Tetrahydro-isoquinolin-1-ones for the treatment of cancer
    1.
    发明授权
    Tetrahydro-isoquinolin-1-ones for the treatment of cancer 有权
    用于治疗癌症的四氢异喹啉-1-酮

    公开(公告)号:US08163744B2

    公开(公告)日:2012-04-24

    申请号:US11909014

    申请日:2006-03-17

    IPC分类号: C07D413/02 A61K31/47

    CPC分类号: C07D217/24

    摘要: The present invention provides a compound selected from compounds of formula I as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy. Compounds of formula (I) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events, heart valvular degenerative disease Moreover, compounds of formula (I) can be used to decrease the side effects from cytotoxic cancer agents and to treat viral infections.

    摘要翻译: 本发明提供了选自式I化合物作为与HDM2蛋白结合的配体的化合物,诱导细胞凋亡和抑制增殖,并具有癌症治疗的治疗效用。 式(I)化合物可用作治疗中风,心肌梗塞,局部缺血,多器官功能衰竭,脊髓损伤,阿尔茨海默氏病,缺血事件的损伤,心脏瓣膜变性疾病的治疗剂。此外,式(I)化合物可 用于减少细胞毒性剂的副作用并治疗病毒感染。

    Tetrahydro-isoquinolines
    5.
    发明授权
    Tetrahydro-isoquinolines 有权
    四氢异喹啉

    公开(公告)号:US08367699B2

    公开(公告)日:2013-02-05

    申请号:US12441266

    申请日:2007-09-14

    IPC分类号: C07D217/02 A61K31/47

    摘要: The present invention provides a compound selected from compounds of formula (A) as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (A) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (A) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.

    摘要翻译: 本发明提供了选自式(A)化合物的化合物作为与HDM2蛋白结合的配体,诱导细胞凋亡和抑制增殖,并具有癌症治疗和预防的治疗效用。 式(A)化合物可用作治疗中风,心肌梗塞,局部缺血,多器官功能衰竭,脊髓损伤,阿尔茨海默病,缺血事件和心脏瓣膜退行性疾病的损伤的治疗剂。 此外,式(A)化合物可用于降低细胞毒性剂,辐射和治疗病毒感染的副作用。

    NOVEL TETRAHYDRO-ISOQUINOLINES
    6.
    发明申请
    NOVEL TETRAHYDRO-ISOQUINOLINES 有权
    新型四氢异喹啉

    公开(公告)号:US20090306130A1

    公开(公告)日:2009-12-10

    申请号:US12441266

    申请日:2007-09-14

    摘要: The present invention provides a compound selected from compounds of formula (A) as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (A) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (A) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.

    摘要翻译: 本发明提供了选自式(A)化合物的化合物作为与HDM2蛋白结合的配体,诱导细胞凋亡和抑制增殖,并具有癌症治疗和预防的治疗效用。 式(A)化合物可用作治疗中风,心肌梗塞,局部缺血,多器官功能衰竭,脊髓损伤,阿尔茨海默病,缺血事件和心脏瓣膜退行性疾病的损伤的治疗剂。 此外,式(A)化合物可用于降低细胞毒性剂,辐射和治疗病毒感染的副作用。

    Combinations of ET-18-O-CH3and anti-cancer agents for the treatment of cancer
    7.
    发明授权
    Combinations of ET-18-O-CH3and anti-cancer agents for the treatment of cancer 有权
    用于治疗癌症的ET-18-O-CH3和抗癌剂的组合

    公开(公告)号:US08324188B2

    公开(公告)日:2012-12-04

    申请号:US12514328

    申请日:2007-11-09

    摘要: A method to determine the utility of small molecules as functional replacements (mimetics) for protein receptor ligands is described. The method uses cellular biological assays on a systematic array of compounds, comprising known protein receptor ligands and other biologically active molecules to determine if a proposed small molecule is a functional equivalent of a receptor ligand, having therapeutic utility as a pharmaceutically relevant and useful agent either alone or in combination with other molecules. Furthermore, the invention provides for a method for the treatment of cancer comprising administering a combination of ET-18-O-CH3 and an anti-cancer agent.

    摘要翻译: 描述了确定小分子作为蛋白质受体配体的功能替代物(模拟物)的效用的方法。 该方法在系统化的化合物阵列上使用细胞生物测定法,其包括已知的蛋白质受体配体和其他生物活性分子,以确定所提出的小分子是否是受体配体的功能等同物,具有作为药学上相关和有用的药剂的治疗效用 单独或与其他分子组合。 此外,本发明提供了治疗癌症的方法,包括给予ET-18-O-CH3和抗癌剂的组合。

    Methods and Compositions for Detecting Receptor Ligand Mimetics
    8.
    发明申请
    Methods and Compositions for Detecting Receptor Ligand Mimetics 有权
    检测受体配体模拟物的方法和组成

    公开(公告)号:US20100111930A1

    公开(公告)日:2010-05-06

    申请号:US12514328

    申请日:2007-11-09

    摘要: A method to determine the utility of small molecules as functional replacements (mimetics) for protein receptor ligands is described. The method uses cellular biological assays on a systematic array of compounds, comprising known protein receptor ligands and other biologically active molecules to determine if a proposed small molecule is a functional equivalent of a receptor ligand, having therapeutic utility as a pharmaceutically relevant and useful agent either alone or in combination with other molecules.

    摘要翻译: 描述了确定小分子作为蛋白质受体配体的功能替代物(模拟物)的效用的方法。 该方法在系统化的化合物阵列上使用细胞生物测定法,其包括已知的蛋白质受体配体和其他生物活性分子,以确定所提出的小分子是否是受体配体的功能等同物,具有作为药学上相关和有用的药剂的治疗效用 单独或与其他分子组合。