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1. 发明授权

US4390626A Immobilized aminoacylase 失效
标题翻译：固定氨基酰化酶
公开(公告)号：US4390626A
公开(公告)日：1983-06-28
申请号：US288170
申请日：1981-07-29
申请人： Ichiro Chibata , Tetsuya Tosa , Takao Mori , Motoki Fujimura
发明人： Ichiro Chibata , Tetsuya Tosa , Takao Mori , Motoki Fujimura
IPC分类号： C12N11/02 , C12N11/06 , C12N11/08 , C12N11/14 , C12P13/04
CPC分类号： C12N11/14 , C12N11/08
摘要： An immobilized aminoacylase is prepared by bonding aminoacylase to a water-insoluble porous anion exchanger such as a porous phenolic resin, porous styrene resin, porous silica or porous glass having anion exchange groups and treating the bonded amino-acylase with a crosslinking agent such as an aliphatic dialdehyde. The porous anion exchanger preferably has a pore size of about 150.degree. to 3,000 A.degree., pore volume of about 0.3 to 1.0 m.sup.1 /g, specific surface area of about 10 to 150 m.sup.2 /g and particle size of above 0.1 to 1.2 mm. Preferred anion exchangers are trimethylammonium-introduced styrene resin and trimethylammonium-introduced silica.
摘要翻译：通过将氨基酰化酶结合到诸如多孔酚醛树脂，多孔苯乙烯树脂，多孔二氧化硅或具有阴离子交换基团的多孔玻璃之类的水不溶性多孔阴离子交换剂上并用交联剂处理粘合的氨基酰化酶来制备固定化的氨基酰化酶，脂肪族二醛。多孔阴离子交换剂的孔径优选为约150〜3000A，孔体积为约0.3〜1.0m1 / g，比表面积为约10〜150m2 / g，粒径为0.1〜1.2mm以上。优选的阴离子交换剂是引入三甲基铵的苯乙烯树脂和引入三甲基铵的二氧化硅。

2. 发明授权

US4309362A Process for the optical resolution of DL-p-hydroxy-phenylglycine 失效
标题翻译： DL-对羟基苯基甘氨酸的光学拆分方法
公开(公告)号：US4309362A
公开(公告)日：1982-01-05
申请号：US885804
申请日：1978-03-13
申请人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo
发明人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo
IPC分类号： C07C145/00
摘要： Seed crystals of an optically active enantiomer of any one of p-hydroxyphenylglycine benzenesulfonate, p-hydroxyphenylglycine p-ethylbenzenesulfonate, p-hydroxyphenylglycine o-toluenesulfonate or p-hydroxyphenylglycine sulfosalicylate are added to a supersaturated solution of the racemic modification of the corresponding p-hydroxyphenylglycine salt. Crystallization of the optically active enantiomer results. Then, the crystals are recovered. Alternatively, crystals of the optically active enantiomer may be added to a hot solution of the racemic modification of the corresponding p-hydroxyphenylglycine salt to produce a supersaturated solution thereof. The solution is then cooled to crystallize out the optically active enantiomer. Optically active p-hydroxyphenylglycine benzenesulfonate, optically active p-hydroxyphenylglycine p-ethylbenzenesulfonate, optically active p-hydroxyphenylglycine o-toluenesulfonate or optically active p-hydroxyphenylglycine sulfosalicylate is thereby obtained.
摘要翻译：将对羟基苯基甘氨酸苯磺酸盐，对羟基苯基甘氨酸对乙基苯磺酸盐，对羟基苯基甘氨酸邻甲苯磺酸盐或对羟基苯基甘氨酸磺基水杨酸盐的光学活性对映异构体的晶种加入到相应对羟基苯基甘氨酸的外消旋体的过饱和溶液盐。导致光学活性对映异构体的结晶。然后，回收晶体。或者，可将光学活性对映异构体的晶体加入相应对羟基苯基甘氨酸盐的外消旋体的热溶液中以产生其过饱和溶液。然后将溶液冷却以使光学活性对映异构体结晶。由此得到光学活性对羟基苯基甘氨酸苯磺酸盐，光学活性对羟基苯基甘氨酸对乙基苯磺酸盐，光学活性对羟基苯基甘氨酸邻甲苯磺酸盐或光学活性对羟基苯基甘氨酸磺基水杨酸盐。

3. 发明授权

US3953291A Process for preparing 6-aminopenicillanic acid 失效
标题翻译：制备6-氨基青霉烷酸的方法
公开(公告)号：US3953291A
公开(公告)日：1976-04-27
申请号：US450655
申请日：1974-03-13
申请人： Ichiro Chibata , Tetsuya Tosa , Tadashi Sato
发明人： Ichiro Chibata , Tetsuya Tosa , Tadashi Sato
IPC分类号： C12N11/08 , C07D499/42 , C08F2/44 , C12N11/04 , C12P37/06 , C12D9/00
CPC分类号： C08F2/44 , C12N11/04 , Y10S435/829 , Y10S435/849 , Y10S435/859 , Y10S435/875 , Y10S435/897
摘要： At least one acryloyl monomer is polymerized in an aqueous suspension containing a penicillin amidase-producing microorganism. The acryloyl monomers employed in the present invention include acryloylamide, N,N'-lower alkylene-bis-acryloylamide, bis(acryloylamidomethyl)ether and N,N'-di-acryloylethyleneurea. The resultant immobilized penicillin amidase-producing microorganism is subjected to enzymatic reaction with penicillin. 6-Amino-penicillanic acid is produced.
摘要翻译：至少一种丙烯酰基单体在含有青霉素酰胺酶生产微生物的水性悬浮液中聚合。本发明中使用的丙烯酰基单体包括丙烯酰胺，N，N'-低级亚烷基 - 双丙烯酰胺，双（丙烯酰氨基甲基）醚和N，N'-二丙烯酰亚乙基脲。所得固定的青霉素酰胺酶生产微生物与青霉素进行酶反应。生产6-氨基 - 青霉烷酸。

4. 发明授权

US4433054A Enzymatic active substance immobilized in a polysaccharide gel matrix 失效
标题翻译：固定在多糖凝胶基质中的酶活性物质
公开(公告)号：US4433054A
公开(公告)日：1984-02-21
申请号：US323288
申请日：1981-11-20
申请人： Ichiro Chibata , Tetsuya Tosa , Isao Takata
发明人： Ichiro Chibata , Tetsuya Tosa , Isao Takata
IPC分类号： C12N11/04 , C12N11/10 , C12N11/12
CPC分类号： C12N11/10 , C12N11/04
摘要： An immobilized enzymatic active substance having an improved stability of enzymatic activity is prepared which comprises an enzymatic active substance such as microbial cells entrapped within a gel matrix of an unsubstituted amino, monoalkylamino or dialkylamino group-introduced polysaccharide having not less than 10 w/w % of sulfate moiety in the molecule thereof such as carrageenan. The immobilized enzymatic active substance is prepared by admixing the enzymatic active substance and an aqueous solution of the polysaccharide and then allowing to form a gel of the polysaccharide.
摘要翻译：制备具有改善的酶活性稳定性的固定化的酶活性物质，其包含酶活性物质，例如包含在不小于10w / w％的未取代氨基，单烷基氨基或二烷基氨基引入的多糖的凝胶基质内的微生物细胞，的分子中的硫酸盐部分，例如角叉菜聚糖。通过混合酶活性物质和多糖的水溶液，然后形成多糖的凝胶来制备固定的酶活性物质。

5. 发明授权

US4415504A p-Hydroxyphenylglycine..alpha.-phenylethanesulfonate, process for production thereof and utilization thereof in resolution of p-hydroxyphenylglycine 失效
标题翻译：对羟基苯基甘氨酸。 α-苯基乙烷磺酸盐，其制备方法和在分离对羟基苯基甘氨酸中的应用
公开(公告)号：US4415504A
公开(公告)日：1983-11-15
申请号：US416338
申请日：1982-09-09
申请人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
发明人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
IPC分类号： C07B57/00 , C07C143/26
CPC分类号： C07C229/36 , C07C227/34 , C07C303/44 , C07C309/24 , C07B2200/07 , Y02P20/582
摘要： p-Hydroxyphenylglycine..alpha.-phenylethanesulfonate which is useful for the production of optically active p-hydroxyphenylglycine and optically active .alpha.-phenylethanesulfonic acid is disclosed. p-Hydroxyphenylglycine..alpha.-phenylethanesulfonate is produced by either reacting DL-p-hydroxyphenylglycine with optically active .alpha.-phenylethanesulfonic acid or reacting (.+-.)-.alpha.-phentylethanesulfonic acid with optically active p-hydroxyphenylglycine to form two diastereomers of DL-p-hydroxyphenylglycine optically active .alpha.-phenylethanesulfonate or optically active p-hydroxyphenylglycine (.+-.)-.alpha.-phenylethanesulfonate, and isolating one diastereomer according to the difference between solubilities of the diastereomers, optionally, combining selective crystallization of one diastereomer and epimerization of another diastereomer in the case of reaction of DL-p-hydroxyphenylglycine and optically active .alpha.-phenylethanesulfonic acid. This reaction is utilized in the resolution of p-hydroxyphenylglycine or .alpha.-phenylethanesulfonic acid by deacidifying the resulting diastereomer.
摘要翻译：对羟基苯基甘氨酸。公开了可用于制备光学活性对羟基苯基甘氨酸和光学活性α-苯乙烷磺酸的α-苯基乙烷磺酸盐。对羟基苯基甘氨酸。 α-苯基乙烷磺酸盐通过使DL-对羟基苯基甘氨酸与光学活性α-苯基乙烷磺酸反应或使（+/-） - α-正丁基乙磺酸与光学活性对羟基苯基甘氨酸反应形成DL-对羟基苯基甘氨酸光学活性的两种非对映异构体 α-苯基乙烷磺酸盐或光学活性对羟基苯基甘氨酸（+/-） - α-苯基乙烷磺酸盐，并根据非对映异构体的溶解度之间的差异分离一种非对映异构体，任选地，将一种非对映异构体的选择性结晶和另一种非对映异构体的差向异构化在另一种非对映异构体的情况下 DL-对羟基苯基甘氨酸和光学活性α-苯基乙烷磺酸的反应。该反应用于通过使得到的非对映异构体脱酸来分离对羟基苯基甘氨酸或α-苯基乙烷磺酸。

6. 发明授权

US4090919A Water-insoluble tannin preparation for immobilization of proteins 失效
标题翻译：用于固定蛋白质的水不溶性单宁制剂
公开(公告)号：US4090919A
公开(公告)日：1978-05-23
申请号：US760441
申请日：1977-01-19
申请人： Ichiro Chibata , Tetsuya Tosa , Takao Mori , Taizo Watanabe , Ryujiro Sano , Yuhsi Matuo
发明人： Ichiro Chibata , Tetsuya Tosa , Takao Mori , Taizo Watanabe , Ryujiro Sano , Yuhsi Matuo
IPC分类号： B01J20/32 , C07H13/12 , C07H15/04 , C07H15/08 , C12N11/02 , C07G7/02 , C07C69/76 , C07G7/00
CPC分类号： C07H13/12 , B01J20/3204 , B01J20/321 , B01J20/3212 , B01J20/3219 , B01J20/3274 , C07H15/04 , C07H15/08 , C12N11/02 , Y10S435/803 , Y10S435/815 , Y10S530/813 , Y10S530/816
摘要： A water-insoluble tannin preparation is obtained by covalent binding or physical adsorption of tannin onto a water-insoluble, hydrophilic carrier. The preparation has a specific affinity for proteins and can be used as an adsorbent for purification, isolation and/or separation of proteins (e.g., Enzymes, albumin, globulin, hormonal proteins) from a mixture of compounds. Further, the water-insoluble tannin preparation having a catalytically active enzyme absorbed thereon can be used as a heterogeneous catalyst to induce enzymatic reactions.
摘要翻译：通过将单宁进行共价结合或物理吸附到不溶于水的亲水载体上获得水不溶性单宁制剂。该制剂对蛋白质具有特异性亲和力，可用作用于从化合物混合物中纯化，分离和/或分离蛋白质（例如酶，白蛋白，球蛋白，激素蛋白质）的吸附剂。此外，具有吸附在其上的催化活性酶的水不溶性单宁制剂可以用作促进酶反应的多相催化剂。

7. 发明授权

US4032641A Nicotinoyl carnitine derivatives 失效
标题翻译：烟酰基肉碱衍生物
公开(公告)号：US4032641A
公开(公告)日：1977-06-28
申请号：US694363
申请日：1976-06-09
申请人： Ichiro Chibata , Munetsugu Miyoshi , Kohki Takashima , Shoji Moriya
发明人： Ichiro Chibata , Munetsugu Miyoshi , Kohki Takashima , Shoji Moriya
IPC分类号： C07D213/80 , A61K31/455 , C07D213/55 , C07D213/56
CPC分类号： C07D213/80
摘要： A nicotinoyl carnitine compound of the formula: ##STR1## wherein R is lower alkoxy, benzyloxy or amino and X is an anionic residue of a pharmaceutically acceptable acid, is prepared by reacting a carnitine derivative of the formula: ##STR2## wherein R is the same as defined above, with nicotinic acid or a functional derivative thereof. The derivative [I] and the pharmaceutically acceptable acid addition salts of said compound are useful as hypolipidemic agents.
摘要翻译：通过使下式的肉碱衍生物：其中R是低级烷氧基，苄氧基或氨基，X是药学上可接受的酸的阴离子残基，通过下式得到的烟酰基肉碱化合物：其中R是低级烷氧基， II]其中R与上述定义相同，与烟酸或其功能衍生物。所述化合物的衍生物[I]和药学上可接受的酸加成盐可用作降血脂药。

8. 发明授权

US4519955A Method for optical resolution of DL-.alpha.-amino acid or (.+-.)-.alpha.-phenylethanesulfonic acid 失效
标题翻译： DL-α-氨基酸或（+/-） - α-苯基乙烷磺酸的光学拆分方法
公开(公告)号：US4519955A
公开(公告)日：1985-05-28
申请号：US585767
申请日：1984-03-02
申请人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
发明人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
IPC分类号： C07C309/24 , C07B57/00 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/34 , C07C229/02 , C07C229/08 , C07C229/26 , C07C277/08 , C07C279/14 , C07C301/00 , C07C303/22 , C07C303/32 , C07C143/26 , C07B19/00 , C07D207/16 , C07D209/20
CPC分类号： C07B57/00
摘要： .alpha.-(S)-amino acid..alpha.-phenylethanesulfonate compounds and methods of optical resolution of .alpha.-amino acids and .alpha.-phenylethanesulfonic acids are described.
摘要翻译： α-（S） - 氨基酸。描述了α-苯基乙烷磺酸盐化合物和α-氨基酸和α-苯基乙烷磺酸的光学拆分方法。

9. 发明授权

US4438044A Di-L-cysteine L-malate and process for the production thereof 失效
标题翻译：二L-半胱氨酸L-苹果酸盐及其生产方法
公开(公告)号：US4438044A
公开(公告)日：1984-03-20
申请号：US284119
申请日：1981-07-16
申请人： Ichiro Chibata , Akihiko Sumi , Osamu Ohtsuki , Nozomu Izutsu
发明人： Ichiro Chibata , Akihiko Sumi , Osamu Ohtsuki , Nozomu Izutsu
IPC分类号： A61K31/195 , A61K31/19 , A61P43/00 , C07C51/00 , C07C59/245 , C07C67/00 , C07C313/00 , C07C323/58 , C07C51/02
CPC分类号： C07C59/245
摘要： Novel di-L-cysteine L-malate of the formula:[HS--CH.sub.2 --CH(NH.sub.3).sup.+ --COOH].sub.2.(.sup.- OOC--CHOH--CH.sub.2 --COO.sup.-)which has excellent storage stability and excellent pharmacological activities and is useful for the preparation of the amino acid infusion solutions, and process for the preparation of the di-L-cysteine L-malate by reacting 2 moles of L-cysteine L-malate and more than 0.9 mole of L-malic acid in an aqueous medium and collecting the resulting crystalline di-L-cysteine L-malate.
摘要翻译：新型二-L-半胱氨酸L-苹果酸盐，其具有优良的储存稳定性和优异的药理活性，具有下式：[HS-CH2-CH（NH3）+ -COOH] 2（ - OOC-CHOH-CH2-COO-）可用于制备氨基酸输液的方法，以及通过使2摩尔L-半胱氨酸L-苹果酸酯与大于0.9摩尔L-苹果酸的水溶液反应来制备二-L-半胱氨酸L-苹果酸L- 收集所得结晶二L-半胱氨酸L-苹果酸盐。

10. 发明授权

US4434107A Process for preparing an optically active p-hydroxyphenylglycine or a salt thereof 失效
标题翻译：制备光学活性对羟基苯基甘氨酸或其盐的方法
公开(公告)号：US4434107A
公开(公告)日：1984-02-28
申请号：US392535
申请日：1982-06-28
申请人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
发明人： Ichiro Chibata , Shigeki Yamada , Chikara Hongo , Ryuzo Yoshioka
IPC分类号： C07B55/00 , C07B31/00 , C07B57/00 , C07C67/00 , C07C227/34 , C07C229/36 , C07C143/30 , C07C101/72
CPC分类号： C07C227/34
摘要： The present invention relates to the optical resolution of a p-hydroxyphenylglycine salt with simultaneous racemization of the undesired enantiomer thereof. The invention is carried out by preferential crystallizing out the desired enantiomer from a supersaturated solution of the racemic modification thereof in a lower aliphatic acid in the presence of an aliphatic or aromatic aldehyde.
摘要翻译：本发明涉及对羟基苯基甘氨酸盐的光学拆分，同时使其不需要的对映异构体进行外消旋化。本发明通过优选在脂族或芳族醛存在下将其外消旋化合物的过饱和溶液在低级脂族酸中结晶出所需的对映体来进行。

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