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1. 发明申请

US20040176441A1 Synthetic methods for preparing procyanidin oligomers 失效
标题翻译：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。

2. 发明申请

US20030100601A1 Method for reducing postprandial oxidative stress using cocoa procyanidins 审中-公开
标题翻译：使用可可原花青素降低餐后氧化应激的方法
公开(公告)号：US20030100601A1
公开(公告)日：2003-05-29
申请号：US10305802
申请日：2002-11-27
申请人： Mars Incorporated
发明人： Harold H. Schmitz , Leo J. Romanczyk JR.
IPC分类号： A61K031/353 , A61K035/78 , A61K009/68
CPC分类号： A23G1/30 , A23G1/426 , A61K31/353 , Y10S426/804
摘要： A method for reducing postprandial oxidative stress and associated pathologies by the dietary intake of cocoa procyanidins, such as epicatechin is disclosed.
摘要翻译：公开了通过膳食摄入可可原花青素（如表儿茶素）减少餐后氧化应激和相关病理学的方法。

3. 发明申请

US20020004523A1 Partially purified cocoa extracts containing cocoa polyphenols 有权
标题翻译：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。

4. 发明申请

US20040228936A1 Compositions for, and methods of, anti-platelet therapy 有权
标题翻译：抗血小板治疗的组合物和方法
公开(公告)号：US20040228936A1
公开(公告)日：2004-11-18
申请号：US10780298
申请日：2004-02-17
申请人： Mars, Incorporated
发明人： Leo J. Romanczyk JR. , Harold H. Schmitz
IPC分类号： A61K031/7048 , A61K031/353 , A61K035/78
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： 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。

5. 发明申请

US20030176620A1 Synthetic methods for polyphenols 失效
公开(公告)号：US20030176620A1
公开(公告)日：2003-09-18
申请号：US10355606
申请日：2003-01-31
申请人： Mars Incorporated
发明人： Leo J. Romanczyk JR. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
IPC分类号： C08G002/00
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.

6. 发明申请

US20030114691A1 Synthetic methods for preparing procyanidin oligomers 失效
标题翻译：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。

7. 发明申请

US20030100775A1 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.

8. 发明申请

US20040175448A1 Pharmaceutical compositions 审中-公开
标题翻译：药物组合物
公开(公告)号：US20040175448A1
公开(公告)日：2004-09-09
申请号：US10790268
申请日：2004-03-01
申请人： Mars, Incorporated
发明人： Leo J. Romanczyk JR. , John F. Hammerstone JR. , Margaret M. Buck
IPC分类号： A61K035/78 , A61K031/353
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。

9. 发明申请

US20030176493A1 Cocoa extracts containing solvent-derived cocoa polyphenols from defatted cocoa beans 失效
标题翻译：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：US20030176493A1
公开(公告)日：2003-09-18
申请号：US10342772
申请日：2003-01-15
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 , A23L001/28
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 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。

10. 发明申请

US20020132018A1 Use of non-alkalized cocoa solids in a drink 有权
标题翻译：在饮料中使用非碱化的可可固体
公开(公告)号：US20020132018A1
公开(公告)日：2002-09-19
申请号：US10011068
申请日：2001-11-08
申请人： MARS, INCORPORATED
发明人： Kirk S. Kealey , Rodney M. Snyder , Leo J. Romanczyk JR. , John F. Hammerstone JR. , Margaret M. Buck , Giovanni G. Cipolla
IPC分类号： A61K035/78
CPC分类号： A23K50/48 , A21D2/364 , A21D13/80 , A23G1/0006 , A23G1/0009 , A23G1/002 , A23G1/0023 , A23G1/02 , A23G1/04 , A23G1/06 , A23G1/30 , A23G1/36 , A23G1/48 , A23G1/56 , A23G2200/00 , A23K50/42 , A23L7/122 , A23L7/126 , A23L7/17 , A23L7/178 , A23L7/196 , A23L9/10 , A23L19/09 , A23L33/10 , A23L33/105 , C11B1/04 , C11B1/06 , C11B1/10
摘要： The present invention is directed to a method of processing a fat-containing bean, e.g., cocoa beans, for producing solids comprising active polyphenols and/or fat-containing products, comprising extracting the fat to produce solids and fat-containing products. Additionally, the inventive method also provides cocoa compositions comprising at least one active polyphenol, wherein the concentration of the polyphenol(s) with respect to the nonfat solids is conserved with respect to the concentration of the active polyphenol(s) in the bean from which the compositions are derived.
摘要翻译：本发明涉及一种处理含脂肪豆，例如可可豆，用于生产包含活性多酚和/或含脂肪产品的固体的方法，其包括提取脂肪以产生固体和含脂肪的产品。另外，本发明的方法还提供了包含至少一种活性多酚的可可组合物，其中多酚相对于无脂固体的浓度相对于豆中的活性多酚的浓度是保守的，衍生出组合物。

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