibitor compounds and methods
    2.
    发明授权
    Fibroblast activation protein inhibitor compounds and methods 有权
    成纤维细胞激活蛋白抑制剂化合物及方法

    公开(公告)号:US07399869B2

    公开(公告)日:2008-07-15

    申请号:US11437182

    申请日:2006-05-18

    IPC分类号: C07D207/00 A01N43/36

    CPC分类号: C07F5/025

    摘要: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

    摘要翻译: 式I和II的氨基末端封闭的肽硼酸酯化合物可用于抑制成纤维细胞激活蛋白(FAP)和其它蛋白酶,以及用于治疗由FAP介导的病症。 使用氨基末端阻断肽硼酸酯化合物及其立体异构体,互变异构体,溶剂化物和其药学上可接受的盐的方法用于体外,原位和体内诊断,预防或治疗哺乳动物细胞或相关病理状况中的这些疾病。 披露

    Purine PI3K inhibitor compounds and methods of use
    3.
    发明授权
    Purine PI3K inhibitor compounds and methods of use 有权
    嘌呤PI3K抑制剂化合物及其使用方法

    公开(公告)号:US08445487B2

    公开(公告)日:2013-05-21

    申请号:US13369941

    申请日:2012-02-09

    CPC分类号: C07D473/32

    摘要: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

    摘要翻译: 式I的嘌呤化合物,并且包括立体异构体,几何异构体,互变异构体,溶剂合物,代谢物和其药学上可接受的盐可用于抑制脂质激酶,包括p110α和PI3K的其他同种型,并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I化合物在体外,原位和体内诊断,预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

    Purine compounds selective for PI3K P110 delta, and methods of use
    4.
    发明授权
    Purine compounds selective for PI3K P110 delta, and methods of use 失效
    对PI3K P110 delta有选择性的嘌呤化合物及其使用方法

    公开(公告)号:US08293736B2

    公开(公告)日:2012-10-23

    申请号:US13181647

    申请日:2011-07-13

    IPC分类号: A61K31/535 C07D413/14

    CPC分类号: C07D473/32

    摘要: The invention provides compounds having the general formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and n are defined herein, compositions including the compounds and method of using the compounds to treat a disease or disorder mediated by the p110 delta isoform of PI3 kinase selected from immune disorders, cancer, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

    摘要翻译: 本发明提供具有以下通式的化合物及其立体异构体,互变异构体或其药学上可接受的盐,其中R1,R2,R3,R4和n如本文所定义,包括化合物的组合物和使用该化合物治疗疾病或病症的方法 由选自免疫疾病,癌症,心血管疾病,病毒感染,炎症,代谢/内分泌功能障碍和神经障碍的PI3激酶的p110δ同种型介导。

    PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
    5.
    发明申请
    PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
    PURINE PI3K抑制剂化合物及其使用方法

    公开(公告)号:US20120135988A1

    公开(公告)日:2012-05-31

    申请号:US13369941

    申请日:2012-02-09

    CPC分类号: C07D473/32

    摘要: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

    摘要翻译: 式I的嘌呤化合物,并且包括立体异构体,几何异构体,互变异构体,溶剂合物,代谢物和其药学上可接受的盐可用于抑制脂质激酶,包括p110α和PI3K的其他同种型,并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I化合物在体外,原位和体内诊断,预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。