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    Synthetic methods for preparing procyanidin oligomers
    3.
    发明授权
    Synthetic methods for preparing procyanidin oligomers 失效
    原花青素低聚物的合成方法

    公开(公告)号：US07282598B2

    公开(公告)日：2007-10-16

    申请号：US10798131

    申请日：2004-03-11

    申请人： Leo J. Romanczyk, Jr. ,  Amit Basak ,  Craig A. Townsend

    发明人： Leo J. Romanczyk, Jr. ,  Amit Basak ,  Craig A. Townsend

    IPC分类号： C07D311/04 ,  C07D311/74 ,  C07D311/76 ,  C07D313/00

    CPC分类号： C07D311/32 ,  Y02P20/55

    摘要： Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4→8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8→8), (8→6), and (6→6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (−)-epicatechin is produced under certain conditions.

    摘要翻译： 公开了用于生产具有“n”原花青素单体单元（其中n为2至18）的直链和支链原花青素低聚物的方法。该方法包括将保护的活化单体与未保护的单体偶联以产生部分保护的（4-> 8）二聚体 。 将二聚体任选地封闭，与活化的受保护的单体偶联以产生部分保护的，任选被封闭的三聚体并脱保护。 可以重复这些步骤以产生更高级的低聚物。 还提供了制备（8-> 8），（8-> 6）和（6-> 6）二聚体和双支链低聚物的方法。 在某些条件下制备8-溴四-O-苄基（ - ） - 表儿茶素的结晶。

    Compositions for, and methods of, treating atherosclerosis
    4.
    发明授权
    Compositions for, and methods of, treating atherosclerosis 有权
    治疗动脉粥样硬化的组合物和方法

    公开(公告)号：US06998417B2

    公开(公告)日：2006-02-14

    申请号：US10127817

    申请日：2002-04-22

    申请人： Leo J. Romanczyk, Jr. ,  Harold H. Schmitz

    发明人： Leo J. Romanczyk, Jr. ,  Harold H. Schmitz

    IPC分类号： A61K31/352 ,  C07D311/62

    CPC分类号： C07H17/06 ,  A23G1/32 ,  A23G3/36 ,  A23K20/111 ,  A23K50/40 ,  A61K9/2018 ,  A61K9/2068 ,  A61K9/4858 ,  A61K31/353 ,  A61K31/7048 ,  A61K36/185 ,  A61K45/06 ,  C07D311/32 ,  C07D311/62 ,  C07D311/64 ,  C11B5/0035 ,  A61K2300/00

    摘要： Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(α)—OH, 3-(β)—OH, 3-(α)—O-sugar, or 3-(β)—O-sugar; bonding between adjacent monomers takes place at positions 4, 6 or 8; a bond of an additional monomeric unit in position 4 has alpha or beta stereochemistry; X, Y and Z are selected from the group consisting of monomeric unit A, hydrogen, and a sugar, with the provisos that as to the at least one terminal monomeric unit, bonding of the additional monomeric unit thereto (the bonding of the additional monomeric unit adjacent to the terminal monomeric unit) is at position 4 and optionally Y=Z=hydrogen; the sugar is optionally substituted with a phenolic moiety, at any position on the sugar, for instance via an ester bond, and pharmaceutically acceptable salts or derivatives thereof (including oxidation products).

    摘要翻译： 公开并要求保护的是可可提取物，化合物，其组合和含有它们的组合物，例如多酚或原花青素，制备此类提取物的方法，化合物和组合物，以及它们的用途，特别是式A的< > n ，其中A是甲醛的单体

    Use of procyanidins in the maintenance of vascular health and modulation of the inflammatory response
    8.
    发明授权
    Use of procyanidins in the maintenance of vascular health and modulation of the inflammatory response 有权
    使用原花青素维持血管健康和调节炎症反应

    公开(公告)号：US06469053B1

    公开(公告)日：2002-10-22

    申请号：US09507717

    申请日：2000-02-18

    申请人： Leo J. Romanczyk, Jr. ,  Harold H. Schmitz

    发明人： Leo J. Romanczyk, Jr. ,  Harold H. Schmitz

    IPC分类号： A61K31353

    CPC分类号： A61K36/185 ,  A61K9/2068 ,  A61K31/353 ,  C07D311/62 ,  C07H17/06

    摘要： Cocoa extracts which include procyanidin monomers and their oligomers are useful in the modulation of inflammatory pathways, in the maintenance of the vascular health of a mammal and as an antibacterial treatment. The liquid or dry cocoa extracts can be included in foods, food supplements and pharmaceuticals for the inhibition of COX activity, the inhibition of LOX activity, the enhancement of nitric oxide production, the modulation of eicosanoids and endothelin, and the modulation of platelet activity.

    摘要翻译： 包括原花青素单体及其低聚物的可可提取物可用于调节炎症途径，维持哺乳动物的血管健康和作为抗菌治疗。 液体或干可可提取物可以包括在食品，食品添加剂和药物中，用于抑制COX活性，抑制LOX活性，增强一氧化氮产生，类花生酸和内皮素的调节以及血小板活性的调节。

    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives
    9.
    发明授权
    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives 失效
    原花青素（4-6或4-8）寡聚体及其衍生物的制备方法

    公开(公告)号：US06207842B1

    公开(公告)日：2001-03-27

    申请号：US08948226

    申请日：1997-10-09

    申请人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    发明人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    IPC分类号： C07D31126

    CPC分类号： C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomers, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomers. Advantageously, polyphenol monomers forming the polyphenol oligomers may be the same or different.

    摘要翻译： 公开了一种制备具有n多酚单体的多酚低聚物的方法，n是2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17个单体的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体可以相同或不同。