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    • 2. 发明申请
    • AGENTS FOR TREATMENT OF DIABETIC RETINOPATHY AND DRUSEN FORMATION IN MACULAR DEGENERATION
    • 用于治疗糖尿病肾病和乳腺癌形成的代谢物
    • WO2005063249A1
    • 2005-07-14
    • PCT/US2004/042562
    • 2004-12-17
    • ALCON, INC.LANDERS, Robert A.BINGAMAN, David P.
    • LANDERS, Robert A.BINGAMAN, David P.
    • A61K31/497
    • A61K31/26A61K31/352A61K31/497
    • Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating diabetic retinopathy or drusen formation in age-related macular degeneration. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid other than genistein, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.
    • 在年龄相关性黄斑变性中治疗糖尿病性视网膜病变或玻璃疣形成的方法中提供了刺激Nrf2蛋白的核易位和随后增加解毒和消除细胞毒性代谢物的基因产物的试剂。 作用于Nrf2 / ARE途径的结构不同的试剂诱导具有化学通用的细胞保护性质的酶和蛋白质的表达,并且是防止有毒代谢物和异生物。 药剂包括某些亲电试剂和氧化剂如迈克尔加成受体,二酚,硫代氨基甲酸酯,醌,1,2-二硫杂环戊烯-3-硫酮,丁基化羟基苯甲醚,除了染料木黄酮以外的类黄酮,异硫氰酸酯,3,5-二叔丁基 - 4-羟基甲苯,乙氧喹,香豆素,其组合,或其药理活性衍生物或类似物。