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    Methods and compositions to lower plasma cholesterol levels
    1.
    发明申请
    Methods and compositions to lower plasma cholesterol levels 审中-公开
    降低血浆胆固醇水平的方法和组合物

    公开(公告)号：US20050196819A1

    公开(公告)日：2005-09-08

    申请号：US11121157

    申请日：2005-05-03

    申请人： Russell Medford ,  Uday Saxena

    发明人： Russell Medford ,  Uday Saxena

    IPC分类号： A61K31/00 ,  G01N33/92 ,  G01N33/53 ,  C12Q1/60 ,  G01N33/537 ,  G01N33/543

    CPC分类号： A61K31/00 ,  G01N33/92 ,  G01N2800/044 ,  Y10S436/805 ,  Y10S436/815 ,  Y10T436/12

    摘要： A method is disclosed for determining whether a compound binds to a lipoprotein such as LDL or VLDL in a manner which will lower plasma cholesterol is provided that includes assessing the ability of the compound to form a complex with the lipoprotein, e.g., LDL or VLDL, and then determining whether the newly formed complex causes a change in the structure of apoB-100 that results in increased binding affinity to the LDL receptor. Also disclosed is a method for lowering cholesterol in a host in need thereof, including a human, is provided that includes the administration of an effective amount of a compound which binds to cholesterol-carrying lipoprotein (e.g. LDL or VLDL) in a manner that alters the three dimensional configuration of the lipoprotein and increases the binding affinity of the apoB-100 protein to the LDL receptor, including those on the surface of a hepatic cell.

    摘要翻译： 公开了一种用于确定化合物是否以降低血浆胆固醇的方式与脂蛋白如LDL或VLDL结合的方法，其包括评估化合物与脂蛋白（例如LDL或VLDL）形成复合物的能力， 然后确定新形成的复合物是否导致apoB-100的结构改变，导致对LDL受体的结合亲和力增加。 还公开了一种降低有需要的宿主（包括人）中胆固醇的方法，其包括施用有效量的与携带胆固醇的脂蛋白（例如LDL或VLDL）结合的化合物，其改变方式 脂蛋白的三维构型，并增加apoB-100蛋白与LDL受体的结合亲和力，包括肝细胞表面的结合亲和力。

    Novel Niacin Compositions for Reduction of Amyloid Beta Peptide 42 (AB42) Production and for Treatment of Alzheimer's Disease
    2.
    发明申请
    Novel Niacin Compositions for Reduction of Amyloid Beta Peptide 42 (AB42) Production and for Treatment of Alzheimer's Disease 审中-公开
    用于还原淀粉样β肽42（AB42）的新型烟酸组合物生产和治疗阿尔茨海默病

    公开(公告)号：US20130338199A1

    公开(公告)日：2013-12-19

    申请号：US13971151

    申请日：2013-08-20

    申请人： Uday Saxena ,  Venkateswarlu Akella

    发明人： Uday Saxena ,  Venkateswarlu Akella

    IPC分类号： C07D213/80

    CPC分类号： C07D213/80 ,  A61K31/085 ,  A61K31/12 ,  A61K31/192 ,  A61K31/196 ,  A61K31/455 ,  A61K2300/00

    摘要： The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (Aβ42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease, Huntington's disease, multiple sclerosis, amytrophic lateral sclerosis and ischemic stroke.

    摘要翻译： 本发明公开了（1）烟酸与α-甲氧基对羟基苯基化合物如丁子香酚，香草醛，阿朴替林，阿魏酸，异钌酸和丁子香酚环氧化物的酚酯混合物和（2）上述杂合体的共晶体，特别是共晶体 烟酸 - 丁子香酚与共晶体如丁子香酚和草酸的混合物（3）包含烟酸和一种或多种小分子/增效剂如丁子香酚，姜黄素，肉桂酸，甲氯芬那酸的组合的新型药物组合物及其在治疗 由淀粉样β肽-42（Abeta42）的过量产生引起的疾病或疾病，其沉积，积累和斑块形成，包括阿尔茨海默氏病，痴呆和轻度认知障碍以及其他神经变性疾病如帕金森病，亨廷顿舞蹈病， 多发性硬化，肌萎缩性侧索硬化和缺血性卒中。