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19 条记录 (耗时 0.025 秒)

    Synthetic methods for preparing procyanidin oligomers
    1.
    发明申请
    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：US20040176441A1

    公开(公告)日：2004-09-09

    申请号：US10798131

    申请日：2004-03-11

    申请人： Mars Incorporated

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

    IPC分类号： C07D45/14 ,  A61K031/353

    CPC分类号： C07D311/32 ,  Y02P20/55

    摘要： Processes are disclosed for the production of linear and branched procyanidin oligomers having nullnnull 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 (4null8) 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 (8null8), (8null6), and (6null6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (null)-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。

    Partially purified cocoa extracts containing cocoa polyphenols
    3.
    发明申请
    Partially purified cocoa extracts containing cocoa polyphenols 有权
    含可可多酚的部分纯化可可提取物

    公开(公告)号：US20020004523A1

    公开(公告)日：2002-01-10

    申请号：US09768473

    申请日：2001-01-24

    申请人： Mars, Incorporated

    发明人： Leo J. Romanczyk JR. ,  John F. Hammerstone JR. ,  Margaret M. Buck

    IPC分类号： A01N043/16 ,  A61K031/35 ,  C07D313/00

    CPC分类号： A61K31/78 ,  A23L33/105 ,  A61K31/353 ,  A61K36/185 ,  C07D311/62

    摘要： Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.

    摘要翻译： 披露和要求的是可可提取物如多酚或原花青素，制备这些提取物的方法，以及它们的用途，特别是抗肿瘤剂和抗氧化剂。 披露和要求的是含有可可多元酚或原花青素的抗肿瘤组合物和用于治疗使用该组合物的患者的方法。 另外公开并要求保护的是用于治疗需要用含有可可多元酚或原花青素的抗肿瘤剂治疗的患者以及含有可可多元酚或原花青素的冻干抗肿瘤组合物的试剂盒。 此外，公开并要求保护的是本发明在抗氧化剂，防腐剂和拓扑异构酶抑制组合物和方法中的用途。

    Synthetic methods for preparing procyanidin oligomers
    6.
    发明申请
    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：US20030114691A1

    公开(公告)日：2003-06-19

    申请号：US10212973

    申请日：2002-08-06

    申请人： Mars Incorporated

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

    IPC分类号： 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 nullnnull 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 (4null8) 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 (8null8), (8null6), and (6null6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (null)-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。

    Synthesis of 4alpha-arylepicatechins
    7.
    发明申请
    Synthesis of 4alpha-arylepicatechins 失效

    公开(公告)号：US20030100775A1

    公开(公告)日：2003-05-29

    申请号：US10214830

    申请日：2002-08-08

    申请人： Mars Incorporated

    发明人： Alan P. Kozikowski ,  Leo J. Romanczyk JR. ,  Werner Tuckmantel

    IPC分类号： C07D311/74

    CPC分类号： C07D311/74 ,  C07D311/62 ,  Y02P20/55

    摘要： Oligomeric procyanidins containing 4null-linked epicatechin units are rare in nature and have hitherto not been accessible through stereoselective synthesis. Provided herein is the preparation of the prototypical dimer, epicatechin-4null,8-epicatechin, by reaction of the protected 4-ketones with aryllithium reagents derived by halogen/metal exchange from the aryl bromides. Removal of the 4-hydroxyl group from the resulting tertiary benzylic alcohols is effected by tri-n-butyltin hydride and trifluoroacetic acid in a completely stereoselective manner, resulting in hydride delivery exclusively from the null face.

    Dimer digallate compositions
    8.
    发明申请
    Dimer digallate compositions 审中-公开
    二聚体digallate组合物

    公开(公告)号：US20040235941A1

    公开(公告)日：2004-11-25

    申请号：US10867160

    申请日：2004-06-14

    申请人： Mars, Incorporated

    发明人： Leo J. Romanczyk JR. ,  Marc E. Lippman

    IPC分类号： C08G002/00 ,  A61K031/353 ,  C07D45/14

    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 monomeric units, 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 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

    摘要翻译： 公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为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单体单元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单元可以是相同或不同的类黄酮化合物。

    Solid compositions and liquid preparations for oral administration which contain cocoa polyphenols
    9.
    发明申请
    Solid compositions and liquid preparations for oral administration which contain cocoa polyphenols 有权
    用于口服给药的固体组合物和液体制剂，其含有可可多酚

    公开(公告)号：US20020049166A1

    公开(公告)日：2002-04-25

    申请号：US09975242

    申请日：2001-10-11

    申请人： Mars Incorporated

    发明人： Leo J. Romanczyk JR. ,  John F. Hammerstone JR. ,  Margaret M. Buck

    IPC分类号： A61K031/7048 ,  A61K035/78

    CPC分类号： A61K31/78 ,  A23L33/105 ,  A61K31/353 ,  A61K36/185 ,  C07D311/62

    摘要： Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.

    摘要翻译： 披露和要求的是可可提取物如多酚或原花青素，制备这些提取物的方法，以及它们的用途，特别是抗肿瘤剂和抗氧化剂。 披露和要求的是含有可可多元酚或原花青素的抗肿瘤组合物和用于治疗使用该组合物的患者的方法。 另外公开并要求保护的是用于治疗需要用含有可可多元酚或原花青素的抗肿瘤剂治疗的患者以及含有可可多元酚或原花青素的冻干抗肿瘤组合物的试剂盒。 此外，公开并要求保护的是本发明在抗氧化剂，防腐剂和拓扑异构酶抑制组合物和方法中的用途。