公开(公告)号：US20040043460A1

公开(公告)日：2004-03-04

申请号：US10669503

申请日：2003-09-25

申请人： Kaneka Corporation

发明人： Shigeru Kawano ,  Miho Horikawa ,  Yoshihiko Yasohara ,  Junzo Hasegawa

IPC分类号： C12P017/10

CPC分类号： C12N9/0004 ,  C12P17/12 ,  C12P17/18 ,  C12P41/002

摘要： The present invention relates to a method of producing an optically active pyridineethanol derivative. More particularly, it relates to a method of producing an optically active polycyclic pyridineethanol derivative by causing an enzyme or enzyme source to act on polycyclic acetylpyridine derivatives. The present invention also relates to a novel enzyme which can be used in the production method mentioned above, a DNA coding for said enzyme, a recombinant vector having said DNA, and a transformant having said recombinant vector. The invention further relates to a method of producing an optically active polycyclic pyridineethanol derivative by causing the above novel enzyme or the above transformant to act on optically inactive polycyclic pyridineethanol derivatives.

摘要翻译： 本发明涉及一种制备光学活性吡啶乙醇衍生物的方法。 更具体地说，本发明涉及通过使酶或酶源作用于多环乙酰基吡啶衍生物来制备光学活性多环吡啶乙醇衍生物的方法。 本发明还涉及可用于上述制备方法的新型酶，编码所述酶的DNA，具有所述DNA的重组载体和具有所述重组载体的转化体。 本发明还涉及通过使上述新型酶或上述转化体作用于光学无活性的多环吡啶乙醇衍生物来制备光学活性多环吡啶乙醇衍生物的方法。

公开(公告)号：US20020006644A1

公开(公告)日：2002-01-17

申请号：US09870209

申请日：2001-05-30

发明人： Ki-Nam Uhm ,  Sang-Chul Lim ,  Jong-Ho Lim

IPC分类号： C12P017/12 ,  C12P017/00 ,  C12P017/10 ,  C12P017/06 ,  C12P017/04

CPC分类号： C12P7/40 ,  C12P41/00 ,  Y02P20/582

摘要： Disclosed is a method for preparing an R- or S-forms of null-substituted heterocyclic carboxylic acid (null-HCCA) and a counter enantiomeric form of null-substituted heterocyclic carboxylic acid ester thereto by use of an enzyme. A racemic null-HCCA is reacted with alcohol to give a racemic null-HCCA ester, which is then brought into contact with an enzyme with enantioselectivity, whereby either R-form or S-form of the racemate is hydrolyzed. Extraction with an organic solvent can obtain enantiomers of the null-HCCA ester. Thus, a certain enantiomeric form of null-HCCA and a counter enantiomeric form of null-HCCA ester thereto, respectively can be prepared with high optical purity at high yields as well as at low cost.

摘要翻译： 公开了一种通过使用酶制备α-取代的杂环羧酸（α-HCCA）的R-或S-型和其对映异构形式的α-取代的杂环羧酸酯的方法。 外消旋的α-HCCA与醇反应得到外消旋的α-HCCA酯，然后与具有对映选择性的酶接触，由此消旋体的R-型或S-型被水解。 用有机溶剂萃取可以得到α-HCCA酯的对映异构体。 因此，可以分别以高收率和低成本制备高光学纯度的α-HCCA的某种对映体形式和α-HCCA酯的对映异构体形式。

公开(公告)号：US20010018450A1

公开(公告)日：2001-08-30

申请号：US09730844

申请日：2000-12-07

发明人： Cordula Hopmann ,  Michael Kurz ,  Heinrich Decker ,  Dominique Le Beller ,  Jozsef Aszodi

IPC分类号： A61K031/4015 ,  C12P017/10 ,  C07D27/24

CPC分类号： C07D207/44 ,  C12P17/10

摘要： A compound named Amycomycin of the formula: 1 is described, as well as its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms. The compound is obtained by growing the microorganism Amycolatopsis species ST101170 (DSM 12216) and is useful as a pharmaceutical, particularly as an antibiotic.

摘要翻译： 描述了具有下式的化合物，称为依霉霉素，以及其药学上可接受的盐和衍生物，其所有立体异构体和互变异构形式。 该化合物是通过生长微生物无菌纲菌种ST101170（DSM121216）获得的，并且可用作药物，特别是作为抗生素。

公开(公告)号：US20030186412A1

公开(公告)日：2003-10-02

申请号：US10088920

申请日：2002-06-03

发明人： Noriyuki Kizaki ,  Yoshihiko Yasohara ,  Junzo Hasegawa

IPC分类号： C12P017/10 ,  C12N009/06 ,  C07H021/04 ,  C12P021/02 ,  C12N001/21 ,  C12N015/74

CPC分类号： C12N9/0008 ,  C12N9/0006 ,  C12P17/10 ,  C12P41/002

摘要： The present invention provides a novel polypeptide producing (S)-N-benzyl-3-pyrrolidinol, a DNA coding for it and a method of using them. A polypeptide having the following physicochemical properties (1) to (5): (1) Action: It asymmetrically reduces N-benzyl-3-pyrrolidinone to produce (S)-N-benzyl-3-pyrrolidinol with NADPH as a coenzyme; (2) Optimum action pH: 4.5 to 5.5; (3) Optimum action temperature: 40null C. to 45null C.; (4) Molecular weight: About 29,000 as determined by gel filtration analysis, about 35,000 as determined by SDS-polyacrylamide gel electrophoresis analysis; (5) Inhibitor: It is inhibited by the divalent copper ion. Further, a polypeptide having the amino acid sequence shown under SEQ ID NO:1 in the sequence listing; or a polypeptide having an amino acid sequence obtainable from the amino acid sequence shown under SEQ ID NO:1 in the sequence listing by substitution, insertion, deletion and/or addition of one or more amino acids and having enzyme activity in asymmetrically reducing N-benzyl-3-pyrrolidinone to produce (S)-N-benzyl-3-pyrrolidinol.

摘要翻译： 本发明提供了产生（S）-N-苄基-3-吡咯烷醇的新型多肽，其编码的DNA及其使用方法。 具有以下物理化学性质的多肽（1）至（5）：（1）作用：不对称地还原N-苄基-3-吡咯烷酮以制备具有NADPH作为辅酶的（S）-N-苄基-3-吡咯烷醇; （2）最佳作用pH：4.5〜5.5; （3）最佳作用温度：40℃〜45℃。 （4）分子量：通过凝胶过滤分析确定约29,000，通过SDS-聚丙烯酰胺凝胶电泳分析测定约35,000; （5）抑制剂：被二价铜离子抑制。 此外，具有序列表中SEQ ID NO：1所示的氨基酸序列的多肽; 或具有通过序列表中SEQ ID NO：1所示的氨基酸序列获得的氨基酸序列的多肽，其通过取代，插入，缺失和/或添加一个或多个氨基酸并具有不对称还原N-末端的酶活性， 苄基-3-吡咯烷酮，得到（S）-N-苄基-3-吡咯烷醇。

公开(公告)号：US20020128307A1

公开(公告)日：2002-09-12

申请号：US09815853

申请日：2001-03-23

发明人： Min Chu ,  Ronald A. Mierzwa ,  Joseph Terracciano ,  Mahesh G. Patel

IPC分类号： A61K038/21 ,  C12P017/10 ,  C12N001/20

CPC分类号： C07D207/44 ,  C12P17/10 ,  C12R1/645

摘要： Novel tetramic acid-type compounds isolated from a CCR-5 active complex produced by fermentation under controlled conditions of a biologically pure culture of the microorganism, Chaetomium globosum Kunze SCH 1705, ATCC 74489., pharmaceutical compositions containing the compounds and the use of the CCR-5 antagonist compounds and compositions to treat HIV-1 infections in humans are disclosed.

摘要翻译： 从在微生物Chaetomium globosum Kunze SCH 1705，ATCC 74489的生物纯培养物的受控条件下通过发酵产生的CCR-5活性复合物分离的新型四聚酸型化合物，含有化合物的药物组合物和CCR的用途 -5拮抗剂化合物和治疗人类HIV-1感染的组合物被公开。

公开(公告)号：US20020106763A1

公开(公告)日：2002-08-08

申请号：US09434906

申请日：1999-11-05

发明人： ZHI LI ,  BERNARD WITHOLT

IPC分类号： C12P017/10

CPC分类号： C12P17/10

摘要： A process for the preparation of optically active 3-hydroxypyrrolidine or N-substituted 3-hydroxypyrrolidines, wherein an oxygen atom is inserted stereoselectively into the corresponding pyrrolidines, respectively, by use of a bacterium having hydroxylation activity, or a prokaryotic host-organism having the gene(s) necessary for the hydroxylation, or an enzyme having hydroxylation activity derived therefrom. The bacterium may be selected from strains having alkane hydroxylases, strains degrading alkanes or mono-alicyclic compounds, or strains from the genera Pseudomonas, Mycobacterium, Corynebacterium, Nocardia, Sphingomonas, Cordona, Rhodococcus, Bacillus, Streptomyces, Sebekia and Methylococcus.

摘要翻译： 或制备光学活性的3-羟基吡咯烷或N-取代的3-羟基吡咯烷的方法，其中通过使用具有羟基化活性的细菌将氧原子立体选择性地插入相应的吡咯烷中，或者具有 羟基化所必需的基因，或由其衍生的具有羟基化活性的酶。 细菌可以选自具有烷烃羟化酶，降解烷烃或单脂环化合物的菌株，或来自假单胞菌属，分枝杆菌属，棒状杆菌属，诺卡氏菌属，鞘氨醇单胞菌属，Cordona，Rhodococcus，Bacillus，Streptomyces，Sebekia和Methylococcus的菌株。

公开(公告)号：US20040091981A1

公开(公告)日：2004-05-13

申请号：US10240056

申请日：2003-01-22

发明人： Keiji Sakamoto ,  Shinji Kita ,  Kazuya Tsuzaki ,  Tadanori Morikawa ,  Sakayu Shimizu ,  Michihiko Kataoka

IPC分类号： C12P017/10 ,  C12P013/00

CPC分类号： C12P13/001 ,  C12P13/008 ,  C12P41/002 ,  Y10S435/822 ,  Y10S435/865 ,  Y10S435/877 ,  Y10S435/911 ,  Y10S435/914 ,  Y10S435/917 ,  Y10S435/918

摘要： A process for producing an optical active null-amino alcohol, the method comprising the step of allowing at least one microorganism selected from the group consisting of microorganisms belonging to the genus Morganella and others, to act on an enantiomeric mixture of an null-aminoketone or a salt thereof having the general formula (I): 1 to produce an optical active null-amino alcohol with the desired optical activity having the general formula (II) described below in a high yield as well as in a highly selective manner: 2

摘要翻译： 一种制备光学活性β-氨基醇的方法，所述方法包括允许至少一种选自属于摩根氏菌属和其他微生物的微生物的微生物作用于α-氨基酮或其对映异构体混合物 其具有通式（I）的盐：以高产率和高度选择性的方式制备具有下述通式（II）的具有所需光学活性的光学活性β-氨基醇：

公开(公告)号：US20040072309A1

公开(公告)日：2004-04-15

申请号：US10469918

申请日：2003-09-05

发明人： Kouji Sato ,  Tsutomu Yagi ,  Yutaka Kitagawa ,  Shigeru Ichikawa ,  Akihiro Imura

IPC分类号： C12P017/10 ,  C07D205/08

CPC分类号： C07D401/04 ,  C07D205/08 ,  C12P17/10 ,  C12P41/003

摘要： A process for producing a compound represented by the following formula (II) which comprises treating a compound represented by the following formula (I) (wherein R1, R2 and R3 represent each a specific substituent) with an enzyme capable of asymmetrically hydrolyzing an ester and the novel compound (II). The process of the present invention makes it possible to easily obtain an optically active 2-azetidinone derivative in a large amount at a low cost. 1

摘要翻译： 一种制备由下式（II）表示的化合物的方法，其包括将下式（I）表示的化合物（其中R 1，R 2和R 3各自表示特定的取代基） 能够不对称地水解酯和新化合物（II）的酶。 本发明的方法能够以低成本容易地获得大量的光学活性2-氮杂环丁酮衍生物。

公开(公告)号：US20030165968A1

公开(公告)日：2003-09-04

申请号：US10376653

申请日：2003-02-27

发明人： Sarita Chauhan ,  Robert Dicosimo ,  Robert D. Fallon ,  John E. Gavagan ,  Mark S. Payne

IPC分类号： C12Q001/68 ,  C07H021/04 ,  C12P017/10 ,  C12P017/12 ,  C12P007/40 ,  C12N009/80 ,  C12N001/21 ,  C12N015/74

CPC分类号： C12P13/00 ,  C12N9/78 ,  C12P7/40 ,  C12P13/002 ,  C12P13/02

摘要： Recombinant microbial strains are provided that express nitrilase enzyme and are useful as biocatalysts for the hydrolysis of nitrile-containing substrates. The recombinant cells are transformed with a foreign gene isolated from Acidovorax facilis 72W encoding a thermostable nitrilase enzyme that catalyzes the hydrolysis of nitrile-containing substrates to carboxylic acids under mild reaction conditions. The nucleotide sequence of the nitrilase gene and the deduced amino acid sequence encoded by the nitrilase gene are provided.

摘要翻译： 提供重组微生物菌株，其表达腈水解酶，并且可用作用于含腈底物水解的生物催化剂。 将重组细胞用分离自Acidovorax facilis 72W的外源基因转化，其编码热稳定的腈水解酶，其在温和的反应条件下催化含腈底物水解成羧酸。 提供了腈水解酶基因的核苷酸序列和由腈水解酶基因编码的推导的氨基酸序列。

公开(公告)号：US20020106762A1

公开(公告)日：2002-08-08

申请号：US09973970

申请日：2001-10-09

申请人： Smith Kline Beecham plc

发明人： Richard Mark Hindley ,  Stefan Roland Woroniecki

IPC分类号： C12P017/14 ,  C12P017/10

CPC分类号： C07D417/12 ,  C12P17/14 ,  C12P17/16 ,  Y10S435/911

摘要： 1 A process for preparing a compound of formula (I), or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, wherein: T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises, treating a compound of formula (II), or a tautomeric form thereof and/or a salt thereof and/or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a microbial reductase obtained from an appropriate red yeast; and thereafter, as required, preparing a pharmaceutically acceptable salt and/or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof; compounds prepared by such a process and the use of such compounds in medicine.