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21. 发明授权

US06630191B1 Aspartyl dipeptide ester derivatives and sweeteners 有权
标题翻译：天冬氨酰二肽酯衍生物和甜味剂
公开(公告)号：US06630191B1
公开(公告)日：2003-10-07
申请号：US09736149
申请日：2000-12-15
申请人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto , Ryoichiro Nakamura
发明人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto , Ryoichiro Nakamura
IPC分类号： A23L1236
CPC分类号： C07K5/06113 , A23L5/44 , A23L27/32
摘要： The present invention relates to novel, aspartyl dipeptide ester derivatives and salts thereof, such as N-[N-(3-(3-hydroxy-4-methoxyphenyl)propyl]-L-&agr;-aspartyl]-L-(&agr;-methyl)phenylalanine 1-methyl ester which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester derivatives and method of producing the novel aspartyl dipeptide ester derivatives.
摘要翻译：本发明涉及新型天冬氨酰二肽酯衍生物及其盐，例如N- [N-（3-（3-羟基-4-甲氧基苯基）丙基] -L-α-天冬氨酰基] -L-（α-甲基）苯丙氨酸1-甲酯，其与常规产品，含有新型天冬氨酰二肽酯衍生物的组合物和产品以及生产新型天冬氨酰二肽酯衍生物的方法相比，具有高度的甜度。

22. 发明授权

US06939987B2 Method for producing Aspartame derivative, method for purifying the same, crystals thereof and uses of the same 失效
标题翻译：天冬甜精衍生物的制造方法，其纯化方法，其结晶及其用途
公开(公告)号：US06939987B2
公开(公告)日：2005-09-06
申请号：US10656228
申请日：2003-09-08
申请人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto
发明人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto
IPC分类号： A23L27/30 , C07K5/072 , C07K5/075 , C07C229/00
CPC分类号： C07K5/06113 , A23L27/32
摘要： N-[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester is prepared by a process comprising: subjecting Aspartame and 3-(3-methoxy-4-hydroxyphenyl)propionaldehyde or derivatives thereof to reductive alkylation in a solvent to produce N-[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester; and crystallizing said compound.
摘要翻译： N- [N- [3-（3-甲氧基-4-羟基苯基）丙基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯的制备方法包括：将阿斯巴甜和3-（3-甲氧基 -4-羟基苯基）丙醛或其衍生物在溶剂中还原烷基化以产生N- [N- [3-（3-甲氧基-4-羟基苯基）丙基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲基酯; 并结晶所述化合物。

23. 发明授权

US06649784B2 Aspartyl dipeptide ester derivatives and sweeteners 失效
公开(公告)号：US06649784B2
公开(公告)日：2003-11-18
申请号：US10109719
申请日：2002-04-01
申请人： Yusuke Amino , Tadashi Takemoto , Kazuko Yuzawa , Ryoichiro Nakamura
发明人： Yusuke Amino , Tadashi Takemoto , Kazuko Yuzawa , Ryoichiro Nakamura
IPC分类号： C07C22900
CPC分类号： C07K5/06113 , A23L27/32
摘要： Aspartyl dipeptide ester derivatives, such as a N-[N-[3-(3,4-dihydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, or salts thereof, having a high degree of sweetness compared to conventional sweeteners. These derivatives are excellent in sweetening potency and may be used as sweetener components in products such as foods and drinks. They may also be used as low calorie sweeteners and in methods of sweetening products. Foods and drinks comprising these derivatives as well as methods for their production.

24. 发明授权

US07329427B2 Process for producing γ-hydroxyamino acid derivatives and monatins 失效
标题翻译：用于生产γ-羟基氨基酸衍生物和monatins的方法
公开(公告)号：US07329427B2
公开(公告)日：2008-02-12
申请号：US10397407
申请日：2003-03-27
申请人： Yusuke Amino , Shigeru Kawahara
发明人： Yusuke Amino , Shigeru Kawahara
IPC分类号： A23L1/236
CPC分类号： C07D209/20 , A23L27/31
摘要： Dihydroisoxazole derivatives are conveniently converted to γ-hydroxyamino acid derivatives which are important as various synthetic intermediates by a catalytic hydrogenation reaction. High-purity monatins which may be used as sweeteners or ingredients thereof can be obtained by subjecting a 5-indolylmethyl-4,5-dihydroisoxazole-3,5-dicarboxylic acid to catalytic hydrogenation.
摘要翻译：二氢异恶唑衍生物方便地转化为γ-羟基氨基酸衍生物，它们通过催化氢化反应作为各种合成中间体是重要的。可以用作甜味剂或其成分的高纯度monatins可以通过使5-吲哚基甲基-4,5-二氢异恶唑-3,5-二羧酸进行催化氢化而获得。

25. 发明授权

US06548096B1 Aspartyl dipeptide ester derivatives and sweeteners 有权
标题翻译：天冬氨酰二肽酯衍生物和甜味剂
公开(公告)号：US06548096B1
公开(公告)日：2003-04-15
申请号：US09684940
申请日：2000-10-10
申请人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto , Ryoichiro Nakamura
发明人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto , Ryoichiro Nakamura
IPC分类号： A23L1236
CPC分类号： C07K5/06113 , A23L27/32
摘要： Low-calory sweeteners comprising novel aspartyl dipeptide ester derivatives and their salts have a sweetening potency of up to 35000 times that of sugar and include compounds such as N-[N-[3-(3-methyl-4-hydroxyphenyl)propyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester and N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.
摘要翻译：包含新型天冬氨酰二肽酯衍生物及其盐的低热量甜味剂具有高达糖的35000倍的甜味效力，并且包括化合物如N- [N- [3-（3-甲基-4-羟基苯基）丙基] - L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯和N- [N- [3-（3-羟基-4-甲氧基苯基）丙基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯。

26. 发明授权

US06335461B1 Process for purification of aspartame derivative 失效
标题翻译：阿斯巴甜衍生物纯化方法
公开(公告)号：US06335461B1
公开(公告)日：2002-01-01
申请号：US09515097
申请日：2000-02-29
申请人： Yusuke Amino , Tadashi Takemoto
发明人： Yusuke Amino , Tadashi Takemoto
IPC分类号： C07C22900
CPC分类号： C07K5/06113 , A23L27/32
摘要： In the separation and purification of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine methyl ester produced in the reductive alkylation of aspartame (APM) with 3,3-dimethylbutylaldehyde, the APM used in the starting material for the alkylation, which is difficult to be separated by recrystallization only from the crude crystals of the reaction product, can be separated and removed by extraction or solution thereof with the specified organic solvent from the concentrated reaction solution of the reductive alkylation or from the crude crystals of the product therefrom, and further N,N-di(3,3-dimethylbutyl)-APM as the by-product can be separated and removed by means for separation and purification, such as crystallization, chromatography, extraction, treatment with the activated charcoal, etc. As a result, N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine methyl ester which is a sweetener having a high degree of sweetness can be purified efficiently, and also the APM derivative in a high purity is possibly produced industrially.
摘要翻译：在用3,3-二甲基丁醛在阿斯巴甜（APM）的还原烷基化中产生的N- [N-（3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸甲酯的分离和纯化中，APM 用于烷基化的原料中，仅通过反应产物的粗结晶难以通过重结晶分离，可以通过从浓缩的还原反应溶液中的特定有机溶剂提取或溶液来分离和除去烷基化或从其产物的粗结晶中分离出来，作为副产物的另外的N，N-二（3,3-二甲基丁基）-APM可以通过分离和纯化如结晶，色谱法，提取，活性炭处理等。结果，作为甜度高的甜味剂的N- [N-（3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸甲酯可以有效净化，还有APM d 高纯度的腐烂可能在工业上生产。

27. 发明授权

US6010733A Aspartylamide derivatives and sweeteners 失效
标题翻译：天冬氨酰胺衍生物和甜味剂
公开(公告)号：US6010733A
公开(公告)日：2000-01-04
申请号：US782949
申请日：1997-01-13
申请人： Tadashi Takemoto , Yusuke Amino , Ryoichiro Nakamura
发明人： Tadashi Takemoto , Yusuke Amino , Ryoichiro Nakamura
IPC分类号： A23L27/30 , C07C237/08 , A23L1/236
CPC分类号： C07C237/08 , C07C2101/14
摘要： Novel aspartylamide derivatives such as N-(.alpha.-L-aspartyl-(1R,2S,4S)-1-methyl-2-hydroxy-4-phenylhexylamide, N-.alpha.-7(N'-3,3-dimethylbutylaspartyl)-(1R,2S,4S)-1-methyl-2-hydroxy-4-phenylhexylamide) and the like, and a sweetener containing the above-mentioned derivatives or salts thereof as an active ingredient, is low-calory and which exhibits a high level of stability, an excellent safety and an excellent sweetness.
摘要翻译：新型天冬氨酰胺衍生物如N-（α-L-天冬氨酰 - （1R，2S，4S）-1-甲基-2-羟基-4-苯基己酰胺，N-7（N'-3,3-二甲基丁基天竺葵酰）（1R，2S，4S）-1-甲基-2-羟基-4-苯基己基酰胺）等，并且含有上述衍生物或其盐作为活性成分的甜味剂是低热量的并且显示出高的水平稳定，安全性好，甜蜜度高。

28. 发明授权

US06899912B2 Method for producing aspartame derivative, method for purifying the same, crystals thereof and uses of the same 失效
标题翻译：阿斯巴甜衍生物的制造方法，其纯化方法，其结晶及其用途
公开(公告)号：US06899912B2
公开(公告)日：2005-05-31
申请号：US10091500
申请日：2002-03-07
申请人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto
发明人： Yusuke Amino , Kazuko Yuzawa , Tadashi Takemoto
IPC分类号： A23L27/30 , C07K5/072 , C07K5/075 , A23L1/236 , C07C229/00
CPC分类号： C07K5/06113 , A23L27/32
摘要： N-[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester is prepared by a process comprising: subjecting Aspartame and 3-(3-methoxy-4-hydroxyphenyl)propionaldehyde or derivatives thereof to reductive alkylation in a solvent to produce N-[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester; and crystallizing said compound.
摘要翻译： N- [N- [3-（3-甲氧基-4-羟基苯基）丙基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯的制备方法包括：将阿斯巴甜和3-（3-甲氧基 -4-羟基苯基）丙醛或其衍生物在溶剂中还原烷基化以产生N- [N- [3-（3-甲氧基-4-羟基苯基）丙基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲基酯; 并结晶所述化合物。

29. 发明授权

US5958496A Aspartyl dipeptide amide derivatives and sweeteners 失效
标题翻译：天冬氨酰二肽酰胺衍生物和甜味剂
公开(公告)号：US5958496A
公开(公告)日：1999-09-28
申请号：US890993
申请日：1997-07-10
申请人： Yusuke Amino , Ryoichiro Nakamura , Tadashi Takemoto
发明人： Yusuke Amino , Ryoichiro Nakamura , Tadashi Takemoto
IPC分类号： A23L27/30 , C07K5/072 , C07K5/075 , A23L1/236 , C07C229/00
CPC分类号： C07K5/06113
摘要： Novel aspartyldipeptidoamides and salts thereof. The apartyldipeptides are useful as a low-calorie sweetener for food and beverage products and have excellent taste and chemical stability.
摘要翻译：新型天冬氨酰二肽酰胺及其盐。这种二十四碳四烯酸可用作食品和饮料产品的低热量甜味剂，具有极好的味道和化学稳定性。

30. 发明授权

US5723165A Aspartyldipeptide derivatives and sweetener compositions containing the same 失效
标题翻译：天冬氨酰二肽衍生物和含有它们的甜味剂组合物
公开(公告)号：US5723165A
公开(公告)日：1998-03-03
申请号：US500405
申请日：1995-07-10
申请人： Tadashi Takemoto , Yusuke Amino , Ryoichiro Nakamura
发明人： Tadashi Takemoto , Yusuke Amino , Ryoichiro Nakamura
IPC分类号： A23L27/30 , C07K5/072 , C07K5/075
CPC分类号： C07K5/06113 , Y10S530/801
摘要： Aspartyldipeptide compounds of the formula (I) L-Asp-X-NH-C*R.sub.1 R.sub.2 (I) where R.sub.1 is alkyl or alkoxymethyl, R.sub.2 is phenyl, benzyl, cyclohexyl or cyclohexylmethyl, C* has an (S) configuration when R.sub.1 is alkyl and an (R) configuration when R.sub.1 is alkoxymethyl and X is a residue of a D-.alpha.-amino acid, a DL-.alpha.-amino acid or a residue of a cyclic or acyclic .alpha.,.alpha.-diallylamino acid and the bond between L-Asp and X is an .alpha.-bond; and their use as active ingredients in sweetener compositions.
摘要翻译：式（I）L-Asp-X-NH-C * R1R2（I）的天冬氨酰二肽化合物，其中R 1是烷基或烷氧基甲基，R 2是苯基，苄基，环己基或环己基甲基，C *具有（S）烷基和（R）构型，当R 1为烷氧基甲基且X为D-α-氨基酸，DL-α-氨基酸或环状或非环状α，α-二烯丙基氨基酸的残基时， L-Asp和X是α键; 以及它们作为甜味剂组合物中的活性成分的用途。

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