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公开(公告)号：US06630191B1
公开(公告)日：2003-10-07
申请号：US09736149
申请日：2000-12-15
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。
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公开(公告)号：US07238830B2
公开(公告)日：2007-07-03
申请号：US09809197
申请日：2001-03-16
IPC分类号： C07C229/00 , A23L1/236
CPC分类号： C07K5/0613 , A23L27/32
摘要： The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.
摘要翻译： 本发明提供N-烷基天冬氨酰二肽化合物及其盐，例如N- [N- [3-（3-羟基-4-甲氧基苯基）-3-甲基丁基] -L-α-天冬氨酰基] -L-苯丙氨酸1- 甲酯，其与常规产品，含有新型天冬氨酰二肽酯化合物的组合物和产品以及生产新型天冬氨酰二肽酯化合物的方法相比，具有高度的甜度。
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公开(公告)号：US5968581A
公开(公告)日：1999-10-19
申请号：US37870
申请日：1998-03-10
CPC分类号： C07K5/06113 , A23L27/32 , C07K5/06104
摘要： Novel dipeptide derivatives, such as N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-phenylalanine methyl ester and N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-tyrosine methyl ester, and sweetening agents comprising, as the active ingredient, anyone of the derivatives and their salts, being low-calorie sweetening agents which are excellent in stability, safety and degree of sweetness, are provided. The products to have been sweetened, comprising such above sweetening agents are also provided.
摘要翻译： 新型二肽衍生物如N-3,3-二甲基丁基-α-L-天冬氨酰-α-甲基-L-苯丙氨酸甲酯和N-3,3-二甲基丁基-α-L-天冬氨酰-α-甲基-L- 酪氨酸甲酯和甜味剂，其包含作为活性成分的任何衍生物及其盐，它们是稳定性，安全性和甜度优异的低热量甜味剂。 还提供了包含这些上述甜味剂的已经变甜的产品。
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公开(公告)号：US5795612A
公开(公告)日：1998-08-18
申请号：US579976
申请日：1995-12-28
CPC分类号： C07K5/06113
摘要： Novel aspartyldipeptideamide derivatives of formula (I): L--Asp--X--NH--C*HR.sub.1 R.sub.2 and salts thereof, wherein X is a D-.alpha.-amino acid residue or a DL-.alpha.-amino acid residue selected from the group consisting of D-alanine, D-.alpha.-aminobutyric acid, D-norvaline, D-valine, D-norleucine, D-leucine, D-isoleucine, D-alloisoleucine, D-t-leucine, D-serine, D-O-methylserine, D-threonine, D-O-methylthreonine, D-allothreonine, D-O-methylallothreonine, D-phenyl glycine and D- or DL furyl glycine, or X is a cyclic or non-cyclic .alpha., .alpha.-dialkyl amino acid residue having 3 to 6 carbon atoms; R.sub.1 is a linear or branched alkyl group having 1 to 6 carbon atoms or an alkoxymethyl group having 2 to 7 carbon atoms in the alkoxy portion; R.sub.2 is a phenyl group having a substituent in its 2, 3- or 4-position selected from the group consisting of F, Cl, Br, I, a hydroxy group, a linear or branched alkoxy group having 1 to 6 carbon atoms, a cyano group, a nitro group, an acetyl group, an amino group and an acetylamino group, or R.sub.2 is a phenyl group having a methylenedioxy group, a trimethylene group or a tetramethylene group in its 2, 3- or 3, 4- position or R.sub.2 is a 2, 3- or 4-pyridyl group, a 2- or 3-furyl group or a 2- or 3-thienyl group; the configuration of C* in formula (I) is (S) or (RS) when R.sub.1 is a linear or branched alkyl group; (R), (S), or (RS) when R.sub.1 is an alkoxymethyl group; and in formula (I), L-Asp and X are .alpha.-bonded.
摘要翻译： 式（I）的新型天冬氨酰二肽酰胺衍生物：L-Asp-X-NH-C * HR1R2及其盐，其中X为D-氨基酸残基或DL-α-氨基酸残基，其选自 D-丙氨酸，D-α-氨基丁酸，D-正缬氨酸，D-缬氨酸，D-正亮氨酸，D-亮氨酸，D-异亮氨酸，D-异亮氨酸，D-L-亮氨酸，D-丝氨酸，DO-甲基丝氨酸，D-苏氨酸 ，D-甲基苏氨酸，D-异亮氨酸，DO-甲基缩氨基丁酸，D-苯基甘氨酸和D-或DL呋喃基甘氨酸，或X是具有3至6个碳原子的环状或非环状α，α-二烷基氨基酸残基; R1是烷氧基部分中具有1至6个碳原子的直链或支链烷基或具有2至7个碳原子的烷氧基甲基; R2是在其选自F，Cl，Br，I，羟基，具有1至6个碳原子的直链或支链烷氧基的2,3或4位中具有取代基的苯基， 氰基，硝基，乙酰基，氨基和乙酰氨基，或者R2是在其3-或4-或3-位上具有亚甲二氧基，三亚甲基或四亚甲基的苯基， R2是2,3-或4-吡啶基，2-或3-呋喃基或2-或3-噻吩基; 当R 1为直链或支链烷基时，式（I）中C *的构型为（S）或（RS） （R），（S）或（RS）; 在式（I）中，L-Asp和X是α键。
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公开(公告)号：US06649784B2
公开(公告)日：2003-11-18
申请号：US10109719
申请日：2002-04-01
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.
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公开(公告)号：US5958496A
公开(公告)日：1999-09-28
申请号：US890993
申请日：1997-07-10
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。
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7.发明授权Aspartyldipeptide derivatives and sweetener compositions containing the same 失效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
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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公开(公告)号：US06548096B1
公开(公告)日：2003-04-15
申请号：US09684940
申请日：2000-10-10
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。
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公开(公告)号：US6010733A
公开(公告)日：2000-01-04
申请号：US782949
申请日：1997-01-13
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。
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10.发明授权2,5-dioxopiperazine compounds and method for preparing .alpha.-aspartyl-L-phenylalanine methyl ester derivatives 失效2,5-二氧代哌嗪化合物和制备α-天冬氨酰-L-苯丙氨酸甲酯衍生物的方法
公开(公告)号：US5294714A
公开(公告)日：1994-03-15
申请号：US965857
申请日：1992-10-23
IPC分类号： C07D241/08 , C07K1/02 , C07K1/113 , C07K5/075 , C07D241/04 , C07C229/00
CPC分类号： C07D241/08 , C07K5/0613
摘要： A method of preparing .alpha.-APM derivatives without using an expensive L-phenylalanine is provided, wherein 2,5-dioxopiperazine-3-acetamide is reacted with acetic anhydride to give N,N'-diacetyl-6-cyanomethyl-2,5-dioxopiperazine, which is then reacted with benzaldehyde in the presence of a strong base to give 1-acetyl-3-benzylidene-6-cyanomethyl-2,5-dioxopiperazine. This is treated with hydrazine to give 3-benzylidene-6-cyanomethyl-2,5-dioxopiperazine, which is then reduced to prepare 3-benzyl-6-cyanomethyl-2,5-dioxopiperazine, which is converted by reaction with methanol in the presence of a strong acid to an .alpha.-APM derivative for use as a sweetener.
摘要翻译： 提供了不使用昂贵的L-苯丙氨酸制备（α）-APM衍生物的方法，其中2,5-二氧代哌嗪-3-乙酰胺与乙酸酐反应，得到N，N'-二乙酰基-6-氰基甲基-2， 然后将其与苯甲醛在强碱存在下反应，得到1-乙酰基-3-亚苄基-6-氰基甲基-2,5-二氧代哌嗪。 用肼处理，得到3-亚苄基-6-氰基甲基-2,5-二氧代哌嗪，然后将其还原，得到3-苄基-6-氰基甲基-2,5-二氧代哌嗪，其通过与甲醇反应而转化 对（α）-APM衍生物存在强酸以用作甜味剂。
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