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31. 发明公开

EP1221448A4 SWEETENER COMPOSITIONS WITH HIGH DEGREE OF SWEETNESS HAVING IMPROVED SWEETNESS, CORRIGENTS AND UTILIZATION THEREOF 审中-公开
标题翻译：甜味剂成分高甜度和改进的甜，矫味剂及其用途
公开(公告)号：EP1221448A4
公开(公告)日：2003-01-15
申请号：EP00961239
申请日：2000-09-26
申请人： AJINOMOTO KK
发明人： ISHII SHOICHI
IPC分类号： A23L2/60 , A23L27/30 , C07K5/072 , C07K5/075 , A23L1/22 , A23L1/236 , C07K5/06
CPC分类号： C07K5/06113 , A23L2/60 , A23L27/32
摘要： Sweetener compositions with a high degree of sweetness having sweetness characteristics approximating more closely to the sweetness characteristics of sucrose which are obtained by blending aspartyl dipeptide ester derivatives which are sweetener components having a high degree of sweetness (for example, N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L- alpha -aspartyl]-L-phenylalanine 1-methyl ester) with at least one compound selected from among other sweetener components having a high degree of sweetness (Aspartame, etc.), saccharides, sugar alcohols and oligosaccharides so as to strengthen the first taste of the derivatives and weaken the after taste, thereby improving the balance of the first taste and the after taste. The above aspartyl dipeptide ester derivatives are also usable as corrigents. By using these corrigents, an effect of largely eliminating or relieving bitterness can be achieved and maintained on compositions (drinks, foods, drugs, etc.), without undesirably affecting the physical properties (in particular, viscosity of liquid compositions) or worsening the qualities (for example, browning) during storage. Thus, drinks, foods, drugs, etc. having favorable taste characteristics with relieved bitterness can be provided.

32. 发明公开

EP1030831A4 PROCESS FOR THE PREPARATION OF AZACYCLOALKYLALKANOYL PSEUDOTETRAPEPTIDES 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON AZACYCLOALKYLALKYNOYL-PSEUDOTETRAPEPTIDEN
公开(公告)号：EP1030831A4
公开(公告)日：2003-01-02
申请号：EP98953345
申请日：1998-10-09
申请人： AVENTIS PHARM PROD INC
发明人： MENCEL JAMES J , STAMMLER ROBERT , DAUBIE CHRISTOPHE , LAVIGNE MICHEL , VANASSE BENOIT J , LIU ROBERT C , LEON PATRICK , D NETTO GEOFFREY A , SLEDESKI ADAM W
IPC分类号： A61K38/00 , A61P7/02 , A61P9/10 , C07C231/02 , C07D211/34 , C07D211/78 , C07D213/56 , C07K1/06 , C07K5/02 , C07K5/072 , C07C227/18 , C07C231/00 , C07C231/08 , C07C231/12 , C07K1/02 , C07K1/13
CPC分类号： C07D211/34 , C07K5/021 , C07K5/06113 , Y02P20/55
摘要： This invention is directed to a process for preparing a pseudotetrapeptide of formula (I) or salt or prodrug thereof wherein (II) is optionally nitrogen protected azaheterocyclyl; (a) is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is -H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR?1, or NR1R2¿, where R?1 and R2¿ are independently -H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or pseudopeptides.
摘要翻译：本发明涉及制备式（I）假四肽或其盐或其前药的方法，其中（II）任选地为氮保护的氮杂环基; （a）是单键或双键; q是1-5; B为烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷芳基或烷基芳烷基; Q2是H或羧酸保护基; J是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，取代的芳基，芳烷基，取代的芳烷基; L是OR1或NR1R2，其中R1和R2独立地是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷芳基或烷基芳烷基; 并且p是1或2，其包含两个二肽或假肽的偶联。

33. 发明公开

EP1261623A1 NEW RETINOL DERIVATIVES, THE METHOD OF PREPARATIONS AND THE USES THEREOF 有权
标题翻译：视黄醇衍生物，它们的表示和使用的方法
公开(公告)号：EP1261623A1
公开(公告)日：2002-12-04
申请号：EP02729592.2
申请日：2002-01-10
申请人： Chebigen Inc.
发明人： SIN, Hong-Sig , PARK, Si-Ho , RHO, Young-Soy , UM, Soo-Jong , KWON, Youn-Ja , PARK, Myoung-Soon , HAN, Hye-Sook , JUNG, Min-Sook , KIM CHO, So-Mi , KIM, Dong-Myong , OH, Deok-Kun , PARK, Jong-Sup
IPC分类号： C07K5/00
CPC分类号： C07K5/06113 , C07K5/0613
摘要： The present invention relates to novel retinol derivatives, the methods of preparation and the uses thereof. According to the present invention, retinol derivatives comprise carboester linkage between di-, tri-, polypeptide having functional group of COOH and retinol. Retinol derivatives in the present invention comprise carboester linkage between amino acid having functional group of di-COOH and retinol. Retinol derivatives comprise carboester linkage between retinol and the compounds having the function group of COOH and multiple double bonds on carbon chain. Retinol derivatives in the present invention comprise carboester linkage between retinol and the compounds having the functional group of di-COOH and one double bond. Retinol derivatives in the present invention comprise ether linkage between the compounds with OH functional group and retinol.

34. 发明公开

EP1236713A1 NOVEL INTERMEDIATE FOR SWEETENER WITH HIGH SWEETNESS AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：新中间体随着高糖果和方法及其甜味剂
公开(公告)号：EP1236713A1
公开(公告)日：2002-09-04
申请号：EP00974890.6
申请日：2000-11-09
申请人： Ajinomoto Co., Inc.
发明人： KAWAHARA,Shigeru Amino Science Lab.Ajinomoto Co.In , MORI,Kenichi Amino Science Lab.Ajinomoto Co., Inc. , NAGASHIMA,Kazutaka Amino Science Lab.AjinomotoCo. , TAKEMOTO,Tadashi Amino Science Lab.Ajinomoto Co.In
IPC分类号： C07C303/30 , C07C309/66 , C07C45/41 , C07C47/277 , C07C51/367 , C07C59/64 , C07K5/075
CPC分类号： C07C51/367 , C07C45/41 , C07C47/277 , C07C303/30 , C07K5/06113 , C07C59/64 , C07C309/66
摘要： From a butyric acid derivative which can be easily and efficiently produced by reacting a hydroxyl-protective derivative of 2-methoxy phenol, wherein the hydroxyl group of 2-methoxy phenol is protected in the form of a sulfonic acid ester (sulfonate), with a 3-methylcrotonic acid in the presence of an acid, a 3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyric acid can be obtained by converting the substituent group at the 3-position of the benzene ring in the butyric acid derivative to a hydroxyl group. From the compound, further by means of a reaction for converting a carboxyl group into a formyl group, a 3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl aldehyde can be easily produced, and the aldehyde derivative can be easily changed into a compound, which is excellent as a sweetener with a high potency of sweetness, by a reductive alkylation reaction with aspartame.
摘要翻译：从其中可以通过使2-甲氧基苯酚的羟基保护的衍生物，worin 2-甲氧基 - 苯酚的羟基的磺酸酯（磺酸酯）的形式被保护，具有可以容易和有效地生成的丁酸衍生物在酸的存在下3-甲基巴豆酸，3-（3-羟基-4-甲氧基 - 苯基）-3-甲基丁酸可以通过将取代基在丁酸衍生物的苯环的3位而得到成羟基。从化合物，此外，通过反应的装置，用于将羧基成甲酰基，3-（3-羟基-4-甲氧基 - 苯基）-3-甲基丁基醛可以容易地制造，以及醛衍生物可以容易地改变成的化合物，所有这些都作为优良甜度的高效力甜味剂，通过与阿斯巴甜还原烷基化反应。

35. 发明公开

EP1215215A1 Platelet aggregation inhibitors containing c-terminal aminergic side chain amino acid residues 失效
标题翻译：死亡细胞死亡C末端氨基末端Seitenketten焓
公开(公告)号：EP1215215A1
公开(公告)日：2002-06-19
申请号：EP02002913.8
申请日：1996-03-22
申请人： G.D. SEARLE & CO.
发明人： Abood, Norman A. , Bovy, Philippe R. , Flynn, Daniel L. , Rico, Joseph G. , Rogers, Thomas E.
IPC分类号： C07K14/75 , C07K5/06 , A61K38/05
CPC分类号： C07K5/021 , A61K38/00 , C07K5/0202 , C07K5/06113
摘要： This invention relates to compounds having the following formula:
or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions containing such compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
摘要翻译：本发明涉及具有下式的化合物：其可用于抑制血小板聚集的或其药学上可接受的盐，含有这些化合物的药物组合物，以及通过施用这些化合物和成分。

36. 发明公开

EP1048223A4 SWEETENER COMPOSITIONS CONTAINING ASPARTAME AND ASPARTAME DERIVATIVE 审中-公开
标题翻译： SUESSTOFFUSUSMENSETZUNGEN ENTHALTEND ASPARTAM SOWIE EINEN ASPARTAMABKOEMMLING
公开(公告)号：EP1048223A4
公开(公告)日：2001-09-12
申请号：EP98967081
申请日：1998-12-08
申请人： AJINOMOTO KK
发明人： KISHISHITA AKIHIRO , NAGASHIMA KAZUTAKA
IPC分类号： A23L27/30 , C07K5/072 , C07K5/075 , A23L1/236 , C07K5/06
CPC分类号： C07K5/06113 , A23L27/32 , C07K5/0613
摘要： Excellent sweetener compositions containing aspartame (APM) and APM derivative and being similar to sucrose in tasting properties, which can be easily, uniformly and efficiently produced at a high purity by the process for producing N-[N-(3,3-dimethylbutyl)-L- alpha -aspartyl]-L-phenylalanine methyl ester by the reductive alkylation of APM and 3,3-dimethylbutyraldehyde, which comprises using 3,3-dimethylbutyraldehyde in an amount at most equimolar to APM for producing N-[N-(3,3-dimethylbutyl)-L- alpha -aspartyl]-L-phenylalanine methyl ester from a portion of the APM existing in the reaction system, then separating the reducing agent from the liquid reaction mixture, and effecting crystallization followed by the separation of the crystals thus precipitated.
摘要翻译：优良的甜味剂组合物含有阿斯巴甜（APM）和APM衍生物并且在品尝性质上类似于蔗糖，通过生产N- [N-（3,3-二甲基丁基）氨基甲酸酯）的方法可以容易地， -L-α-天冬氨酰基] -L-苯丙氨酸甲酯通过APM和3,3-二甲基丁醛的还原烷基化，其包括使用最多与APM等摩尔量的3,3-二甲基丁醛用于生产N- [N-（ 3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸甲酯从反应体系中存在的一部分APM中分离出来，然后从液体反应混合物中分离出还原剂，并进行结晶，然后分离晶体因此沉淀。

37. 发明公开

EP1076064A4 NOVEL ASPARTAME DERIVATIVE CRYSTAL AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译： NEUARTIGER KRISTALL EINES ASPARTAMDERIVATS SOWIE VERFAHREN ZU DESSEN HERSTELLUNG
公开(公告)号：EP1076064A4
公开(公告)日：2001-09-05
申请号：EP99917152
申请日：1999-04-26
申请人： AJINOMOTO KK
发明人： KISHISHITA AKIHIRO , NAGASHIMA KAZUTAKA , ISHIDA HIROTOSHI , NAGAI TAKESHI
IPC分类号： A23L27/30 , C07K1/14 , C07K5/072 , C07K5/075 , A23L1/236 , C07K1/02 , C07K5/06
CPC分类号： C07K5/06113
摘要： A process for producing crystals of a methyl ester of N-[N-(3,3-dimethylbutyl)-L- alpha -aspartyl]-L-phenylalanine which comprises precipitating the ester from an aqueous solution thereof at a crystallization temperature of 25 DEG C or lower, further cooling the solution if desired, subsequently separating the precipitated crystals (B-form crystals) by solid-liquid separation, and then drying the crystals. The thus-dried crystals are novel crystals (D-form crystals) of the ester which have an excellent rate of dissolution. These crystals, when examined by X-ray powder diffractometry, have characteristic X-ray diffraction peaks at least at diffraction angles of 5.4 DEG , 8.4 DEG , 18.8 DEG , and 17.6 DEG (2 theta , CuK alpha line).
摘要翻译：一种生产N- [N-（3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸甲酯晶体的方法，该方法包括在25℃结晶温度下从其水溶液中沉淀酯如果需要，进一步冷却溶液，随后通过固液分离分离沉淀的晶体（B型晶体），然后干燥晶体。如此干燥的晶体是具有优异溶解速率的酯的新型晶体（D型晶体）。当用X射线粉末衍射法检测时，这些晶体至少在衍射角为5.4°，8.4°，18.8°和17.6°（2θ，CuKα线）时具有特征X射线衍射峰。

38. 发明授权

EP0879243B1 ACIDE N-(3,3-DIMETHYLBUTYL)-L-ASPARTYL-D-ALPHA-AMINOALCANOIQUE N-(S)-1-PHENYL-1-ALCANAMIDE UTILE COMME AGENT EDULCORANT 失效
标题翻译： N-（3,3-二甲基丁基）-L-阿糖胞苷-D-阿氨酸 - 氨基-1-辛烯-1-烷酰胺，ALS SSTSOFF VERWENDBAR
公开(公告)号：EP0879243B1
公开(公告)日：2001-05-30
申请号：EP97903422.0
申请日：1997-02-07
申请人： NOFRE, Claude , TINTI, Jean-Marie
发明人： NOFRE, Claude , TINTI, Jean-Marie
IPC分类号： C07K5/06 , A23L1/236
CPC分类号： C07K5/06113 , A23L27/30
摘要： Compounds of formula (I), wherein Y is C2H5, CH(CH3)2 or (R) CH(OH)CH3, and R" is (S) CH(C2H5)C6H5, (S) CH(CH3)C6H5, or (R) CH(CH2OCH3)C6H5, are disclosed. The compounds are useful as sweeteners.

39. 发明公开

EP1088829A1 NOVEL ASPARTYL DIPEPTIDE ESTER DERIVATIVES AND SWEETENERS 审中-公开
标题翻译：新的天冬氨酰二肽衍生物和甜味剂
公开(公告)号：EP1088829A1
公开(公告)日：2001-04-04
申请号：EP99923954.4
申请日：1999-06-07
申请人： Ajinomoto Co., Inc.
发明人： AMINO, Yusuke, c/o Ajinomoto Co., Inc. , YUZAWA, Kazuko, c/o Ajinomoto Co.,Inc , TAKEMOTO, Tadashi, c/o Ajinomoto Co., Inc. , NAKAMURA, Ryoichiro, c/o Ajinomoto Co., Inc.
IPC分类号： C07K5/075 , A23L1/236 , C07K5/06
CPC分类号： C07K5/06113 , A23L5/44 , A23L27/32
摘要： There are provided novel aspartyl dipeptide ester derivatives (including salts thereof) such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-α-aspartyl]-L-(α-methyl)phenylalanine 1-methyl ester which are usable as sweeteners, and sweeteners, foods and the like containing the same.
These derivatives are usable as low-calory sweeteners especially excellent in the degree of sweetness in comparison with the conventional products.

40. 发明公开

EP1070726A1 ASPARTYL DIPEPTIDE ESTER DERIVATIVES AND SWEETENERS 有权
标题翻译： ASPARTYLDIPEPTIDESTER-DERIVATE UNDSÜSSUNGSMITTEL
公开(公告)号：EP1070726A1
公开(公告)日：2001-01-24
申请号：EP99932431.2
申请日：1999-03-11
申请人： Ajinomoto Co., Inc.
发明人： Amino, Yusuke Amino , Yuzawa, Kazuko , Takemoto, Tadashi , Nakamura, Ryoichiro
IPC分类号： C07K5/075 , A23L1/236
CPC分类号： C07K5/06113 , A23L27/32
摘要： Novel aspartyl dipeptide ester derivatives (including salts thereof) having an excellent sweetening effect and usable as sweeteners such as N-[N-[3-(3-methyl-4-hydroxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester and N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester, and excellent sweeteners,etc. containing these novel derivatives are provided.
A low-calory sweetener having especially an excellent sweetening potency can be provided in comparison with conventional ones.
摘要翻译：具有优异甜味作用的新型天冬氨酰二肽酯衍生物（包括其盐），可用作甜味剂如N- N-（3-甲基-4-羟基苯基）丙基-L-天冬氨酰基-L-苯丙氨酸1-甲基酯和N- N- 3-（3-羟基-4-甲氧基苯基）丙基-L-α-天门冬酰基-L-苯丙氨酸1-甲酯，以及优异的甜味剂等。含有这些新型衍生物。与传统甜味剂相比，可以提供特别优异的甜味效果的低热量甜味剂。

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