Perlecan transgenic animals and methods of identifying compounds for the treatment of amyloidoses
    1.
    发明授权
    Perlecan transgenic animals and methods of identifying compounds for the treatment of amyloidoses 有权
    Perlecan转基因动物和鉴定用于治疗淀粉样变性的化合物的方法

    公开(公告)号:US06563016B1

    公开(公告)日:2003-05-13

    申请号:US09536231

    申请日:2000-03-27

    IPC分类号: A01K6700

    摘要: The invention provides a transgenic non-human animal expressing a perlecan encoding transgene. Also provided is a double-transgenic non-human animal expressing a perlecan and a amyloid encoding transgene. A method of screening for a compound which alters the rate or extent of amyloid deposition is additionally provided. The method consists of: (a) constructing a perlecan transgenic animal; (b) administering an effective amount of a test compound to said perlecan transgenic animal; and (c) determining whether said test compound alters the extent or rate of amyloid deposition. Finally, the invention provides a method of screening for a compound which alters the rate or extent of amyloid deposition. The method consists of: (a) constructing a perlecan/amyloid double-transgenic animal; (b) administering an effective amount of a test compound to said perlecan/amyloid double-transgenic animal; and (c) determining whether said test compound alters the extent or rate of amyloid deposition.

    摘要翻译: 本发明提供了表达编码转基因的全基因组的转基因非人动物。 还提供了表达perlecan和编码转基因淀粉样蛋白的双转基因非人动物。 另外提供筛选改变淀粉样蛋白沉积速度或程度的化合物的方法。 该方法包括:(a)构建一个全基因组转基因动物; (b)向所述perlecan转基因动物施用有效量的测试化合物; 和(c)确定所述测试化合物是否改变淀粉样蛋白沉积的程度或速率。 最后,本发明提供了筛选改变淀粉样蛋白沉积速度或程度的化合物的方法。 该方法包括:(a)构建一个perlecan /淀粉样蛋白双转基因动物; (b)向所述perlecan /淀粉样蛋白双转基因动物施用有效量的测试化合物; 和(c)确定所述测试化合物是否改变淀粉样蛋白沉积的程度或速率。

    Compounds, Compositions and Methods for the Treatment of Inflammatory Diseases
    5.
    发明申请
    Compounds, Compositions and Methods for the Treatment of Inflammatory Diseases 失效
    化合物,组合物和治疗炎症疾病的方法

    公开(公告)号:US20120058998A1

    公开(公告)日:2012-03-08

    申请号:US13268170

    申请日:2011-10-07

    CPC分类号: A61K31/055

    摘要: A method of inhibiting the inflammatory process, the method comprising administering to a mammal suffering from inflammation a therapeutically effective amount of a pharmaceutical composition comprising a compound where: R is a C1-C10 alkylene group, in which, when the number of carbon atoms is at least 2, there are optionally 1 or 2 non-adjacent double bonds; 1 to 3 non-adjacent methylene groups are optionally replaced by NR1 (where R1 is H, alkyl, or acyl), O, or S; and 1 or 2 methylene groups are optionally replaced by a carbonyl or hydroxymethylene group and pharmaceutically acceptable esters or salts of the compounds and wherein the inflammatory process results from a disease selected from the group consisting of ulcerative colitis, endotoxic shock, rheumatoid arthritis, juvenile arthritis, osteoarthritis, psoriasis, Crohn's disease, inflammatory bowel disease, multiple sclerosis, insulin dependent diabetes mellitus, gout, psoriatic arthritis, reactive arthritis, vital or post-viral arthritis and ankylosing spondylarthritis.

    摘要翻译: 一种抑制炎症过程的方法,所述方法包括向患有炎症的哺乳动物施用治疗有效量的药物组合物,其包含化合物,其中:R是C1-C10亚烷基,其中当碳原子数为 至少2个,可选地是1或2个不相邻的双键; 1至3个不相邻的亚甲基任选被NR 1(其中R 1是H,烷基或酰基),O或S取代; 和1或2个亚甲基任选地被羰基或羟基亚甲基和化合物的药学上可接受的酯或盐代替,并且其中所述炎性过程由选自溃疡性结肠炎,内毒素性休克,类风湿性关节炎,幼年型关节炎 ,骨关节炎,牛皮癣,克罗恩病,炎性肠病,多发性硬化,胰岛素依赖性糖尿病,痛风,银屑病关节炎,反应性关节炎,重要或后病毒性关节炎和强直性脊柱关节炎。

    PROANTHOCYANIDINS FOR THE TREATMENT OF AMYLOID AND ALPHA-SYNUCLEIN DISEASES
    7.
    发明申请
    PROANTHOCYANIDINS FOR THE TREATMENT OF AMYLOID AND ALPHA-SYNUCLEIN DISEASES 审中-公开
    用于治疗淀粉样变性和阿尔茨海默病的PROANTHOCYANIDINS

    公开(公告)号:US20100197778A1

    公开(公告)日:2010-08-05

    申请号:US12475097

    申请日:2009-05-29

    摘要: A method of treating an amyloid disease, or a disease characterized by IAPP amyloid fibrils or islet amyloid deposits, in a mammalian subject. The method includes administering to the mammal a therapeutically effective amount of a various disclosed procyanidins or proanthocyanidins characterized by disclosed general formulae. A pharmaceutical composition and use of the composition comprising a therapeutically effective amount of a procyanidin and a pharmaceutically acceptable excipient. The therapeutic amount of the proanthocyanidin is selected for efficacy in treating IAPP amyloid fibrils or islet amyloid deposits in a mammalian subject.

    摘要翻译: 哺乳动物受试者中治疗淀粉样蛋白病或IAPP淀粉样蛋白原纤维或胰岛淀粉样沉积物特征的疾病的方法。 该方法包括向哺乳动物施用治疗有效量的各种所​​公开的原花青素或原花青素,其特征在于所公开的通式。 药物组合物和组合物的用途,其包含治疗有效量的原花青素和药学上可接受的赋形剂。 选择原花青素的治疗量用于在哺乳动物受试者中治疗IAPP淀粉样蛋白原纤维或胰岛淀粉样蛋白沉积物的功效。

    Substituted N-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies
    8.
    发明授权
    Substituted N-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies 有权
    取代的N-芳基苯甲酰胺和相关化合物用于治疗淀粉样蛋白病和突触核蛋白病

    公开(公告)号:US07745490B2

    公开(公告)日:2010-06-29

    申请号:US11328748

    申请日:2006-01-09

    IPC分类号: C07C303/00 A01N41/06

    CPC分类号: C07C311/08

    摘要: Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.

    摘要翻译: 取代的正芳基苯甲酰胺,相关化合物及其药学上可接受的衍生物,其合成,含有它们的药物组合物及其在治疗淀粉样蛋白疾病中的用途,包括A&bgr; 提供淀粉样变性,例如在阿尔茨海默病中观察到的,IAPP淀粉样变性,例如在2型糖尿病中观察到的,以及突触核蛋白病,例如在帕金森病中观察到的,并且制备用于这种治疗的药物。