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1. 发明授权

US06335453B1 Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids 有权
标题翻译：制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰氨基酸的药理学可接受盐的方法
公开(公告)号：US06335453B1
公开(公告)日：2002-01-01
申请号：US09269107
申请日：1999-03-19
申请人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
发明人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
IPC分类号： C07K5062
CPC分类号： C07K5/0222 , C07K5/06026
摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
摘要翻译：提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，和形成其药理学上可接受的盐，其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

2. 发明授权

US06518436B2 Process for preparing pharmacologically acceptable salt of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效
标题翻译：制备正（（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法
公开(公告)号：US06518436B2
公开(公告)日：2003-02-11
申请号：US09989186
申请日：2001-11-21
申请人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
发明人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
IPC分类号： C07D20704
CPC分类号： C07K5/0222 , C07K5/06026
摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S) -ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxy-anhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
摘要翻译：提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，并形成其药学上可接受的盐，其中通过在含水液体中进行一系列操作直至形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

3. 发明授权

US06204393B1 Method for crystallizing maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline 失效
标题翻译： N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰-L-脯氨酸的马来酸盐结晶方法
公开(公告)号：US06204393B1
公开(公告)日：2001-03-20
申请号：US09508801
申请日：2000-03-17
申请人： Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07K5062
CPC分类号： C07K5/06026
摘要： A process for simply and easily crystallizing a maleate salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (enalapril) having a high quality out of an aqueous liquid, which comprises mixing an aqueous liquid having a pH of not less than 4 and containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, maleic acid and a base with an amount of an acid sufficient to convert substantially all the base into a neutral salt.
摘要翻译：一种从水性液体中简单且容易地结晶出具有高质量的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰-L-脯氨酸（依那普利）的马来酸盐的方法，其包括将含有不少于4的pH并含有N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰-L-脯氨酸，马来酸和碱的量的水溶液，其含量足以基本上转化所有的碱都成为中性盐。

4. 发明授权

US06713628B2 Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效
标题翻译：制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐的方法
公开(公告)号：US06713628B2
公开(公告)日：2004-03-30
申请号：US10295897
申请日：2002-11-18
申请人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
发明人： Yasuyoshi Ueda , Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse
IPC分类号： C07D20704
CPC分类号： C07K5/0222 , C07K5/06026
摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
摘要翻译：提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，和形成其药理学上可接受的盐，其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

5. 发明授权

US06359155B1 Process for the preparation of 3-hydroxytetrahydrofuran 失效
标题翻译： 3-羟基四氢呋喃的制备方法
公开(公告)号：US06359155B1
公开(公告)日：2002-03-19
申请号：US09719686
申请日：2001-02-15
申请人： Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Nobuo Nagashima , Yasuhiro Saka , Tatsuya Honda , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Koichi Kinoshita , Tadashi Moroshima , Yoshifumi Yanagida , Nobuo Nagashima , Yasuhiro Saka , Tatsuya Honda , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D30720
CPC分类号： C07C29/147 , C07B2200/07 , C07D307/20 , Y02P20/55 , C07C31/42
摘要： An industrial advantage process for producing high-purity 3-hydroxytetrahydrofuran easily and simply, which comprises reducing a 4-halo-3-hydroxybutyric acid ester (1) with a boron hydride compound and/or an aluminum hydride compound as a reducing agent in an organic solvent immiscible with water; treating the reaction mixture with an acid and water to thereby effect conversion to the corresponding 4-halo-1,3-butanediol and at the same time giving an aqueous solution containing said compound; carrying out the cyclization reaction of the 4-halo-1,3-butanediol in said aqueous solution; extracting the resulting 3-hydroxytetrahydrofuran from the 3-hydroxytetrahydrofuran-containing aqueous solution using an organic solvent immiscible with water; and isolating the 3-hydroxytetrahydrofuran by concentration and/or distillation of the solution obtained.
摘要翻译：用于容易且简单地生产高纯度3-羟基四氢呋喃的工业优势方法，其包括用硼氢化合物和/或氢化铝化合物作为还原剂还原4-卤代-3-羟基丁酸酯（1）与水不混溶的有机溶剂;用酸和水处理反应混合物，从而转化为相应的4-卤代-1,3-丁二醇，同时得到含有所述化合物的水溶液;进行环化反应所述水溶液中的4-卤代-1,3-丁二醇;使用与水不混溶的有机溶剂从含3-羟基四氢呋喃的水溶液中萃取所得3-羟基四氢呋喃; 通过所得溶液的浓缩和/或蒸馏来使3-羟基四氢呋喃分离。

6. 发明授权

US06271393B1 Process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline 有权
标题翻译：制备N2-（1（S） - 羧基-3-苯基丙基）-L-赖氨酰-L-脯氨酸的方法
公开(公告)号：US06271393B1
公开(公告)日：2001-08-07
申请号：US09554827
申请日：2000-07-17
申请人： Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Tadashi Moroshima , Yoshifumi Yanagida , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D20706
CPC分类号： C07K5/0222
摘要： The process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline in a simple, efficient and industrially advantageous manner, including the following steps: 1) subjecting N2-(1(S)-alkoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysyl-L-proline (1) to alkali hydrolysis in a mixed solution composed of water and a hydrophilic organic solvent using an inorganic base in an amount of n molar equivalents (n ≧ 3) per mole of the above compound (1), 2) neutralizing the hydrolysis product using an inorganic acid in an amount of (n − 1) to n molar equivalents (n ≧ 3) to form a compound (2) and removing the inorganic salt formed by causing the same to precipitate out from a solvent system suited for decreasing the solubility of the inorganic salt, and 3) causing the compound (2) existing in the mixture after removal of the inorganic salt to crystallize out at the isoelectric point thereof and thereby recovering the compound (2) in the form of crystals while retaining the salts including the trifluoroacetic acid-derived organic acid salt in a state dissolved in the mother liquor.
摘要翻译：包括以下步骤制备N2-（1（S） - 羧基-3-苯基丙基）-L-赖氨酰-L-脯氨酸的方法，包括以下步骤：1）使N2-（1（S ） - 烷氧基羰基-3-苯基丙基）-N6-三氟乙酰基-L-赖氨酰-L-脯氨酸（1）在由水和亲水性有机溶剂组成的混合溶液中使用n摩尔当量的无机碱进行碱水解（ n）= 3），2）使用（n-1）〜n摩尔当量（n> = 3）的无机酸中和水解产物，形成化合物（2）），并且通过使其从适合于降低无机盐的溶解度的溶剂体系中析出而形成的无机盐，以及3）除去无机盐以使其结晶出来，使存在于混合物中的化合物（2）结晶出来其等电点，从而以晶体的形式回收化合物（2），同时保留盐将三氟乙酸衍生的有机酸盐以溶解在母液中的状态。

7. 发明授权

US06720449B2 Process for preparing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US06720449B2
公开(公告)日：2004-04-13
申请号：US09926346
申请日：2002-02-05
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D20308
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性N-保护的氮丙啶-2-羧酸衍生物，在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，天然和非天然旋光氨基酸可以是通过简单的程序从便宜的材料生产。

8. 发明授权

US07109352B2 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US07109352B2
公开(公告)日：2006-09-19
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D203/02 , C07D203/08
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物是通过N-保护光学活性3-卤代丙氨酸衍生物进行环化，或环化该衍生物进行N-保护而得到光学活性N-保护的氮丙啶-2-羧酸衍生物在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

9. 发明申请

US20050143586A1 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US20050143586A1
公开(公告)日：2005-06-30
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24 , C07D203/16
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性N-保护的氮丙啶-2-羧酸衍生物，在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

10. 发明申请

US20100016634A1 METHOD FOR STABILIZING CARBODIIMIDE DERIVATIVE AND STABILIZED COMPOSITION THEREOF 审中-公开
标题翻译：用于稳定碳二亚胺衍生物和稳定化合物的方法
公开(公告)号：US20100016634A1
公开(公告)日：2010-01-21
申请号：US12439005
申请日：2007-08-30
申请人： Kunihiko Seno , Masao Okuda , Hiroaki Kawasaki , Tadashi Moroshima , Yasuyoshi Ueda
发明人： Kunihiko Seno , Masao Okuda , Hiroaki Kawasaki , Tadashi Moroshima , Yasuyoshi Ueda
IPC分类号： C07C267/00
CPC分类号： C07C267/00
摘要： Disclosed is a method for stabilizing a carbodiimide derivative (1) which is a condensing agent useful for production of general synthetic chemical products. Also disclosed is a stabilized composition of the carbodiimide derivative. The method is characterized in that the carbodiimide derivative (1) is handled in an atmosphere wherein the concentration of molecular oxygen in the gas phase within a container is set at not more than 3% by volume and/or in the co-presence of at least one compound selected from the group consisting of antioxidants, N-oxyl compounds, sulfur compounds, amines and Lewis acids.
摘要翻译：公开了一种稳定碳二亚胺衍生物（1）的方法，碳二亚胺衍生物（1）是可用于生产一般合成化学产品的缩合剂。还公开了碳二亚胺衍生物的稳定化组合物。该方法的特征在于，将碳二亚胺衍生物（1）在容器内气相中的分子氧浓度设定为3体积％以下和/或共存于选自抗氧化剂，N-氧基化合物，硫化合物，胺和路易斯酸的至少一种化合物。

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