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1. 发明申请

US20060223152A1 Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
标题翻译：光学活性2-烯丙基羧酸衍生物及其制备方法
公开(公告)号：US20060223152A1
公开(公告)日：2006-10-05
申请号：US10553394
申请日：2004-04-16
申请人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
发明人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C12P13/00 , C07F3/02
CPC分类号： C07C233/18 , C07B2200/07 , C07C51/06 , C07C67/20 , C07C233/05 , C07C271/64 , C12P7/40 , C12P41/005 , C07C57/03 , C07C69/533
摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process. An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.
摘要翻译：本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备，和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。

2. 发明授权

US07282605B2 Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
标题翻译：光学活性2-烯丙基羧酸衍生物及其制备方法
公开(公告)号：US07282605B2
公开(公告)日：2007-10-16
申请号：US10553394
申请日：2004-04-16
申请人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
发明人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C07C291/00 , C07C237/16 , C07C237/18 , C07C237/20
CPC分类号： C07C233/18 , C07B2200/07 , C07C51/06 , C07C67/20 , C07C233/05 , C07C271/64 , C12P7/40 , C12P41/005 , C07C57/03 , C07C69/533
摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process.An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.
摘要翻译：本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备，和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。

3. 发明申请

US20110236955A1 ARYLACYLAMIDASE GENE AND METHOD OF USING THE SAME 审中-公开
标题翻译： ARYLACYLAMIDASE基因及其使用方法
公开(公告)号：US20110236955A1
公开(公告)日：2011-09-29
申请号：US11576560
申请日：2005-09-26
申请人： Noriyuki Kizaki , Noriyuki Ito , Yoshihiko Yasohara , Toru Nagasawa
发明人： Noriyuki Kizaki , Noriyuki Ito , Yoshihiko Yasohara , Toru Nagasawa
IPC分类号： C12N9/80 , C12N15/55 , C12N15/63 , C12N1/21
CPC分类号： C12N9/80
摘要： The present invention provides an efficient method of producing an arylacylamidase. In an aspect, the present invention provides (a) a DNA comprising the base sequence shown in the sequence listing under SEQ ID NO:1, or (b) a DNA capable of hybridizing, under stringent conditions, with a DNA comprising the base sequence complementary to the base sequence shown in the sequence listing under SEQ ID NO:1 and coding for a polypeptide having arylacylamidase activity. In another aspect, the invention provides a polypeptide encoded by the DNA mentioned above and having arylacylamidase activity, a vector containing the DNA mentioned above, a transformant which is transformed using the DNA or the vector mentioned above, and a method for producing an arylacylamidase which comprises cultivating the transformant mentioned above and obtaining the arylacylamidase from the culture medium.
摘要翻译：本发明提供了生产芳基酰胺酶的有效方法。一方面，本发明提供（a）包含SEQ ID NO：1中的序列表中所示的碱基序列的DNA，或（b）能够在严格条件下与包含碱基序列的DNA杂交的DNA 与SEQ ID NO：1中的序列表中所示的碱基序列互补，并编码具有芳基酰胺酶活性的多肽。另一方面，本发明提供由上述DNA编码并具有芳基酰胺酶活性的多肽，含有上述DNA的载体，使用上述DNA或载体转化的转化体及其制备方法，包括培养上述转化体并从培养基中获得芳酰胺酰胺酶。

4. 发明授权

US09481870B2 Nucleic acid encoding a polypeptide having aminotransferase activity, vectors and host cells comprising the nucleic acid 有权
标题翻译：编码具有氨基转移酶活性的多肽的核酸，载体和包含该核酸的宿主细胞
公开(公告)号：US09481870B2
公开(公告)日：2016-11-01
申请号：US13876400
申请日：2011-09-28
申请人： Toru Nagasawa , Toyokazu Yoshida , Kouichi Ishida , Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
发明人： Toru Nagasawa , Toyokazu Yoshida , Kouichi Ishida , Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
IPC分类号： C07H21/00 , C12N1/21 , C12N1/19 , C12P17/00 , C12P41/00 , C12N1/15 , C12N9/10 , C12P17/10
CPC分类号： C12N9/1096 , C12P17/10 , C12P41/006 , C12Y206/01 , Y02P20/52
摘要： A method for efficiently producing an optically active amino compound useful as an intermediate for pharmaceutical preparations, agricultural chemicals, or the like, from a ketone compound is provided. Specifically, a polypeptide having high resistance to a water-soluble organic solvent and novel transaminase activity for generating (S)-1-benzyl-3-pyrrolidinone with high optical purity of 93% or more, a gene encoding the same, and a transformant expressing the gene at a high level are also provided herein.
摘要翻译：提供了从酮化合物有效地制备用作药物制剂，农药等的中间体的光学活性氨基化合物的方法。具体地说，对水溶性有机溶剂具有高抗性的多肽和具有93％以上的光学纯度的（S）-1-苄基-3-吡咯烷酮的新型转氨酶活性，编码该多肽的基因，以及转化体本文还提供了表达高水平的基因。

5. 发明申请

US20090148899A1 METHOD FOR PRODUCING OPTICALLY-ACTIVE AMINE COMPOUND, RECOMBINANT VECTOR, AND TRANSFORMANT CONTAINING THE VECTOR 有权
标题翻译：生产光活性胺化合物的方法，重组载体和包含载体的转化体
公开(公告)号：US20090148899A1
公开(公告)日：2009-06-11
申请号：US12302460
申请日：2007-05-28
申请人： Shigeru Kawano , Noriyuki Ito , Yoshihiko Yasohara
发明人： Shigeru Kawano , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C12P13/00 , C12N15/63 , C12N1/21 , C12P21/00
CPC分类号： C12P13/008 , C12N9/0004 , C12N9/0006 , C12N9/1096 , C12P13/001 , C12P13/002 , C12P17/10
摘要： The present invention relates to a method for producing an optically-active amine compound. The method is characterized by using a transaminase (A), an α-keto acid reductase (B), and an enzyme (C), each having specific properties, in an identical reaction system to convert a ketone compound into a corresponding optically-active amine compound in which a carbon atom with an amino group bonded thereto serves as an asymmetric point. The present invention also relates to a recombinant vector for use in the method. The present invention makes it possible to efficiently produce an optically-active amine compound.
摘要翻译：本发明涉及一种光学活性胺化合物的制造方法。该方法的特征在于在相同的反应体系中使用转氨酶（A），α-酮酸还原酶（B）和具有特定性质的酶（C），以将酮化合物转化为相应的光学活性具有与其结合的氨基的碳原子作为不对称点的胺化合物。本发明还涉及用于该方法的重组载体。本发明使得有效地制备光学活性胺化合物成为可能。

6. 发明申请

US20140004575A1 MODIFIED AMINOTRANSFERASE, GENE THEREOF, AND METHOD FOR PRODUCING OPTICALLY ACTIVE AMINO COMPOUND USING SAME 有权
标题翻译：改性氨基转移酶及其基因及其生产使用其的光学活性氨基化合物的方法
公开(公告)号：US20140004575A1
公开(公告)日：2014-01-02
申请号：US14004293
申请日：2012-03-09
申请人： Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
发明人： Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
IPC分类号： C12N9/10
CPC分类号： C12N9/1096 , C12P13/001 , C12P13/04 , C12P41/006
摘要： Provided is a method for efficiently producing from a ketone compound an optically active amino compound useful as an intermediate of a drug, an agricultural chemical, or the like. Provided are: a polypeptide having aminotransferase activity that is increased in stereoselectivity, heat resistance, and resistance to amine compounds compared to the wild type enzyme by means of modifying an aminotransferase derived from Pseudomonas fluorescens; a gene encoding the polypeptide; and a transformant that expresses the gene at a high level.
摘要翻译：提供一种从酮化合物有效地制备用作药物，农药等的中间体的光学活性氨基化合物的方法。提供：通过修饰衍生自荧光假单胞菌的氨基转移酶，与野生型酶相比，具有增加立体选择性，耐热性和耐胺性化合物的氨基转移酶活性的多肽; 编码该多肽的基因; 以及高水平表达基因的转化体。

7. 发明授权

US08168412B2 Method for producing optically-active amine compound, recombinant vector, and transformant containing the vector 有权
标题翻译：生产光学活性胺化合物，重组载体和含有该载体的转化体的方法
公开(公告)号：US08168412B2
公开(公告)日：2012-05-01
申请号：US12302460
申请日：2007-05-28
申请人： Shigeru Kawano , Noriyuki Ito , Yoshihiko Yasohara
发明人： Shigeru Kawano , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C12P13/00
CPC分类号： C12P13/008 , C12N9/0004 , C12N9/0006 , C12N9/1096 , C12P13/001 , C12P13/002 , C12P17/10
摘要： The present invention relates to a method for producing an optically-active amine compound. The method is characterized by using a transaminase (A), an α-keto acid reductase (B), and an enzyme (C), each having specific properties, in an identical reaction system to convert a ketone compound into a corresponding optically-active amine compound in which a carbon atom with an amino group bonded thereto serves as an asymmetric point. The present invention also relates to a recombinant vector for use in the method. The present invention makes it possible to efficiently produce an optically-active amine compound.
摘要翻译：本发明涉及一种光学活性胺化合物的制造方法。该方法的特征在于在相同的反应体系中使用转氨酶（A），α-酮酸还原酶（B）和具有特定性质的酶（C），以将酮化合物转化为相应的光学活性具有与其结合的氨基的碳原子作为不对称点的胺化合物。本发明还涉及用于该方法的重组载体。本发明使得有效地制备光学活性胺化合物成为可能。

8. 发明申请

US20130196389A1 NOVEL TRANSAMINASE EXHIBITING HIGH ACTIVITY FOR GLUTAMIC ACID, GENE ENCODING SAME, AND METHOD FOR USING THEM 有权
标题翻译：新型透明质酸酶展示用于谷氨酸的高活性，编码它们的基因及其使用方法
公开(公告)号：US20130196389A1
公开(公告)日：2013-08-01
申请号：US13876412
申请日：2011-09-28
申请人： Noriyuki Ito , Akiko Nishi , Shigeru Kawano , Yoshihiko Yasohara
发明人： Noriyuki Ito , Akiko Nishi , Shigeru Kawano , Yoshihiko Yasohara
IPC分类号： C12N9/10
CPC分类号： C12N9/1096 , C12P17/10 , C12P41/006 , C12Y206/01 , Y02P20/52
摘要： A method for inexpensively and efficiently producing an optically active amino compound useful as an intermediate for pharmaceutical preparations, agricultural chemicals, or the like, from a ketone compound is provided. Specifically, a polypeptide exhibiting higher activity for glutamic acid as an amino donor than that for L-alanine, and, having novel transaminase activity for generating (S)-1-benzyl-3-pyrrolidinone with high optical purity of 93% or more, a gene encoding the same, and a transformant expressing the gene at a high level are also provided herein.
摘要翻译：提供了一种从酮化合物廉价有效地制备用作药物制剂，农药等的中间体的旋光性氨基化合物的方法。具体而言，对于产生具有93％以上光学纯度的（S）-1-苄基-3-吡咯烷酮的新型转氨酶活性，作为氨基供体的谷氨酸比L-丙氨酸具有较高活性的多肽，本发明还提供了编码该基因的基因，以及高水平表达该基因的转化体。

9. 发明授权

US09481871B2 Nucleic acid encoding a polpeptide having aminotransferase activity, vectors and host cells comprising the nucleic acid 有权
标题翻译：编码具有氨基转移酶活性的多肽的核酸，载体和包含该核酸的宿主细胞
公开(公告)号：US09481871B2
公开(公告)日：2016-11-01
申请号：US13876412
申请日：2011-09-28
申请人： Noriyuki Ito , Akiko Nishi , Shigeru Kawano , Yoshihiko Yasohara
发明人： Noriyuki Ito , Akiko Nishi , Shigeru Kawano , Yoshihiko Yasohara
IPC分类号： C07H21/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N9/10 , C12P41/00 , C12P17/10
CPC分类号： C12N9/1096 , C12P17/10 , C12P41/006 , C12Y206/01 , Y02P20/52
摘要： A method for inexpensively and efficiently producing an optically active amino compound useful as an intermediate for pharmaceutical preparations, agricultural chemicals, or the like, from a ketone compound is provided. Specifically, a polypeptide exhibiting higher activity for glutamic acid as an amino donor than that for L-alanine, and, having novel transaminase activity for generating (S)-1-benzyl-3-pyrrolidinone with high optical purity of 93% or more, a gene encoding the same, and a transformant expressing the gene at a high level are also provided herein.
摘要翻译：提供了一种从酮化合物廉价有效地制备用作药物制剂，农药等的中间体的旋光性氨基化合物的方法。具体而言，对于产生具有93％以上光学纯度的（S）-1-苄基-3-吡咯烷酮的新型转氨酶活性，作为氨基供体的谷氨酸比L-丙氨酸具有较高活性的多肽，本发明还提供了编码该基因的基因，以及高水平表达该基因的转化体。

10. 发明授权

US09029113B2 Modified aminotransferase, gene thereof, and method for producing optically active amino compound using same 有权
标题翻译：修饰的氨基转移酶及其基因，以及使用其制备光学活性氨基化合物的方法
公开(公告)号：US09029113B2
公开(公告)日：2015-05-12
申请号：US14004293
申请日：2012-03-09
申请人： Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
发明人： Noriyuki Ito , Shigeru Kawano , Yoshihiko Yasohara
IPC分类号： C12N9/10 , C12P17/12 , C12P13/00 , C12P13/04 , C12P41/00
CPC分类号： C12N9/1096 , C12P13/001 , C12P13/04 , C12P41/006
摘要： Provided is a method for efficiently producing from a ketone compound an optically active amino compound useful as an intermediate of a drug, an agricultural chemical, or the like. Provided are: a polypeptide having aminotransferase activity that is increased in stereoselectivity, heat resistance, and resistance to amine compounds compared to the wild type enzyme by means of modifying an aminotransferase derived from Pseudomonas fluorescens; a gene encoding the polypeptide; and a transformant that expresses the gene at a high level.
摘要翻译：提供一种从酮化合物有效地制备用作药物，农药等的中间体的光学活性氨基化合物的方法。提供：通过修饰衍生自荧光假单胞菌的氨基转移酶，与野生型酶相比，具有增加立体选择性，耐热性和耐胺性化合物的氨基转移酶活性的多肽; 编码该多肽的基因; 以及高水平表达基因的转化体。

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