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1. 发明授权

US4165311A Addition compound of dipeptide derivative and amino acid derivative 失效
标题翻译：二肽衍生物和氨基酸衍生物的加成化合物
公开(公告)号：US4165311A
公开(公告)日：1979-08-21
申请号：US870108
申请日：1978-01-17
申请人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
发明人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
IPC分类号： C07K5/072 , C07K5/075 , C07C103/52 , C12B1/00
CPC分类号： C07K5/0613
摘要： Addition compounds having the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents, or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2 together with methods for preparing (I) and for decomposing (I) into the constituent dipeptide esters and amino acid esters.
摘要翻译：具有式（I）的加成化合物，其中R 1表示脂族氧基羰基，可具有核取代基的苄氧基羰基，或苯甲酰基，芳族磺酰基或芳族亚磺酰基; R 2表示甲基，异丙基，异丁基，异戊基或苄基; R3表示低级烷氧基，苄氧基或二苯甲氧基，n表示1或2，以及用于制备（I）和用于将（I）分解成组分二肽酯和氨基酸酯的方法。

2. 发明授权

US4436925A Addition compound of dipeptide derivative and amino acid derivative 失效
标题翻译：二肽衍生物和氨基酸衍生物的加成化合物
公开(公告)号：US4436925A
公开(公告)日：1984-03-13
申请号：US270025
申请日：1982-06-03
申请人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
发明人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
IPC分类号： C07K5/072 , C07K5/075 , C07C101/00
CPC分类号： C07K5/0613
摘要： Addition compounds have the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2.The addition compounds are produced by reacting an N-substituted monoaminodicarboxylic acid having the formula ##STR2## with an amino carboxlic acid ester having the formula in an aqueous medium in the presence of a protease and reacting the resulting dipeptide ester with the amino carboxylic acid ester and separating the addition compound.The addition compounds can be decomposed into the constituent dipeptide esters and amino acid esters by the action of an acid.
摘要翻译：加成化合物具有式（I）其中R 1表示脂族氧羰基，可具有核取代基的苄氧基羰基或苯甲酰基，芳族磺酰基或芳族亚磺酰基; R 2表示甲基，异丙基，异丁基，异戊基或苄基; R3表示低级烷氧基，苄氧基或二苯甲氧基，n表示1或2.加成化合物通过使具有式（IV）的式（I）所示的N-取代的单氨基二羧酸与式（V）在水性介质中，在蛋白酶存在下，使得到的二肽酯与氨基羧酸酯反应并分离加成化合物。加成化合物可以通过酸的作用分解成组分二肽酯和氨基酸酯。

3. 发明授权

US4256836A Addition compound of dipeptide derivative and amino acid derivative 失效
标题翻译：二肽衍生物和氨基酸衍生物的加成化合物
公开(公告)号：US4256836A
公开(公告)日：1981-03-17
申请号：US20058
申请日：1979-03-13
申请人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
发明人： Yoshikazu Isowa , Muneki Ohmori , Kaoru Mori , Tetsuya Ichikawa , Yuji Nonaka , Keiichi Kihara , Kiyotaka Oyama , Heijiro Satoh , Shigeaki Nishimura
IPC分类号： C07K5/072 , C07K5/075 , C07C103/52 , C12P21/02
CPC分类号： C07K5/0613
摘要： Addition compounds having the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents, or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2 are produced by reacting an N-substituted monoaminodicarboxylic acid having the formula ##STR2## with an amino carboxylic acid ester having the formula ##STR3## in the presence of a protease.
摘要翻译：具有式（I）的加成化合物，其中R 1表示脂族氧基羰基，可具有核取代基的苄氧基羰基，或苯甲酰基，芳族磺酰基或芳族亚磺酰基; R 2表示甲基，异丙基，异丁基，异戊基或苄基; R3表示低级烷氧基，苄氧基或二苯甲氧基，n表示1或2是通过使具有式（IV）的N-取代的单氨基二羧酸与具有式（VI）的氨基羧酸酯反应制备的，在蛋白酶的存在下。

4. 发明授权

US4284721A Method for manufacturing dipeptides 失效
标题翻译：二肽制造方法
公开(公告)号：US4284721A
公开(公告)日：1981-08-18
申请号：US136347
申请日：1980-04-01
申请人： Kiyotaka Oyama , Shigeaki Nishimura , Yuji Nonaka , Tsutomu Hashimoto , Keiichi Kihara
发明人： Kiyotaka Oyama , Shigeaki Nishimura , Yuji Nonaka , Tsutomu Hashimoto , Keiichi Kihara
IPC分类号： C12P21/02 , C07K5/072 , C07K5/075 , C07C103/52
CPC分类号： C07K5/0613
摘要： An improvement in a method for manufacturing dipeptides from an N-substituted aspartic acid and a phenylalanine lower alkyl ester. The two starting materials are allowed to react with each other in the presence of an immobilized metallo-proteinase in an organic solvent immiscible with water. The enzyme can be recovered for reuse thereof. The loss of materials due to the hydrolysis of the phenylalanine lower alkyl ester is reduced, so that use of the phenylalanine lower alkyl ester in a nearly stoichiometric quantity suffices for the reaction to ensure an improved yield and reduction in cost of industrial production.
摘要翻译：从N-取代天冬氨酸和苯丙氨酸低级烷基酯制备二肽的方法的改进。允许两种起始物质在固定化的金属蛋白酶存在下在与水不混溶的有机溶剂中相互反应。该酶可以回收再利用。由于苯丙氨酸低级烷基酯的水解导致的材料损失减少，因此使用近乎化学计量的苯丙氨酸低级烷基酯足以使反应保证提高的产率和降低工业生产的成本。

5. 发明授权

US4212946A Process for recovering protease 失效
标题翻译：回收蛋白酶的方法
公开(公告)号：US4212946A
公开(公告)日：1980-07-15
申请号：US907203
申请日：1978-05-18
申请人： Yuji Nonaka , Kiyotaka Oyama , Heijiro Satoh
发明人： Yuji Nonaka , Kiyotaka Oyama , Heijiro Satoh
IPC分类号： C12N9/00 , C07K5/06 , C07K5/075 , C12N9/50 , C12P21/02 , C12N9/48 , C07G7/02
CPC分类号： C12N9/50 , C12P21/02 , Y10S435/816
摘要： Protease is recovered by reacting a first amino acid whose amino group is protected with a protective group with a second amino acid whose carboxyl group is protected with a protective group, in an aqueous medium in the presence of a protease to result a peptide synthesis to deposit the addition compound of a dipeptide and said second C-terminal protected amino acid; dissolving said addition compound by adding an organic solvent to a precipitate separated from the reaction mixture and isolating the protease from an organic solvent suspension or dissolving said addition compound by adding a water immiscible organic solvent and separating the organic solvent phase by a liquid-liquid separation.The addition compound can be dissolved in an organic solvent after separating the precipitate from the reaction mixture.The addition compound can be also dissolved by adding a water-immiscible organic solvent to the reaction mixture and the organic solvent phase can be separated from the aqueous phase.
摘要翻译：通过使氨基被保护基团的第一个氨基酸与其羧基被保护基团保护的第二个氨基酸在水性介质中在蛋白酶存在下反应，从而使肽合成沉积，从而回收蛋白酶二肽和所述第二C末端保护的氨基酸的加成化合物; 通过向从反应混合物分离的沉淀物中加入有机溶剂来溶解所述加成化合物，并从有机溶剂悬浮液中分离蛋白酶或通过加入与水不混溶的有机溶剂溶解所述加成化合物并通过液 - 液分离分离有机溶剂相。在从反应混合物中分离出沉淀物后，加成化合物可以溶解在有机溶剂中。加成化合物也可以通过向反应混合物中加入与水不混溶的有机溶剂而溶解，并且有机溶剂相可以与水相分离。

6. 发明授权

US4212945A Process for recovering protease 失效
标题翻译：回收蛋白酶的方法
公开(公告)号：US4212945A
公开(公告)日：1980-07-15
申请号：US907006
申请日：1978-05-18
申请人： Yuji Nonaka , Kiyotaka Oyama , Heijiro Satoh
发明人： Yuji Nonaka , Kiyotaka Oyama , Heijiro Satoh
IPC分类号： C12N9/00 , C07K5/06 , C07K5/075 , C12N9/50 , C12P21/02 , C12N9/48 , C07G7/02
CPC分类号： C12N9/50 , C12P21/02 , Y10S435/816
摘要： Protease is recovered by reacting a first amino acid whose amino group is protected with a protective group with a second amino acid whose carboxyl group is protected with a protective group, in an aqueous medium in the presence of a protease to result a peptide synthesis to deposit the addition compound of a dipeptide and said second C-terminal protected amino acid; dissolving said addition compound into the aqueous medium by adding a polar organic solvent which is miscible with water and separating an insoluble material from the resulting suspension by a solid-liquid separation to isolate the protease.
摘要翻译：通过使氨基被保护基团的第一个氨基酸与其羧基被保护基团保护的第二个氨基酸在水性介质中在蛋白酶存在下反应，从而使肽合成沉积，从而回收蛋白酶二肽和所述第二C末端保护的氨基酸的加成化合物; 通过加入与水混溶的极性有机溶剂将所述加成化合物溶解在水性介质中，并通过固液分离从所得悬浮液中分离出不溶物，分离蛋白酶。

7. 发明授权

US4564471A Method for reductive elimination of protecting groups 失效
标题翻译：还原消除保护基团的方法
公开(公告)号：US4564471A
公开(公告)日：1986-01-14
申请号：US188107
申请日：1980-09-17
申请人： Katsumi Sugiyama , Hideo Takeda , Hiroko Sato , Yuji Nonaka , Kiyotaka Oyama , Masashige Kubo
发明人： Katsumi Sugiyama , Hideo Takeda , Hiroko Sato , Yuji Nonaka , Kiyotaka Oyama , Masashige Kubo
IPC分类号： C07B31/00 , C07B51/00 , C07C67/00 , C07C227/00 , C07C227/16 , C07C227/18 , C07C227/20 , C07C231/00 , C07K1/06 , C07K1/12 , C07K5/075 , C07C101/02
CPC分类号： C07K1/12 , C07K5/0613 , Y02P20/55
摘要： The invention provides a novel and efficient method for the elimination of protecting groups, e.g. benzyloxycarbonyl group, from a protected amino acid, peptide or derivative thereof having at least one functional group protected by a protecting group, e.g. a lower alkyl ester of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine by catalytic hydrogen reduction to produce free amino acid, peptide or derivative thereof. In contrast to the conventional procedures in which the reaction is carried out in a solvent dissolving both the starting compound and the product compound or a solvent dissolving the starting compound but not dissolving the product compound, the inventive method utilizes a binary two-phase reaction medium composed of water and an organic solvent not freely miscible with water such as toluene. The reaction takes place in the organic phase containing the starting compound dissolved and the catalyst dispersed therein whereas the reaction product which is water-soluble is smoothly and successively transferred into the aqueous phase so that advantages are obtained in the unexpectedly high yield of the product as well as in the easiness of handling the reaction mixture after completion of the reaction.
摘要翻译：本发明提供了一种用于消除保护基团的新型和有效的方法，例如，苄氧羰基，被保护的氨基酸，具有至少一个被保护基保护的官能团的肽或衍生物。 N-苄氧羰基-α-L-天冬氨酰基-L-苯丙氨酸的低级烷基酯通过催化氢还原反应产生游离氨基酸，肽或其衍生物。与在溶解起始化合物和产物化合物的溶剂或溶解起始化合物但不溶解产物化合物的溶剂中进行反应的常规方法相反，本发明的方法利用二元二相反应介质由水和不能与水如甲苯自由混溶的有机溶剂组成。反应发生在含有溶解的起始化合物和分散在其中的催化剂的有机相中，而水溶性的反应产物顺利地依次转移到水相中，从而获得了产品出乎意料的高产率的优点，以及在反应完成后容易处理反应混合物。

8. 发明授权

US4309341A Method for purifying .alpha.- L-aspartyl-L-phenylalanine lower alkyl ester 失效
标题翻译： α-L-天冬氨酰-L-苯丙氨酸低级烷基酯的纯化方法
公开(公告)号：US4309341A
公开(公告)日：1982-01-05
申请号：US138728
申请日：1980-04-09
申请人： Masashige Kubo , Yuji Nonaka , Keiichi Kihara
发明人： Masashige Kubo , Yuji Nonaka , Keiichi Kihara
IPC分类号： B01D15/00 , C07C67/00 , C07C231/00 , C07K5/072 , C07K5/075 , C07C103/52
CPC分类号： C07K5/0613 , Y10S530/801
摘要： A method for purifying an .alpha.-L-aspartyl-L- phenylalanine lower alkyl ester containing impurities. The .alpha.-L-aspartyl-L-phenylalanine lower alkyl ester is brought into contact with a Cl-type anion exchange resin in an aqueous medium to have the impurities adsorbed by the anion exchange resin. The impurities contained in the .alpha.-L-aspartyl-L-phenylalanine lower ester, particularly diketopiperazine and .alpha.-L-aspartyl-L-phenylalanine are selectively and easily removed. The desired matter thus can be easily recovered and disposal of waste liquid, etc. can also be carried out without difficulty.
摘要翻译：一种纯化含有杂质的α-L-天冬氨酰-L-苯丙氨酸低级烷基酯的方法。使α-L-天冬氨酰基-L-苯丙氨酸低级烷基酯与水性介质中的Cl型阴离子交换树脂接触，使杂质被阴离子交换树脂吸附。包含在α-L-天冬氨酰基-L-苯丙氨酸低级酯，特别是二酮哌嗪和α-L-天冬氨酰基-L-苯丙氨酸中的杂质是有选择且易于除去的。因此可以容易地回收所需的物质，也可以毫无困难地进行废液等的处理。

9. 发明授权

US3943161A Process for producing conjugated dienes containing a cyano group 失效
标题翻译：制备含有氰基的共轭二烯的方法
公开(公告)号：US3943161A
公开(公告)日：1976-03-09
申请号：US527653
申请日：1974-11-27
申请人： Yuji Nonaka , Keiichi Kihara , Toshio Hironaka , Yasuhiro Oda
发明人： Yuji Nonaka , Keiichi Kihara , Toshio Hironaka , Yasuhiro Oda
IPC分类号： C07B61/00 , B01J23/00 , B01J27/00 , B01J31/00 , C07C67/00 , C07C253/00 , C07C255/07 , C07C255/34 , C08F36/04 , C07C120/00 , C07C121/30 , C07C121/52
CPC分类号： C07C255/00
摘要： Conjugated dienes containing a cyano group having the formula ##EQU1## wherein R.sub.1 and R.sub.2 represent hydrogen atom, an alkyl group or a phenyl group are produced by dehydrating 2-cyano-3-hydroxy-1-olefins in the presence of an alkaline catalyst while continually removing the product being formed from the reaction system.
摘要翻译：通过使2-氰基-3-羟基-1-丁烯脱水得到含有式CNR1 || CH2 = C-CH = C-R2的氰基的共轭二烯，其中R1和R2表示氢原子，烷基或苯基，在碱性催化剂的存在下连续除去由反应体系形成的产物。

10. 发明申请

US20100113390A1 OLIGOSACCHARIDES DERIVED FROM FUCOIDAN 审中-公开
标题翻译：来自FUCOIDAN的OLIGOSACCHARIDES
公开(公告)号：US20100113390A1
公开(公告)日：2010-05-06
申请号：US12524414
申请日：2007-01-26
申请人： Shigeaki Fujikawa , Yuko Fukui , Hiroshi Watanabe , Yuji Nonaka , Takeshi Yasumoto , Hideo Naoki
发明人： Shigeaki Fujikawa , Yuko Fukui , Hiroshi Watanabe , Yuji Nonaka , Takeshi Yasumoto , Hideo Naoki
IPC分类号： A61K31/715 , C07H3/04 , C07H3/06 , C07H5/10 , A61P3/04
CPC分类号： C07H11/00 , A23L33/10 , A23V2002/00 , A61K8/60 , A61K2800/782 , A61Q5/02 , A61Q19/00 , C07H7/033 , C07H13/06 , A23V2200/326 , A23V2200/332 , A23V2250/50 , A23V2250/28
摘要： The present invention provides a fucoidan-derived low molecular weight compound with a good quality of taste, which has a specified structure and function and is free from problems in absorption, antigenicity, uniformity, an anticoagulant activity and so on, which problems arise when developing fucoidan, a sulfated polysaccharide having an extremely large molecular weight, as drugs or health foods. As a result of analyzing low molecular weight compounds obtained by acid hydrolysis of fucoidan, the inventors have identified fucoidan oligosaccharides (I) to (XI). Further, these oligosaccharides have been found to have anti-obesity and/or blood glucose elevation suppressing effects through inhibition of carbohydrate and/or lipid absorption as a result of α-glucosidase inhibition and/or lipase inhibition.
摘要翻译：本发明提供具有优良品质的岩藻依聚糖衍生的低分子量化合物，其具有特定的结构和功能，并且不存在吸收，抗原性，均匀性，抗凝血活性等问题，当发展时出现问题岩藻依聚糖，分子量极大的硫酸化多糖作为药物或保健食品。通过分析由岩藻依聚糖酸水解获得的低分子量化合物的结果，本发明人鉴定了岩藻依聚糖寡糖（I）至（XI）。此外，已经发现这些寡糖通过由于α-葡糖苷酶抑制和/或脂肪酶抑制而抑制碳水化合物和/或脂质吸收而具有抗肥胖和/或血糖升高抑制作用。

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