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    Isolation, purification and synthesis of procyanidin B2 and uses thereof
    5.
    发明申请
    Isolation, purification and synthesis of procyanidin B2 and uses thereof 有权
    原花青素B2的分离，纯化和合成及其用途

    公开(公告)号：US20080306142A1

    公开(公告)日：2008-12-11

    申请号：US12119212

    申请日：2008-05-12

    申请人： Gerardo Castillo ,  Beth Nguyen ,  Paula Choi ,  Lesley Larsen ,  Stephen Lorimer ,  Alan Snow

    发明人： Gerardo Castillo ,  Beth Nguyen ,  Paula Choi ,  Lesley Larsen ,  Stephen Lorimer ,  Alan Snow

    IPC分类号： A61K31/353 ,  A61P25/28

    CPC分类号： C07D407/04 ,  C07D311/62 ,  C07D321/10 ,  C07D323/00

    摘要： Methods for the synthesis, isolation, and purification of procyanidin B2 are disclosed. The synthetic methods utilize epicatechin as a starting material and produce procyanidin B2 in high yields. The isolation methods extract procyanidin B2 from a sample of bark powder from plant matter of the genus Uncaria. The isolated and/or synthesized procyanidin B2 is used to treat amyloid disease, such as Alzheimer's disease and Parkinson's disease as well as improve cognitive performance and increase learning and memory in Alzheimer's patients. Pharmaceutical compositions containing the synthesized and/or isolated procyanidin B2 are also disclosed.

    摘要翻译： 公开了原花青素B2的合成，分离和纯化方法。 合成方法利用表儿茶素作为原料，以高产率生产原花青素B2。 分离方法从Uncaria属植物物质的树皮粉样品中提取原花青素B2。 分离和/或合成的原花青素B2用于治疗淀粉样变性疾病，如阿尔茨海默病和帕金森病，以及提高阿尔茨海默病患者的认知能力和增加学习和记忆能力。 还公开了含有合成和/或分离的原花青素B2的药物组合物。

    Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants
    6.
    发明授权
    Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants 有权
    分离淀粉样蛋白抑制化合物的方法和使用分离自Un藜和相关植物的化合物

    公开(公告)号：US07314642B2

    公开(公告)日：2008-01-01

    申请号：US10624435

    申请日：2003-07-21

    申请人： Gerardo Castillo ,  Paula Y. Choi ,  Beth Nguyen ,  Alan D. Snow

    发明人： Gerardo Castillo ,  Paula Y. Choi ,  Beth Nguyen ,  Alan D. Snow

    IPC分类号： A61K36/00 ,  A61K31/35

    CPC分类号： A61K36/74 ,  A61K31/215 ,  A61K31/353 ,  A61K2300/00

    摘要： Assay-guided affinity fractionation and reverse phase high pressure liquid chromatography (HPLC) methodology to isolate, test and characterize the most active water-soluble ingredients within Cat's Claw, or Uncaria tomentos. These components appear to account for the majority of the amyloid or Aβ fibrillogenesis inhibitory activity. Individual fractions and/or compounds as isolated by HPLC are tested in relevant in vitro and/or animal models, and found to consistently demonstrate inhibition of amyloid or Aβ fibrillogenesis. Related extraction methods are disclosed.

    摘要翻译： 测定指导的亲和力分离和反相高压液相色谱（HPLC）方法来分离，测试和表征Cat's Claw或Uncaria tomentos中最活跃的水溶性成分。 这些组分似乎占淀粉样蛋白或Abeta原纤维发生抑制活性的大部分。 在相关体外和/或动物模型中测试通过HPLC分离的各个级分和/或化合物，并且发现其一致地证明对淀粉样蛋白或Aβ原纤维生成的抑制。 公开了相关提取方法。

    Small peptides for the treatment of Alzheimer's disease and other beta-amyloid protein fibrillogenesis disorders
    8.
    发明申请
    Small peptides for the treatment of Alzheimer's disease and other beta-amyloid protein fibrillogenesis disorders 有权
    用于治疗阿尔茨海默病和其他β-淀粉样蛋白原纤维发生障碍的小肽

    公开(公告)号：US20050244334A1

    公开(公告)日：2005-11-03

    申请号：US11016706

    申请日：2004-12-16

    申请人： Gerardo Castillo ,  Thomas Lake ,  Beth Nguyen ,  Virginia Sanders ,  Alan Snow

    发明人： Gerardo Castillo ,  Thomas Lake ,  Beth Nguyen ,  Virginia Sanders ,  Alan Snow

    IPC分类号： A61K38/08 ,  A61K38/10 ,  A61K51/00

    CPC分类号： A61K38/08 ,  A61K38/10 ,  C07K7/08 ,  G01N33/6896 ,  G01N2800/2821

    摘要： A pharmaceutical composition that includes a peptide of formula Y-(X-aa)-Z. (X-aa) is generally an amino acid sequence selected from -Arg-Val-Ser-Val-Arg-Trp-, -Arg-Val-Ala-Val-Ile-, -His-Gly-Arg-Leu-Val-Phe-, -Leu-Ala-Phe-Val-Leu-Arg-, and -Thr-Leu-Phe-Leu-Ala-Arg-. And Y is generally an amino terminal modifying group selected from an amino acid, a N-acylated amino acid, a peptide, a N-acylated peptide, and hydrogen. And Z- is carboxyl-terminal modifying group selected from hydrogen, an amino acid, a C-amidated amino acid, a peptide, a C-amidated peptide, or an amide or hydroxyl group such as an alkyl amide, an aryl amide, or an alcohol. A composition of matter that includes at least one of the peptide sequences -Arg-Val-Ala-Val-Ile-, -Leu-Ala-Phe-Val-Leu-Arg-, -Thr-Leu-Phe-Leu-Ala-Arg-, -Arg-Val-Ser-Val-Arg-Trp-, -His-Gly-Arg-Leu-Val-Phe-. Preferably at least one amino acid of the peptide sequence is a D-amino acid.

    摘要翻译： 一种药物组合物，其包含式Y-（X-aa）-Z的肽。 （X-aa）通常是选自-Arg-Val-Ser-Val-Arg-Trp-，-Arg-Val-Ala-Val-Ile-，-His-Gly-Arg-Leu-Val- Phe-，-Leu-Ala-Phe-Val-Leu-Arg-和-Thr-Leu-Phe-Leu-Ala-Arg-。 Y通常是选自氨基酸，N-酰化氨基酸，肽，N-酰化肽和氢的氨基末端修饰基团。 Z-是选自氢，氨基酸，C-酰胺化氨基酸，肽，C-酰胺化肽或酰胺或羟基的羧基末端修饰基团，例如烷基酰胺，芳基酰胺或 一个酒精。 包含至少一个肽序列-Arg-Val-Ala-Val-Ile-，-Leu-Ala-Phe-Val-Leu-Arg-，-Thr-Leu-Phe-Leu-Ala- Arg-，-Arg-Val-Ser-Val-Arg-Trp-，-His-Gly-Arg-Leu-Val-Phe-。 优选地，肽序列的至少一个氨基酸是D-氨基酸。

    Isolation, purification and synthesis of procyanidin B2 and uses thereof
    10.
    发明授权
    Isolation, purification and synthesis of procyanidin B2 and uses thereof 有权
    原花青素B2的分离，纯化和合成及其用途

    公开(公告)号：US09133176B2

    公开(公告)日：2015-09-15

    申请号：US12119212

    申请日：2008-05-12

    申请人： Gerardo Castillo ,  Beth Nguyen ,  Paula Choi ,  Lesley Larsen ,  Stephen Lorimer ,  Alan Snow

    发明人： Gerardo Castillo ,  Beth Nguyen ,  Paula Choi ,  Lesley Larsen ,  Stephen Lorimer ,  Alan Snow

    IPC分类号： C07D323/00 ,  C07D321/00 ,  C07D311/00 ,  C07D407/04 ,  C07D321/10 ,  C07D311/62

    CPC分类号： C07D407/04 ,  C07D311/62 ,  C07D321/10 ,  C07D323/00

    摘要： Methods for the synthesis, isolation, and purification of procyanidin B2 are disclosed. The synthetic methods utilize epicatechin as a starting material and produce procyanidin B2 in high yields. The isolation methods extract procyanidin B2 from a sample of bark powder from plant matter of the genus Uncaria. The isolated and/or synthesized procyanidin B2 is used to treat amyloid disease, such as Alzheimer's disease and Parkinson's disease as well as improve cognitive performance and increase learning and memory in Alzheimer's patients. Pharmaceutical compositions containing the synthesized and/or isolated procyanidin B2 are also disclosed.

    摘要翻译： 公开了原花青素B2的合成，分离和纯化方法。 合成方法利用表儿茶素作为原料，以高产率生产原花青素B2。 分离方法从Uncaria属植物物质的树皮粉样品中提取原花青素B2。 分离和/或合成的原花青素B2用于治疗淀粉样变性疾病，如阿尔茨海默病和帕金森病，以及提高阿尔茨海默病患者的认知能力和增加学习和记忆能力。 还公开了含有合成和/或分离的原花青素B2的药物组合物。