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公开(公告)号：US5712305A
公开(公告)日：1998-01-27
申请号：US687885
申请日：1996-07-26
IPC分类号： A23L1/30 , A23G1/02 , A23G1/30 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/7048 , A61K31/78 , A61K36/00 , A61K36/18 , A61K36/185 , A61P35/00 , C07D311/62 , C07D311/78 , A01N43/16
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.
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公开(公告)号：US07820713B2
公开(公告)日：2010-10-26
申请号：US11745698
申请日：2007-05-08
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。
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43.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
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。-
44.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
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。
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45.发明授权公开(公告)号：US06517841B2
公开(公告)日：2003-02-11
申请号：US09975242
申请日：2001-10-11
IPC分类号： C07D31178
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.
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公开(公告)号：US06420572B1
公开(公告)日：2002-07-16
申请号：US09169554
申请日：1998-10-09
IPC分类号： C07D31160
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。
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47.发明授权Use of cocoa solids having high cocoa polyphenol content in tabletting compositions and capsule filling compositions 失效在压片组合物和胶囊填充组合物中使用具有高可可多元酚含量的可可固体公开(公告)号：US06297273B1
公开(公告)日：2001-10-02
申请号：US08831245
申请日：1997-04-02
IPC分类号： A61K920
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-(&agr;)-OH, 3-(&bgr;)-OH, 3-(&agr;)-O-sugar, or 3-(&bgr;)-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： 公开和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，化合物和组合物的方法，以及它们的用途，特别是式An的聚合化合物，其中 A是下式的单体：其中n是2至18的整数，使得存在至少一个末端单体单元A和一个或多个另外的单体单元; R是3-（α）-OH， 3-（β）-OH，3-（α）-O-糖或3-（β）-O-糖;相邻单体之间的键合发生在位置4,6或8;附加单体单元的键 位置4具有α或β立体化学; X，Y和Z选自单体单元A，氢和糖，条件是对于至少一个末端单体单元，附加单体单元 单元（其中附加的单体单元与末端单体相邻） 单元）位于第4位并且任选地Y = Z =氢;糖任选被酚部分取代，在糖上的任何位置，例如通过酯键，以及其药学上可接受的盐或其衍生物（包括氧化产物）。
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公开(公告)号：US6156791A
公开(公告)日：2000-12-05
申请号：US198551
申请日：1998-11-23
IPC分类号： A23L1/30 , A23G1/02 , A23G1/30 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/7048 , A61K31/78 , A61K36/00 , A61K36/18 , A61K36/185 , A61P35/00 , C07D311/62 , C07D311/78 , A01N43/16
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以及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。
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公开(公告)号：US5891905A
公开(公告)日：1999-04-06
申请号：US839446
申请日：1997-04-14
IPC分类号： A23L1/30 , A23G1/02 , A23G1/30 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/7048 , A61K31/78 , A61K36/00 , A61K36/18 , A61K36/185 , A61P35/00 , C07D311/62 , C07D311/78 , A01N43/02 , A01N43/16 , A61K31/335
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。
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50.发明授权公开(公告)号：US07244855B2
公开(公告)日：2007-07-17
申请号：US10481729
申请日：2003-10-02
IPC分类号： C07D311/00
CPC分类号： C07D311/62 , C07D417/12 , C07D417/14
摘要： Various processes are disclosed for preparing procyanidin oligomers having (4,8)-interflavan linkages. In an improved process, a tetra-O-protected-epicatechin or -catechin monomer or oligomer is coupled with a protected, C-4 alkoxy-activated-epicatechin or -catechin monomer in the presence of an acidic clay instead of a Lewis acid. In a second process, a 5,7,3′,4′-tetra-O-protected or preferably penta-O-protected-epicatechin or -catechin monomer or oligomer is reacted with a tetra-O-protected or preferably penta-O-protected-epicatechin or -catechin monomer having a thio activating group at the C-4 position; the coupling is carried out in the presence of silver tetrafluoroborate. In third process, two molecules of a penta-O-protected-epicatechin or -catechin monomer activated with a 2-(benzothiazolyl)thio group at the C-4 position are self-condensed in the presence of silver tetrafluoroborate. An improved two-step process for preparing a C-4 alkoxy activated tetra-O-benzyl-protected, 8-bromo-blocked-epicatechin or -catechin monomer is also provided. 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（4,8） - 连续黄烷键的原花青素低聚物的各种方法。 在改进的方法中，在酸性粘土代替路易斯酸的情况下，将四-O-保护的表儿茶素或儿茶素单体或低聚物与受保护的C-4烷氧基 - 表儿茶素或儿茶素单体偶合。 在第二种方法中，5,7,3'，4'-四-O-保护的或优选五-O-保护的表儿茶素或儿茶素单体或低聚物与四-O-保护的或优选五-O 在C-4位具有硫代活化基团的保护表儿茶素或儿茶素单体; 在四氟硼酸银的存在下进行偶合。 在第三种方法中，在四氟硼酸银存在下，用2-（苯并噻唑基）硫基在C-4位上活化的五分子保护的表儿茶素或儿茶素单体的两分子是自缩合的。 还提供了一种用于制备C-4烷氧基活化的四-O-苄基保护的8-溴封闭的表儿茶素或儿茶素单体的改进的两步法。 还公开了使用天然衍生的和合成制备的原花青素（4beta，8）4质子以治疗癌症。
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