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    Cocoa extracts as antioxidants
    2.
    发明授权
    Cocoa extracts as antioxidants 有权
    可可提取物作为抗氧化剂

    公开(公告)号：US07820713B2

    公开(公告)日：2010-10-26

    申请号：US11745698

    申请日：2007-05-08

    申请人： Leo J. Romanczyk, Jr. ,  John F. Hammerstone, Jr. ,  Margaret M. Buck

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

    IPC分类号： A01N43/16 ,  A61K31/35 ,  C07D313/00 ,  A23L1/28

    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 topoisomerase-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。

    Preparation of (+)-Catechin, (-)-Epicatechin, (-)-Catechin, and (+)-Epicatechin and Their 5,7,3',4'-Tetra-O-Benzyl Analogues
    5.
    发明申请
    Preparation of (+)-Catechin, (-)-Epicatechin, (-)-Catechin, and (+)-Epicatechin and Their 5,7,3',4'-Tetra-O-Benzyl Analogues 审中-公开
    （+） - 儿茶素，（ - ） - 表儿茶素，（ - ） - 儿茶素和（+） - 表儿茶素及其5,7,3'，4'-四-O-苄基类似物

    公开(公告)号：US20100048920A1

    公开(公告)日：2010-02-25

    申请号：US11993141

    申请日：2006-06-28

    申请人： Leo J. Romanczyk, JR. ,  Pradeep K. Sharma ,  Daming Gou ,  Yanni Gou

    发明人： Leo J. Romanczyk, JR. ,  Pradeep K. Sharma ,  Daming Gou ,  Yanni Gou

    IPC分类号： C07D311/02 ,  C07C45/78

    CPC分类号： C07C41/18 ,  C07C45/71 ,  C07C45/74 ,  C07D311/62 ,  C07C49/84 ,  C07C47/575 ,  C07C43/23

    摘要： Processes for preparing racemic mixtures of 5,7,3′,4′-tetra-O-benzyl-(±)-catechin and (±)-epicatechin involves (i) condensing 2-hydroxy-4,6-bis(benzyloxy)-acetophenone and 3,4-bis(benzyloxy)benzaldehyde, cyclizing the resulting compound, oxidizing the resulting compound; (ii) dihydroxylating (E)-3-(3′,4′-bis(benzyloxy)phenyl)prop-2-ene-1-ol and reducing the 1,2-diol; or (iii) coupling 3,5-bis(benzyloxy)phenol with (E)-3,5-bis(benzyloxy)-2-(3′,4′-bis(benzyloxy)phenyl)allyl)phenol and cyclizing the resulting chalcone.A process for preparing the benzylated epimers of catechin and epicatechin involves seven steps. 3,4-Bis(benzyloxy)benzaldehyde is coupled with 2-hydroxy-4,6-benzyloxy-acetophenone to form a chalcone. The chalcone is selectively reduced to an alkene. The phenolic group of the alkene is protected. The protected alkene is asymetrically dihydroxylated. The resulting compound is deprotected, cyclized, and finally hydrolyzed.Epimers resulting from these processes are chemically resolved or separated by chiral high pressure liquid chromatography.Also disclosed is a method for preparing enantiomerically pure 5,7,3′,4′-tetra-O-benzyl-(+)-catechin from a racemic mixture using dibenzoyl-L-tartaric acid monomethyl ester.Further, disclosed is an improved process for preparing dibenzoyl-L-tartaric acid monomethyl ester.

    摘要翻译： 制备5,7,3'，4'-四-O-苄基 - （±） - 儿茶素和（±） - 表儿茶素的外消旋混合物的方法包括（i）将2-羟基-4,6-双（苄氧基） 苯乙酮和3,4-双（苄氧基）苯甲醛，使所得化合物环化，氧化所得化合物; （ⅱ）二羟基化（E）-3-（3'，4'-双（苄氧基）苯基）丙-2-烯-1-醇并还原1,2-二醇; 或（iii）将3,5-二（苄氧基）苯酚与（E）-3,5-双（苄氧基）-2-（3'，4'-双（苄氧基）苯基）烯丙基）苯偶合并使所得 查耳酮 制备儿茶素和表儿茶素的苄化的差向异构体的方法涉及七个步骤。 将3,4-双（苄氧基）苯甲醛与2-羟基-4,6-苄氧基 - 苯乙酮偶联以形成查耳酮。 查耳酮选择性还原成烯烃。 烯烃的酚基被保护。 受保护的烯是非对称二羟基化的。 将所得化合物脱保护，环化，最后水解。 通过手性高压液相色谱法化学拆分或分离由这些方法得到的异构体。 还公开了使用二苯甲酰基-L-酒石酸单甲酯从外消旋混合物制备对映体纯的5,7,3'，4'-四-O-苄基 - （+） - 儿茶素的方法。 此外，公开了二苯甲酰基-L-酒石酸单甲酯的改进方法。

    Tetra- and penta-o-benzyl-protected, C-4 activated-epicatechin and -catechin monomers and processes for their preparation and use
    6.
    发明授权
    Tetra- and penta-o-benzyl-protected, C-4 activated-epicatechin and -catechin monomers and processes for their preparation and use 失效
    四 - 和五 - 邻 - 苄基保护的C-4活化表儿茶素和儿茶素单体及其制备和使用方法

    公开(公告)号：US07507831B2

    公开(公告)日：2009-03-24

    申请号：US11329467

    申请日：2006-01-11

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

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

    IPC分类号： C07D417/12 ,  C07D311/30

    CPC分类号： C07D311/62 ,  C07D417/12 ,  C07D417/14

    摘要： Various processes are disclosed for preparing protected epicatechin oligomers having (4β,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3′,4′-benzyl protected or a 3 -acetyl-, 5,7,3′,4′-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3 -O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3′,4′-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3′,4′-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio) epicatechin or catechin. The use of naturally-derived and synthetically-prepared procyanidin (4β,8)4-pentamers to treat cancer is also disclosed.

    摘要翻译： 公开了用于制备具有（4beta，8） - 间连环的保护的表儿茶素低聚物的各种方法。 在一个方法中，四氧化物保护的表儿茶素单体或低聚物在保护的C-4活化的表儿茶素单体的存在下，在酸性粘土如失
    桑土粘土的存在下偶合。 在另一种方法中，将5,7,3'，4'-苄基保护或3-乙酰基，5,7,3'，4'-苄基保护的表儿茶素或儿茶素单体或低聚物与3-O-乙酰基 -4 - [（2-苯并噻唑基）硫基] -5,7,3'，4'-四-O-苯甲酸酯在四氟硼酸银的存在下反应。 在另一种方法中，在C-4位上用2-（苯并噻唑基）硫基活化的两个5,7,3'，4'-苄基保护的表儿茶素单体在四氟硼酸银的存在下交联。 还公开了使未保护的表儿茶素或儿茶素单体与4-（苄硫基）表儿茶素或儿茶素反应的方法。 还公开了使用天然衍生的和合成制备的原花青素（4beta，8）4-五聚体来治疗癌症。

    Food products containing polyphenol(s) and L-arginine to stimulate nitric oxide
    8.
    发明授权
    Food products containing polyphenol(s) and L-arginine to stimulate nitric oxide 有权
    食品中含有多酚和L-精氨酸刺激一氧化氮

    公开(公告)号：US06805883B2

    公开(公告)日：2004-10-19

    申请号：US10176126

    申请日：2002-06-19

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

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

    IPC分类号： A61K3578

    CPC分类号： A23G1/44 ,  A23G1/48 ,  A23G1/56 ,  A23G2200/10 ,  A23G2200/14 ,  A23L33/105 ,  A23L33/175 ,  A23V2002/00 ,  A61K31/197 ,  A61K36/185 ,  A61K2300/00 ,  A23V2250/2132 ,  A23V2250/0606

    摘要： Foods and pharmaceuticals which contain cocoa and/or nut procyanidin(s) in combination with L-arginine are effective to induce a physiological increase in nitric oxide production in a mammal having ingested the product. A preferred food product is a confection, particularly a dark or milk chocolate containing nuts. The procyanidins may be natural or synthetic and may be provided by food ingredients such as chocolate liquor and/or cocoa solids prepared from underfermented beans and nut skins. The L-arginine may be natural or synthetic and may be provided by food ingredients such as nut meats, nut pastes, and/or nut flours, seeds, seed pastes, and/or seed flours, or gelatin. The beneficial health effects may include, for example, reduced blood pressure, resistance to cardiovascular disease, and anticancer activity.

    摘要翻译： 含有可可和/或坚果原花青素与L-精氨酸组合的食品和药物有效地诱导摄入该产品的哺乳动物中一氧化氮产生的生理增加。 优选的食品是甜食，特别是含有坚果的黑色或牛奶巧克力。 原花青素可以是天然的或合成的，并且可以由食物成分提供，例如由未发酵的豆和坚果皮制备的巧克力浆和/或可可固体。 L-精氨酸可以是天然的或合成的，并且可以由食品成分例如坚果肉，坚果糊和/或坚果面粉，种子，种子糊和/或种子面粉或明胶提供。 有益的健康影响可以包括例如降低血压，抗心血管疾病和抗癌活性。

    Cocoa extracts containing solvent-derived cocoa polyphenols from defatted cocoa beans
    9.
    发明授权
    Cocoa extracts containing solvent-derived cocoa polyphenols from defatted cocoa beans 失效
    含脱脂可可豆的溶剂衍生可可多酚的可可提取物

    公开(公告)号：US06790966B2

    公开(公告)日：2004-09-14

    申请号：US10342772

    申请日：2003-01-15

    申请人： Leo J. Romanczyk, Jr. ,  John F. Hammerstone, Jr. ,  Margaret M. Buck

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

    IPC分类号： A23F500

    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。

    Synthesis of epecatechin-4&agr;, 8-epicatechin dimers and derivatives thereof
    10.
    发明授权
    Synthesis of epecatechin-4&agr;, 8-epicatechin dimers and derivatives thereof 失效
    表儿茶素-4α，8-表儿茶素二聚体及其衍生物的合成

    公开(公告)号：US06720432B2

    公开(公告)日：2004-04-13

    申请号：US10214830

    申请日：2002-08-08

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

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

    IPC分类号： C07D31500

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

    摘要： Oligomeric procyanidins containing 4&agr;-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-4&agr;,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 &bgr; face.

    摘要翻译： 含有4α-连接的表儿茶素单元的低聚原花青素在自然界中是罕见的，并且迄今尚未通过立体选择性合成进行。 本文提供了通过将受保护的4-酮与芳基溴化物的卤素/金属交换衍生的芳基锂试剂反应制备原型二聚体，表儿茶素-4α，8-表儿茶素。 从所得叔苄醇中除去4-羟基由三正丁基锡氢化物和三氟乙酸以完全立体选择的方式进行，从而产生仅从β面产生的氢化物。