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    • 4. 发明授权
    • Methods for treating glioma
    • 治疗胶质瘤的方法
    • US08748445B2
    • 2014-06-10
    • US11791588
    • 2005-10-27
    • W. Joon ChungHarald Sontheimer
    • W. Joon ChungHarald Sontheimer
    • A01N43/54A61K31/505A01N43/40A61K31/44A01N41/10A61K31/10C07D239/02C07D213/72C07D211/72C07D211/84C07C315/00C07C317/00
    • G01N33/566A61K31/00A61K31/63
    • The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.
    • 本公开提供了治疗和/或预防需要胱氨酸以维持或发展疾病状态的疾病状态的方法。 此外,描述了筛选和鉴定用于治疗这种疾病状态的新型治疗剂的方法。 在一个实施方案中,疾病状态是癌症,例如但不限于神经胶质瘤。 在该实施方案中,提供了通过抑制胱氨酸摄取或减少细胞内胱氨酸浓度来治疗和预防神经胶质瘤的方法。 本公开内容教导了神经胶质瘤细胞依赖于系统Xc用于胱氨酸摄取。 系统Xc的药理学抑制导致细胞内谷胱甘肽的快速消耗,导致细胞生长减少。 相比之下,非恶性星形胶质细胞和皮层神经元在Xc抑制剂存在下保持存活,并通过替代氨基酸转运体继续摄取胱氨酸。
    • 8. 发明授权
    • Method for producing 3-mercaptoaniline compound
    • 3-巯基苯胺化合物的制备方法
    • US08334410B2
    • 2012-12-18
    • US12743389
    • 2008-11-28
    • Kentaro Kawazoe
    • Kentaro Kawazoe
    • C07C209/00C07C323/00C07C317/00
    • C07C319/02C07C303/22C07C309/86C07C323/34
    • A method for producing a 3-mercaptoaniline compound, which is a known intermediate for a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide derivative, useful as a pesticide, and a method for producing a compound which can be used as a starting material in producing the 3-mercaptoaniline compound are disclosed. In one embodiment the nitro group and the chlorosulfonyl group of a 3-nitrobenzenesulfonyl chloride compound represented by general formula (1): are reduced in the presence of an acid catalyst to produce a compound of general formula (2): In the above general formulas (1) and (2), R represents an alkyl group or a cyclic alkyl group, and X represents a halogen atom.
    • 作为可用作农药的3-(1H-1,2,4-三唑-1-基)苯硫醚衍生物的已知中间体的3-巯基苯胺化合物的制造方法及其制造方法 可以用作生产3-巯基苯胺化合物的原料。 在一个实施方案中,通式(1)表示的3-硝基苯磺酰氯化合物的硝基和氯磺酰基在酸催化剂的存在下还原,得到通式(2)的化合物:在上述通式 (1)和(2)中,R表示烷基或环状烷基,X表示卤素原子。