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    • 3. 发明申请
    • METHOD OF TREATING CANCER USING ADENOSINE AND ITS ANALOGS
    • 使用腺嘌呤及其类似物治疗癌症的方法
    • WO2004030621A3
    • 2004-12-09
    • PCT/US0330701
    • 2003-09-30
    • UNIV BOSTONRAVID KATYALU JUN
    • RAVID KATYALU JUN
    • A61K31/7076A61K31/70
    • A61K31/137A61K31/56A61K31/7076
    • The present invention provides methods of treating individuals having malignancies associated with estrogen receptor activity comprising administering to an individual affected with said malignancy, an effective amount of adenosine analog in a pharmaceutical carrier to downregulate or diminish estrogen receptors in the cells. The invention further provides methods of identifying novel adenosine analogues capable of treating malignant cells expressing estrogen receptors. The invention also provides kits comprising adenosine analogs for downregulating estrogen receptors in cells and kits for screening for novel adenosine analogs capable of downregulating estrogen receptors. Further, the invention provides uses of adenosine analogs in downregulation of estrogen receptors, cell growth and cell cycle, as well as pharmaceutical compositions comprising adenosine analogs effective in suppressing cellular growth, cell cycle or downregulating estrogen receptors.
    • 本发明提供了治疗患有与雌激素受体活性相关的恶性肿瘤的个体的方法,其中包括对受到所述恶性肿瘤影响的个体施用有效量的药物载体中的腺苷类似物以下调或减少细胞中的雌激素受体。 本发明还提供鉴定能够治疗表达雌激素受体的恶性细胞的新型腺苷类似物的方法。 本发明还提供了包含用于下调细胞中雌激素受体的腺苷类似物的试剂盒和用于筛选能够下调雌激素受体的新型腺苷类似物的试剂盒。 此外,本发明提供了腺苷类似物在下调雌激素受体,细胞生长和细胞周期中的用途,以及包含有效抑制细胞生长,细胞周期或下调雌激素受体的腺苷类似物的药物组合物的用途。
    • 9. 发明申请
    • BACTERIAL THIOREDOXIN REDUCTASE INHIBITORS AND METHODS FOR USE THEREOF
    • 细菌三氧化二氮还原酶抑制剂及其使用方法
    • WO2007137255A2
    • 2007-11-29
    • PCT/US2007069455
    • 2007-05-22
    • THIOREDOXIN SYSTEMS ABTHYOGEN PHARMACEUTICALS INCHOLMGREN ARNELU JUNVLAMIS-GARDIKAS ALEXIOSZHAO RONGKANDASAMY KENGMAN LARSENGSTRAND LARSHOFFNER SVEN
    • HOLMGREN ARNELU JUNVLAMIS-GARDIKAS ALEXIOSZHAO RONGKANDASAMY KENGMAN LARSENGSTRAND LARSHOFFNER SVEN
    • A61K31/41
    • C07D421/04A61K31/381A61K31/41C07D293/12
    • The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of E.coli TrxR with K i of 0.14 µM and 0.46 µM, respectively. E.coli mutants lacking glutathione reductase or glutathione were much more sensitive to inhibition by ebselen. Since either glutaredoxin or thioredoxin systems are electron donors to ribonucleotide reductase, ebselen targets primarily glutathione and glutaredoxin-negative bacteria, a class which includes major pathogens. Ebselen, and similar compounds are therefore useful as antibacterial agents, even for multiresistant strains. Two major pathogenic bacteria, which previously had not been known to be sensitive to ebselen, Mycobacterium tuberculosis (tuberculosis) and Helicobacter pylori (stomach ulcer and cancer), were shown to be excellent targets. Helicobacter
    • Ebselen的作用机制区分细菌和哺乳动物硫氧还蛋白还原酶(TrxR)。 它显示哺乳动物Trx的快速氧化,并且通过NADPH-TrxR催化依次硒硒酚与过氧化氢的周转,因此是哺乳动物抗氧化剂。 依布硒及其二硒化物是分别具有0.14μM和0.46μM的KI大肠杆菌TrxR的强竞争性抑制剂。 缺乏谷胱甘肽还原酶或谷胱甘肽的大肠杆菌突变体对依贝硒的抑制更敏感。 由于谷氧还蛋白或硫氧还蛋白系统是核糖核苷酸还原酶的电子供体,依普硒靶主要是谷胱甘肽和谷氧还蛋白阴性细菌,一类包括主要病原体。 因此,依布硒林和类似化合物可用作抗菌剂,即使对于多抗性菌株也是有用的。 以前不知道对ebselen,结核分枝杆菌(结核分枝杆菌)和幽门螺杆菌(胃溃疡和癌症)敏感的两种主要致病菌被证明是优异的靶标。 幽门螺杆菌