Rapid induction of Alzheimer's amyloid plaque formation by sulfated glycosaminoglycans
    6.
    发明申请
    Rapid induction of Alzheimer's amyloid plaque formation by sulfated glycosaminoglycans 审中-公开
    通过硫酸化糖胺聚糖快速诱导阿尔茨海默氏淀粉样斑块形成

    公开(公告)号:US20080044917A1

    公开(公告)日:2008-02-21

    申请号:US11487149

    申请日:2006-07-14

    Abstract: A method of induction of amyloid plaques includes immobilizing a quantity of a selected sulfated glycosaminoglycan (SGAG) on a selected medium and adding to the immobilized SGAG on the medium a quantity of dissolved low fibrillar Aβ 1-40 (LFAβ). The LFAβ is added preferably in a Aβ:SGAG w/w ratio of about 1:1. SGAGs are preferably selected from heparin, heparan sulfate, keratan sulfate, dermatan sulfate, chondroitin-4-sulfate and chondroitin-6-sulfate. Screening methods and kits for screening either immobilize a quantity of a selected sulfated glycosaminoglycan (SGAG) on a selected medium, followed by adding to a quantity of dissolved low fibrillar Aβ 1-40 (LFAβ) a selected quantity of the selected amyloid therapeutic candidate to create a test solution, and then adding to the immobilized SGAG on the medium a selected quantity of the test solution to test for inhibition, or preform amyloid plaques on the medium by immobilizing a quantity of a selected sulfated glycosaminoglycan (SGAG) or a GAG-related macromolecule on a selected medium and then adding a selected quantity of dissolved low fibrillar Aβ 1-40 (LFAβ), followed by adding to the amyloid plaques on the medium a selected quantity of a test solution of a selected amyloid therapeutic candidate to test for disruption.

    Abstract translation: 诱导淀粉样蛋白斑块的方法包括将一定数量的选择的硫酸葡糖胺聚糖(SGAG)固定在选定的培养基上,并向培养基上的固定化SGAG加入一定量的溶解的低纤维Aβ1-40(LFAbeta)。 LFAbeta优选以约1:1的Abeta:SGAG w / w比添加。 SGAG优选选自肝素,硫酸乙酰肝素,硫酸角质素,硫酸皮肤素,硫酸软骨素-4-硫酸盐和硫酸软骨素-6-硫酸盐。 用于筛选的筛选方法和试剂盒在选定的培养基上固定一定量的选择的硫酸葡糖胺聚糖(SGAG),然后将一定量的所选择的淀粉样蛋白治疗候选物加入到一定量的溶解的低纤维Aβ1-40(LFAbeta)中 产生一个测试溶液,然后在培养基上加入一定量的测试溶液中的固定化SGAG以测试抑制,或者通过将一定量的选择的硫酸糖胺聚糖(SGAG)或GAG- 然后加入选定量的溶解的低纤维Abeta 1-40(LFAbeta),然后向培养基上的淀粉样蛋白斑添加选定量的所选淀粉样蛋白治疗候选物的测试溶液,以测试 中断

    Compounds, compositions and methods for the treatment of inflammatory diseases
    8.
    发明授权
    Compounds, compositions and methods for the treatment of inflammatory diseases 失效
    用于治疗炎性疾病的化合物,组合物和方法

    公开(公告)号:US08754133B2

    公开(公告)日:2014-06-17

    申请号:US13268170

    申请日:2011-10-07

    CPC classification number: A61K31/055

    Abstract: 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.

    Abstract translation: 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。

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