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    Novel Carbonyl Reductase, Gene Therefor and Use Thereof
    3.
    发明申请
    Novel Carbonyl Reductase, Gene Therefor and Use Thereof 失效
    新型羰基还原酶，其基因及其用途

    公开(公告)号：US20090029430A1

    公开(公告)日：2009-01-29

    申请号：US11665065

    申请日：2005-10-20

    申请人： Noriyuki Kizaki ,  Mokoto Ueda ,  Daisuke Moriyama ,  Naoaki Taoka ,  Yoshihiko Yasohara

    发明人： Noriyuki Kizaki ,  Mokoto Ueda ,  Daisuke Moriyama ,  Naoaki Taoka ,  Yoshihiko Yasohara

    IPC分类号： C12P7/02 ,  C07H21/04 ,  C07K14/00 ,  C12N15/63 ,  C12N1/21

    CPC分类号： C12N9/0006 ,  C12P7/04 ,  C12P7/62 ,  C12P13/002 ,  C12P41/002

    摘要： The present invention is to provide a process for efficiently producing an optically active alcohol including (R)-3-hydroxy-3-phenylpropanenitrile. One of the features of the present invention is a polypeptide having an activity of asymmetrically reducing 3-oxo-3-phenylpropanenitrile isolated from a microorganism belonging to the genus Candida to produce (R)-3-hydroxy-3-phenylpropanenitrile, DNA encoding the polypeptide and a transformant of producing the polypeptide. Another feature of the present invention is a process for producing an optically active alcohol such as (R)-3-hydroxy-3-phenylpropanenitrile by reducing a carbonyl compound such as 3-oxo-3-phenylpropanenitrile by use of the polypeptide or the transformant.

    摘要翻译： 本发明提供一种有效制备包含（R）-3-羟基-3-苯基丙腈的光学活性醇的方法。 本发明的特征之一是具有不对称还原从属于念珠菌属的微生物分离的3-氧代-3-苯基丙腈的活性的多肽，以产生（R）-3-羟基-3-苯基丙腈，编码 多肽和产生多肽的转化体。 本发明的另一个特征是通过使用多肽或转化体还原羰基化合物如3-氧代-3-苯基丙腈来制备光学活性醇如（R）-3-羟基-3-苯基丙腈的方法 。

    Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same
    4.
    发明授权
    Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same 失效
    取代的乙酰基吡啶衍生物及其制备用于光学活性β3激动剂的中间体的方法

    公开(公告)号：US06642387B2

    公开(公告)日：2003-11-04

    申请号：US10305105

    申请日：2002-11-27

    申请人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    发明人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    IPC分类号： C07D21346

    CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/74 ,  C07D213/75 ,  C07D405/04

    摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16)

    摘要翻译： 目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。 由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原反应来制备由通式（10）表示的光学活性羟乙基吡啶衍生物（其中*表示不对称碳原子），并进一步衍生为中间体 的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物，

    Process for producing simvastatin
    5.
    发明授权
    Process for producing simvastatin 有权
    辛伐他汀生产工艺

    公开(公告)号：US06331641B1

    公开(公告)日：2001-12-18

    申请号：US09601794

    申请日：2000-09-28

    申请人： Naoaki Taoka ,  Kenji Inoue

    发明人： Naoaki Taoka ,  Kenji Inoue

    IPC分类号： C07D30930

    CPC分类号： C07D319/06 ,  C07D309/30 ,  Y02P20/55

    摘要： This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor, which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting diol lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.

    摘要翻译： 本发明提供了一种用于生产作为HMG-CoA还原酶抑制剂的伟大用途的辛伐他汀的简单和有效的方法，其包括用无机碱和仲或叔醇脱氢洛伐他汀，并使所得二醇内酯用缩酮进行选择性保护 或缩醛保护基，酰化和去保护 - 内酯化得到辛伐他汀。

    METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF
    6.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF 审中-公开
    用于生产光学活性的3-氨基哌啶或其盐的方法

    公开(公告)号：US20150166481A1

    公开(公告)日：2015-06-18

    申请号：US14633622

    申请日：2015-02-27

    申请人： Kohei MORI ,  Masutoshi NOJIRI ,  Akira NISHIYAMA ,  Naoaki TAOKA

    发明人： Kohei MORI ,  Masutoshi NOJIRI ,  Akira NISHIYAMA ,  Naoaki TAOKA

    IPC分类号： C07D211/60 ,  C07D211/56

    CPC分类号： C07D211/60 ,  C07B57/00 ,  C07D211/56 ,  C12P17/12 ,  C12P41/006

    摘要： The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.

    摘要翻译： 本发明涉及一种光学活性3-氨基哌啶或其盐的制备方法。 在该方法中，外消旋的丙内酰胺立体选择性地水解，得到光生活性的哌甲酰胺和光学活性的啮齿二甲酸，在衍生自生物体的酶源存在下，然后将光学活性的哌甲酰胺衍生成光学活性的氨基哌啶或其盐 通过酰化，Hofmann重排，氨基脱保护和进一步去保护; 或通过用BOC，霍夫曼重排和进一步去保护的选择性保护将光学活性的哌甲酰胺衍生成光学活性氨基哌啶或其盐。 通过本发明可以通过适用于工业制造的容易的方法从廉价且容易获得的原料中制备用作药物中间体的光学活性3-氨基哌啶或其盐。

    Carbonyl reductase, gene therefor and use thereof
    9.
    发明授权
    Carbonyl reductase, gene therefor and use thereof 失效
    羰基还原酶，其基因及其用途

    公开(公告)号：US08008461B2

    公开(公告)日：2011-08-30

    申请号：US11665065

    申请日：2005-10-20

    申请人： Noriyuki Kizaki ,  Makoto Ueda ,  Daisuke Moriyama ,  Naoaki Taoka ,  Yoshihiko Yasohara

    发明人： Noriyuki Kizaki ,  Makoto Ueda ,  Daisuke Moriyama ,  Naoaki Taoka ,  Yoshihiko Yasohara

    IPC分类号： C07H21/04 ,  C12N9/02 ,  C12P21/02 ,  C12P13/00 ,  C07C255/01

    CPC分类号： C12N9/0006 ,  C12P7/04 ,  C12P7/62 ,  C12P13/002 ,  C12P41/002

    摘要： The present invention is to provide a process for efficiently producing an optically active alcohol including (R)-3-hydroxy-3-phenylpropanenitrile. One of the features of the present invention is a polypeptide having an activity of asymmetrically reducing 3-oxo-3-phenylpropanenitrile isolated from a microorganism belonging to the genus Candida to produce (R)-3-hydroxy-3-phenylpropanenitrile, DNA encoding the polypeptide and a transformant of producing the polypeptide. Another feature of the present invention is a process for producing an optically active alcohol such as (R)-3-hydroxy-3-phenylpropanenitrile by reducing a carbonyl compound such as 3-oxo-3-phenylpropanenitrile by use of the polypeptide or the transformant.

    摘要翻译： 本发明提供一种有效制备包含（R）-3-羟基-3-苯基丙腈的光学活性醇的方法。 本发明的特征之一是具有不对称还原从属于念珠菌属的微生物分离的3-氧代-3-苯基丙腈的活性的多肽，以产生（R）-3-羟基-3-苯基丙腈，编码 多肽和产生多肽的转化体。 本发明的另一个特征是通过使用多肽或转化体还原羰基化合物如3-氧代-3-苯基丙腈来制备光学活性醇如（R）-3-羟基-3-苯基丙腈的方法 。

    Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof
    10.
    发明授权
    Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof 有权
    光学活性-3-氨基-2-羟基丙基丙烯酰胺衍生物及其盐的制备方法

    公开(公告)号：US07834190B2

    公开(公告)日：2010-11-16

    申请号：US12227788

    申请日：2007-05-22

    申请人： Kohei Mori ,  Akira Nishiyama ,  Naoaki Taoka ,  Daisuke Moriyama ,  Nobuo Nagashima

    发明人： Kohei Mori ,  Akira Nishiyama ,  Naoaki Taoka ,  Daisuke Moriyama ,  Nobuo Nagashima

    IPC分类号： C07D263/08 ,  C07D303/02

    CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C67/31 ,  C07C231/18 ,  C07C237/04 ,  C07C237/22 ,  C07C2601/02 ,  C07D263/16 ,  C07D301/24 ,  C07D303/16 ,  C07D303/48 ,  C12P7/42 ,  C12P13/02 ,  C12P41/002 ,  C07C69/675

    摘要： An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.

    摘要翻译： 本申请的目的是提供从便宜的廉价起始材料制备光学活性3-氨基-2-羟基丙基环丙基酰胺衍生物或其盐的工业上可行的方法。 其衍生物或其盐可用作药物的中间体。 本申请还希望提供衍生物的有用中间体。 目的是通过以下方法实现。 首先，容易获得的2-卤代-3-氧代丙酸衍生物被不对称地还原，然后环氧化以产生光学活性的环氧羧酸衍生物。 接下来，通过与环丙胺反应将衍生物转化为光学活性的环氧酰胺衍生物，然后与腈反应，得到光学活性的恶唑啉酰胺衍生物。 随后，恶唑啉骨架的选择性酸溶剂解产生光学活性3-氨基-2-羟基丙基丙烯酰胺衍生物或其盐。