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1. 发明申请

US20060166342A1 Process for producing optically active 3-hydroxypropionic ester derivative 有权
标题翻译：光学活性3-羟基丙酸酯衍生物的制备方法
公开(公告)号：US20060166342A1
公开(公告)日：2006-07-27
申请号：US10536768
申请日：2003-12-08
申请人： Naoaki Taoka , Daisuke Moriyama , Kohei Mori , Takahiro Oishi
发明人： Naoaki Taoka , Daisuke Moriyama , Kohei Mori , Takahiro Oishi
IPC分类号： C12P7/62
CPC分类号： C12P7/62 , C07C67/313 , C07D317/60 , C12P17/04 , C12P41/002 , C07C69/716
摘要： The present invention is to provide a process for simply producing an optically active 3-hydroxypropionic ester derivative useful as a medicament intermediate from an inexpensive material. More specifically, the present invention is directed to a process for producing an optically active 3-hydroxypropionic ester derivative comprising reacting an acetic ester derivative available at low cost with abase and a formic ester, thereby converting the acetic ester derivative into a 2-formylacetic ester derivative, and thereafter, stereospecifically reducing the formyl group of the derivative by use of an enzymatic source capable of stereoselectively reducing the formyl group of the derivative.
摘要翻译：本发明提供一种简单地制造用作廉价材料的药物中间体的光学活性3-羟基丙酸酯衍生物的方法。更具体地说，本发明涉及一种光学活性3-羟基丙酸酯衍生物的制备方法，其包括将低成本获得的乙酸酯衍生物与甲酸酯反应，由此将乙酸酯衍生物转化为2-甲酰基乙酸酯衍生物，然后通过使用能够立体选择性还原衍生物的甲酰基的酶源立体选择性还原衍生物的甲酰基。

2. 发明授权

US07666659B2 Process for producing optically active 3-hydroxypropionic ester derivative 有权
标题翻译：光学活性3-羟基丙酸酯衍生物的制备方法
公开(公告)号：US07666659B2
公开(公告)日：2010-02-23
申请号：US10536768
申请日：2003-12-08
申请人： Naoaki Taoka , Daisuke Moriyama , Kohei Mori , Takahiro Oishi
发明人： Naoaki Taoka , Daisuke Moriyama , Kohei Mori , Takahiro Oishi
IPC分类号： C12P41/00
CPC分类号： C12P7/62 , C07C67/313 , C07D317/60 , C12P17/04 , C12P41/002 , C07C69/716
摘要： The present invention is to provide a process for simply producing an optically active 3-hydroxypropionic ester derivative useful as a medicament intermediate from an inexpensive material. More specifically, the present invention is directed to a process for producing an optically active 3-hydroxypropionic ester derivative comprising reacting an acetic ester derivative available at low cost with a base and a formic ester, thereby converting the acetic ester derivative into a 2-formylacetic ester derivative, and thereafter, stereospecifically reducing the formyl group of the derivative by use of an enzymatic source capable of stereoselectively reducing the formyl group of the derivative.
摘要翻译：本发明提供一种简单地制造用作廉价材料的药物中间体的光学活性3-羟基丙酸酯衍生物的方法。更具体地，本发明涉及一种光学活性3-羟基丙酸酯衍生物的制备方法，其包括使低成本获得的乙酸酯衍生物与碱和甲酸酯反应，从而将乙酸酯衍生物转化为2-甲酰基乙酸酯衍生物，然后使用能够立体选择性还原衍生物的甲酰基的酶源，立体选择性还原衍生物的甲酰基。

3. 发明申请

US20100048909A1 Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof 有权
公开(公告)号：US20100048909A1
公开(公告)日：2010-02-25
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： C07D263/12 , C07D303/38 , C07C237/06
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.

4. 发明授权

US07834190B2 Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof 有权
标题翻译：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。

5. 发明授权

US08338142B2 Method for producing optically active 3-aminopiperidine or salt thereof 有权
标题翻译：光学活性3-氨基哌啶或其盐的制备方法
公开(公告)号：US08338142B2
公开(公告)日：2012-12-25
申请号：US12449645
申请日：2008-02-18
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： C12P17/12
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。

6. 发明申请

US20100105917A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF 有权
标题翻译：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：US20100105917A1
公开(公告)日：2010-04-29
申请号：US12449645
申请日：2008-02-18
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： C07D211/98 , C12P17/12 , C07D211/60
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。

7. 发明申请

US20060105435A1 Process for producing optically active alpha-methylcysteine derivative 审中-公开
标题翻译：光学活性α-甲基半胱氨酸衍生物的制备方法
公开(公告)号：US20060105435A1
公开(公告)日：2006-05-18
申请号：US10515658
申请日：2003-06-05
申请人： Takahiro Ohishi , Hirokazu Nanba , Masanobu Sugawara , Masashi Izumida , Tatsuya Honda , Kohei Mori , Satohiro Yanagisawa , Nobuo Nagashima , Kenji Inoue
发明人： Takahiro Ohishi , Hirokazu Nanba , Masanobu Sugawara , Masashi Izumida , Tatsuya Honda , Kohei Mori , Satohiro Yanagisawa , Nobuo Nagashima , Kenji Inoue
IPC分类号： C12P13/12 , C12P17/00
CPC分类号： C12P13/12 , C07C319/06 , C07D233/76 , C12P17/04 , C12P17/10 , C12P41/009 , C07C323/58
摘要： The present invention provides a simple industrial process for producing an L- or D-optically active α-methylcysteine derivative or its salt, which is a useful pharmaceutical intermediate, from readily available, inexpensive raw materials. In a process for producing an L- or D-optically active α-methylcysteine derivative or its salt, a racemic N-carbamoyl-α-methylcysteine derivative or its salt is D-selectively cyclized with hydantoinase to produce a D-5-methyl-5-thiomethylhydantoin derivative or its salt and an N-carbamoyl-α-methyl-L-cysteine derivative or its salt, which are then subjected to deprotection of the amino group and the sulfur atom, and hydrolysis.
摘要翻译：本发明提供了一种用于从容易得到的廉价原料生产L-或D-光学活性α-甲基半胱氨酸衍生物或其盐的简单工业方法，其是有用的药物中间体。在制备L-或D-光学活性α-甲基半胱氨酸衍生物或其盐的方法中，外消旋的N-氨基甲酰基-α-甲基半胱氨酸衍生物或其盐与乙内酰脲酶D选择性环化以产生D-5-甲基 - 5-硫代甲基乙内酰脲衍生物或其盐和N-氨基甲酰基-α-甲基-L-半胱氨酸衍生物或其盐，然后对氨基和硫原子进行脱保护和水解。

8. 发明申请

US20060044200A1 Multibeam antenna 失效
标题翻译：多波束天线
公开(公告)号：US20060044200A1
公开(公告)日：2006-03-02
申请号：US11201424
申请日：2005-08-11
申请人： Kohei Mori
发明人： Kohei Mori
IPC分类号： H01Q13/10
CPC分类号： H01Q13/10 , H01Q19/30
摘要： The present invention has been made to reduce the size and thickness of a multibeam antenna capable of switching the directivity in multi directions. The present invention provides a multibeam antenna including an antenna element array including one or more feed element and N (N: natural number) parasitic elements, wherein the electrical length of one or more parasitic elements are made variable.
摘要翻译：本发明是为了减小能够切换多方向性的多波束天线的尺寸和厚度。本发明提供一种多波束天线，其包括天线元件阵列，其包括一个或多个馈电元件和N（N：自然数）寄生元件，其中一个或多个寄生元件的电长度可变。

9. 发明授权

US5187934A Tandem type master cylinder 失效
标题翻译：串联式主缸
公开(公告)号：US5187934A
公开(公告)日：1993-02-23
申请号：US758882
申请日：1991-09-11
申请人： Kohei Mori
发明人： Kohei Mori
IPC分类号： B60T11/20 , B60T11/236 , F16J15/18
CPC分类号： F16J15/183 , B60T11/20 , B60T11/236
摘要： A tandem type master cylinder is disclosed having a housing with a through-bore defining an intermediate portion and opposed end portions. The diameter of each end portion is larger than the diameter of the intermediate portion, and the junctures between the end portions and the intermediate portion define step parts within the housing. Seal assemblies are positioned within the housing at the step junctures formed by the intermediate portion and the end portions and are retained in position by a plug secured within each end portion. Primary and Secondary pistons are disposed for guided movement along the intermediate portion of the housing, and return springs are provided within the housing for urging each piston to its initial rest position.
摘要翻译：公开了一种串联式主缸，具有具有限定中间部分和相对端部的通孔的壳体。每个端部的直径大于中间部分的直径，并且端部和中间部分之间的接合部限定了壳体内的台阶部分。密封组件在由中间部分和端部形成的台阶接合处定位在壳体内，并且通过固定在每个端部内的插塞保持就位。主活塞和次级活塞设置成沿着壳体的中间部分引导运动，并且复位弹簧设置在壳体内，用于将每个活塞推到其初始静止位置。

10. 发明授权

US4989498A Hydraulic actuator 失效
标题翻译：液压执行机构
公开(公告)号：US4989498A
公开(公告)日：1991-02-05
申请号：US374971
申请日：1989-07-03
申请人： Kohei Mori , Noboru Sekiguchi
发明人： Kohei Mori , Noboru Sekiguchi
IPC分类号： F15B15/14 , B60T11/20 , B60T11/22 , B60T11/236 , F16J15/32
CPC分类号： F16J15/3236 , B60T11/20 , B60T11/22 , B60T11/236 , F16J15/3248
摘要： Improvement in an annular seal for use in a hydraulic actuator is obtained in accordance with the present invention, which annular seal is of the type including fitting holes to be inserted by projections formed in a piston guide and is adapted to be mounted between a piston guide sleeve and the piston guide, by the provision of annular projections extending in an annular shape and in the axial direction of the seal in the inner and outer circumferential portions with respect to the location of the fitting holes or in the circumferential area of the piston guide corresponding to that circumferential portions.
摘要翻译：根据本发明获得了用于液压致动器的环形密封件的改进，该环形密封件是包括形成在活塞导向件中的突起插入的装配孔，并且适于安装在活塞导向件套筒和活塞引导件，通过设置环形突起，其相对于装配孔的位置或活塞导向件的周向区域在内周和外周部分沿环形形状和轴向方向延伸对应于该周向部分。

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