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1. 发明授权

US5284754A Process for the continuous conversion of cephalosporin derivatives into glutaryl-7-aminocephalosporanic acid derivatives 失效
标题翻译：将头孢菌素衍生物连续转化为戊二酰-7-氨基头孢烷酸衍生物的方法
公开(公告)号：US5284754A
公开(公告)日：1994-02-08
申请号：US754000
申请日：1991-09-03
申请人： Thomas Bayer , Klaus Sauber
发明人： Thomas Bayer , Klaus Sauber
IPC分类号： C07D501/20 , C12N9/06 , C12N11/08 , C12N11/10 , C12P35/00 , C12P35/06
CPC分类号： C12N9/0024 , C12N11/08 , C12N11/10 , C12P35/06 , Y10S435/911
摘要： A process for the continuous conversion of cephalosporin derivatives into glutaryl-7-aminocephalosporanic acid derivativesA process for the continuous conversion of cephalosporin derivatives into the corresponding glutaryl-7-aminocephalosporanic acid derivatives in the presence of a catalyst containing D-amino-acid oxidase is described. The product yield can be increased, where appropriate, by addition of hydrogen peroxide.
摘要翻译：将头孢菌素衍生物连续转化为戊二酰-7-氨基头孢烷酸衍生物的方法在含有D-氨基酸氧化酶的催化剂存在下，将头孢菌素衍生物连续转化成相应的戊二酰-7-氨基头孢烷酸衍生物的方法是描述。通过加入过氧化氢可以适当地增加产物的产率。

2. 发明授权

US4783404A L-aminoacid oxidase from yeasts of the genus cryptococcus, their preparation and use 失效
标题翻译：来自隐球菌属酵母的L-氨基酸氧化酶，其制备和用途
公开(公告)号：US4783404A
公开(公告)日：1988-11-08
申请号：US650638
申请日：1984-09-14
申请人： Werner Aretz , Klaus Sauber
发明人： Werner Aretz , Klaus Sauber
IPC分类号： C12N1/16 , C12N9/06 , C12P7/40 , C12P41/00 , C12R1/645 , C12P7/62 , C12P7/44
CPC分类号： C12N9/0022 , C12P41/006 , C12P7/40 , C12R1/645 , Y10S435/911
摘要： Yeasts of the genus cryptococcus, preferably of the species C. Laurentii, form, in the presence of aminoacids, an L-aminoacid oxidase which stereospecifically converts L-aminoacids and their derivatives into the corresponding .alpha.-ketoacids. The immobilized cells are advantageously used for this conversion, which can also be used to resolve racemates.
摘要翻译：隐球菌属的酵母，优选品种C. Laurentii，在氨基酸存在下，形成L-氨基酸氧化酶，其立体选择性地将L-氨基酸及其衍生物转化成相应的α-酮酸。固定的细胞有利地用于该转化，其也可用于溶解外消旋体。

3. 发明授权

US5506202A Insulin derivatives, a process for the preparation thereof, the use thereof, and a pharmaceutical formulation containing them 失效
标题翻译：胰岛素衍生物，其制备方法，其用途和含有它们的药物制剂
公开(公告)号：US5506202A
公开(公告)日：1996-04-09
申请号：US442296
申请日：1995-05-16
申请人： Laszlo Vertesy , Karl Geisen , Gunther J. Riess , Klaus Sauber
发明人： Laszlo Vertesy , Karl Geisen , Gunther J. Riess , Klaus Sauber
IPC分类号： C12P21/02 , A61K38/00 , A61K38/28 , A61P3/08 , A61P3/10 , C07H21/04 , C07K1/06 , C07K1/08 , C07K1/20 , C07K14/575 , C07K14/62 , C12N15/09 , C12R1/19 , C12R1/465
CPC分类号： C07K14/62 , A61K38/00
摘要： New insulin derivatives, a process for their preparation and use, and a pharmaceutical formulation containing them are disclosed. The derivatives contain the basic amino acid arginine at the amino-terminal position of the insulin A-chain, and various amino acid substitutions at the carboxyl terminus of the insulin B-chain. The compounds are suitable for the treatment of diabetes mellitus, have a delayed profile of action and are very well tolerated.
摘要翻译：公开了新的胰岛素衍生物，其制备和使用的方法以及含有它们的药物制剂。衍生物含有胰岛素A链氨基末端位置的碱性氨基酸精氨酸，胰岛素B链羧基末端的各种氨基酸取代。该化合物适用于治疗糖尿病，具有延迟的作用特征并且耐受性良好。

4. 发明授权

US4931476A Crosslinked polymers and a process for their preparation 失效
标题翻译：交联聚合物及其制备方法
公开(公告)号：US4931476A
公开(公告)日：1990-06-05
申请号：US89443
申请日：1987-08-26
申请人： Otto Mauz , Siegfried Noetzel , Klaus Sauber
发明人： Otto Mauz , Siegfried Noetzel , Klaus Sauber
IPC分类号： A61K39/385 , A61K39/44 , A61K47/30 , C08F2/12 , C08F16/14 , C08F20/32 , C08F26/00 , C08F216/14 , C08F220/28 , C08F220/32 , C08F226/00 , C08F226/02 , C12N11/08 , G01N33/545
CPC分类号： C08F216/14 , C08F220/28 , C08F226/00 , C12N11/08
摘要： Crosslinked polymers which are produced from monomers containing epoxide groups, crosslinking monomers and, where appropriate, other monoethylenically unsaturated monomers are composed of principally spherical porous particles and are very suitable as carrier materials for the immobilization of biologically active substances.
摘要翻译：由含有环氧基的单体，交联单体和适当的其它单烯属不饱和单体制备的交联聚合物由主要为球形的多孔颗粒组成，非常适合用作固定生物活性物质的载体材料。

5. 发明授权

US4568706A Macroporous bead polymers, a process for their preparation and their use 失效
标题翻译：大孔珠聚合物，其制备方法及其用途
公开(公告)号：US4568706A
公开(公告)日：1986-02-04
申请号：US614137
申请日：1984-05-25
申请人： Siegfried Noetzel , Otto Mauz , Klaus Sauber
发明人： Siegfried Noetzel , Otto Mauz , Klaus Sauber
IPC分类号： A61K47/48 , B01D15/08 , B01J20/26 , C08F20/54 , C12N11/08 , C08J9/00
CPC分类号： C08F20/54 , A61K47/48176 , B01D15/08 , B01J20/26 , C12N11/08 , B01D15/3809
摘要： The invention relates to bead polymers based on monomers of the formula ##STR1## in which X is hydrogen or methyl, R denotes an aliphatic hydrocarbon radical having 1 to 12 carbon atoms, and Y denotes OH or NH.sub.2, which have been prepared using a special dispersion stabilizer. They are particularly distinguished by high porosity and are very suitable as carrier materials for biologically active substances.
摘要翻译：本发明涉及基于式（I）的单体的珠粒聚合物，其中X是氢或甲基，R表示具有1至12个碳原子的脂族烃基，Y表示OH或NH 2，其已经制备使用特殊的分散稳定剂。它们特别是高孔隙度的区别，并且非常适合作为生物活性物质的载体材料。

6. 发明授权

US5599702A D-amino acid oxidase from Trigonopsis variabilis immobilized on porous copolymer beads 失效
标题翻译：固定在多孔共聚物珠上的来自不同变种的D-氨基酸氧化酶
公开(公告)号：US5599702A
公开(公告)日：1997-02-04
申请号：US443017
申请日：1995-05-17
申请人： Klaus Sauber
发明人： Klaus Sauber
IPC分类号： C08F8/12 , C08F218/08 , C12N11/08 , C12N11/18 , C12P17/18 , C12P35/06 , C12R1/01 , C12N11/06 , C12P35/00
CPC分类号： C12N11/18 , C12N11/08 , C12P35/06 , Y10S435/911
摘要： D-amino acid oxidase (DAO) in purified, partially purified or crude form is immobilized on a porous bead-shaped support that is a copolymer of vinyl acetate and/or vinyl alcohol and a crosslinking agent. A preferred crosslinking agent is N,N'-divinylethyleneurea. The amount of crosslinking agent is 1 to 60% by weight of the copolymer, and acyloxy groups of vinyl acetate may be present on the support as such or may have been hydrolyzed to hydroxyl groups. The support preferably has a mean particle size of 20 to 800 .mu.m and a mean pore diameter of 2 to 10,000 nm. The D-amino acid oxidase is preferably obtained from Trigonopsis variabilis and purified by ion exchange chromatography. The D-amino acid oxidase may be covalently bonded to a spacer such as epichlorohydrin or its homolog that is bound to the support. Catalase may also be immobilized.
摘要翻译：纯化，部分纯化或粗制的D-氨基酸氧化酶（DAO）固定在作为乙酸乙烯酯和/或乙烯醇和交联剂的共聚物的多孔珠状载体上。优选的交联剂是N，N'-二乙烯基亚乙基脲。交联剂的量为共聚物的1至60重量％，乙酸乙烯酯的酰氧基可以存在于载体上，或者可能已经水解成羟基。该载体的平均粒径优选为20〜800μm，平均孔径为2〜10,000nm。 D-氨基酸氧化酶优选得自变形变种，并通过离子交换层析纯化。 D-氨基酸氧化酶可以共价结合到间隔基如表氯醇或其与载体结合的同系物。过氧化氢酶也可以被固定化。

7. 发明授权

US5538946A Hirudin derivatives with delayed action 失效
标题翻译：水蛭素衍生物具有延迟作用
公开(公告)号：US5538946A
公开(公告)日：1996-07-23
申请号：US895436
申请日：1992-06-05
申请人： Peter Crause , Paul Habermann , Martin Kramer , Rainer Obermeier , Klaus Sauber , Dominique Tripier
发明人： Peter Crause , Paul Habermann , Martin Kramer , Rainer Obermeier , Klaus Sauber , Dominique Tripier
IPC分类号： C12N9/99 , A61K38/00 , A61K38/55 , A61K47/48 , A61P7/02 , C07K1/113 , C07K1/20 , C07K1/22 , C07K14/81 , C07K14/815 , C07K17/10 , C12P21/02 , C12R1/645 , C07K5/00 , C07K7/00 , C07K3/00
CPC分类号： A61K47/4823 , C07K14/815 , A61K38/00
摘要： The present invention relates to hirudin derivatives which are formed from hirudin or the physiologically acceptable salt thereof and a carrier, to a process for the preparation thereof, and to the use thereof as thrombin inhibitor.
摘要翻译：本发明涉及由水蛭素或其生理学上可接受的盐和载体形成的水蛭素衍生物，其制备方法及其作为凝血酶抑制剂的用途。

8. 发明授权

US5162212A Transaminase from E. coli DH-1 (ATCC 33849) 失效
标题翻译：来自大肠杆菌DH-1（ATCC 33849）的转氨酶
公开(公告)号：US5162212A
公开(公告)日：1992-11-10
申请号：US854516
申请日：1992-03-20
申请人： Arno Schulz , Klaus Bartsch , Dominique Tripier , Klaus Sauber
发明人： Arno Schulz , Klaus Bartsch , Dominique Tripier , Klaus Sauber
IPC分类号： C12N9/10 , C12N11/08 , C12P13/04 , C12R1/19
CPC分类号： C12N11/08 , C12N9/1096 , C12P13/04 , Y10S435/849
摘要： A new transaminase has been isolated from E. coli DH-1 (ATCC 33849). It is possible to use the transaminase with great efficiency to prepare L-phosphinothricin and gamma-aminobutyric acid from appropriate precursors by transferring an amino group from glutamate.
摘要翻译：已经从大肠杆菌DH-1（ATCC 33849）中分离出新的转氨酶。通过从谷氨酸转移氨基，可以高效地使用转氨酶从合适的前体制备L-膦丝菌素和γ-氨基丁酸。

9. 发明授权

US4389488A Process for the enzymatic preparation of L-2-amino-4-methylphosphinobutyric acid 失效
标题翻译：用于酶制剂L-2-氨基-4-甲基膦酰基丁酸的方法
公开(公告)号：US4389488A
公开(公告)日：1983-06-21
申请号：US332852
申请日：1981-12-21
申请人： Susanne Grabley , Klaus Sauber
发明人： Susanne Grabley , Klaus Sauber
IPC分类号： C12P7/52 , C07F9/30 , C12P13/04 , C12P41/00 , C07B19/02 , C12R1/19
CPC分类号： C12P13/04 , C07F9/301 , Y10S435/849
摘要： A process for the enzymatic preparation of L-2-amino-4-methylphosphinobutyric acid by enzymatic cleavage of the corresponding N-arylacetyl derivatives using penicillin-G-acylase.
摘要翻译：通过使用青霉素-G-酰基转移酶相应的N-芳基乙酰基衍生物酶切制备L-2-氨基-4-甲基膦酰基丁酸的方法。

10. 发明授权

US5130246A Process for producing transaminase from E. coli ATCC 33849 失效
标题翻译：从大肠杆菌ATCC 33849生产转移酶的方法
公开(公告)号：US5130246A
公开(公告)日：1992-07-14
申请号：US359591
申请日：1989-06-01
申请人： Arno Schulz , Klaus Bartsch , Dominique Tripier , Klaus Sauber
发明人： Arno Schulz , Klaus Bartsch , Dominique Tripier , Klaus Sauber
IPC分类号： C12N9/10 , C12N11/08 , C12P13/04 , C12R1/19
CPC分类号： C12N11/08 , C12N9/1096 , C12P13/04 , Y10S435/849
摘要： A process for the preparation of a purified transaminase having a molecular weight of 20,000 to 250,000 daltons, an isoelectric point at a pH between 3.0 and 8.0, a pH optimum in a range from 5.0 to 10.0 and a substrate specificity for the transamination of (3-carboxy-3-oxo-propyl)-methyl-phosphinic acid or the esters thereof.The production of the enzyme comprises cultivating E. coli ATCC 33849, disrupting the cultivated E. coli ATCC 33849, obtaining a supernatant therefrom containing the enzyme and isolating the transaminase by heating the supernatant at a temperature and for a time sufficient to denature proteins other than the transaminase and than finally removing the denatured proteins from the supernatant.
摘要翻译：一种制备分子量为20,000至250,000道尔顿的纯化转氨酶的方法，pH 3.0至8.0之间的等电点，最适pH为5.0至10.0的pH值和（3 - 羧基-3-氧代 - 丙基） - 甲基 - 次膦酸或其酯。酶的生产包括培养大肠杆菌ATCC 33849，破坏培养的大肠杆菌ATCC 33849，从其中获得含有该酶的上清液，并通过在足以使蛋白质以外的蛋白质变性的温度和时间下加热上清液来分离转氨酶转氨酶，最后从上清液中除去变性的蛋白质。

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