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1. 发明授权

US09181217B2 Method for producing optically active naphthalene compound 有权
标题翻译：光学活性萘化合物的制造方法
公开(公告)号：US09181217B2
公开(公告)日：2015-11-10
申请号：US14240466
申请日：2012-08-24
申请人： Koji Matsuyama , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Koichi Tanimoto
发明人： Koji Matsuyama , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Koichi Tanimoto
IPC分类号： C07B53/00 , C07C25/06 , C07C255/03 , C07D401/04
CPC分类号： C07D401/04 , C07B53/00 , C07C25/06 , C07C255/03
摘要： The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.).
摘要翻译：本发明提供了用于制造用作皮炎等的治疗剂的光学活性萘化合物的工业上有利的方法。具体而言，本发明提供了一种光学活性萘化合物[I]的制造方法，其特征在于，在碱的存在下，使化合物[a-1]和化合物[b-1] 和由Pd化合物和叔膦配体组成的催化剂（步骤a）; 在氢供体和由钌化合物和手性配体制备的络合物的存在下，或者在光学活性的恶唑硼烷化合物（CBS催化剂）存在下，不对称地氢化化合物[c-1] 和硼氢化合物（步骤b）; 和用还原剂处理化合物[d-1]（步骤c）的步骤。（上述式中，Ra和Rb表示相同或不同的低级烷基，X1表示卤素原子。

2. 发明申请

US20150152082A1 METHOD FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE COMPOUND 有权
标题翻译：用于生产光学活性萘基化合物的方法
公开(公告)号：US20150152082A1
公开(公告)日：2015-06-04
申请号：US14240466
申请日：2012-08-24
申请人： Koji Matsuyama , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Koichi Tanimoto
发明人： Koji Matsuyama , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Koichi Tanimoto
IPC分类号： C07D401/04 , C07C255/03 , C07C25/06
CPC分类号： C07D401/04 , C07B53/00 , C07C25/06 , C07C255/03
摘要： The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.)
摘要翻译：本发明提供了用于制造用作皮炎等的治疗剂的光学活性萘化合物的工业上有利的方法。具体而言，本发明提供了一种光学活性萘化合物[I]的制造方法，其特征在于，在碱的存在下，使化合物[a-1]和化合物[b-1] 和由Pd化合物和叔膦配体组成的催化剂（步骤a）; 在氢供体和由钌化合物和手性配体制备的络合物的存在下，或者在光学活性的恶唑硼烷化合物（CBS催化剂）存在下，不对称地氢化化合物[c-1] 和硼氢化合物（步骤b）; 和用还原剂处理化合物[d-1]（步骤c）的步骤。（上式中，Ra和Rb表示相同或不同的低级烷基，X1表示卤素原子。）

3. 发明授权

US09056850B2 Process for the preparation of compounds useful as inhibitors of SGLT 有权
公开(公告)号：US09056850B2
公开(公告)日：2015-06-16
申请号：US12578934
申请日：2009-10-14
申请人： Walter Ferdinand Maria Filliers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Christopher Teleha
发明人： Walter Ferdinand Maria Filliers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Christopher Teleha
IPC分类号： C07D409/04 , C07D333/12 , C07D409/10
CPC分类号： C07D333/12 , C07D409/10 , C07H7/04 , C07H13/04
摘要： The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

4. 发明申请

US20100099883A1 PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT 有权
标题翻译：制备作为SGLT抑制剂的化合物的方法
公开(公告)号：US20100099883A1
公开(公告)日：2010-04-22
申请号：US12578934
申请日：2009-10-14
申请人： Walter Ferdinand Maria Fillers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada
发明人： Walter Ferdinand Maria Fillers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada
IPC分类号： C07D409/04 , C07D409/10 , C07D333/12
CPC分类号： C07D333/12 , C07D409/10 , C07H7/04 , C07H13/04
摘要： The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
摘要翻译：本发明涉及一种制备具有抑制活性的化合物的新方法，所述化合物对存在于肠或肾中的钠依赖性葡萄糖转运蛋白（SGLT）具有抑制活性。

5. 发明申请

US20050038260A1 Intermediate for biotin and process for producing the same 失效
标题翻译：生物素的中间体及其制备方法
公开(公告)号：US20050038260A1
公开(公告)日：2005-02-17
申请号：US10496660
申请日：2002-12-04
申请人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
发明人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
IPC分类号： C07D233/32 , C07D277/14 , C07D495/04 , C07F3/02 , C07F3/06 , C07D498/02
CPC分类号： C07F3/06 , C07D233/34 , C07D495/04 , C07F3/02
摘要： The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
摘要翻译：本发明提供一种制备在工业上有利的生物素的合成中间体的方法，并公开了由式（I）表示的化合物的制备方法：其中R 1和R 2可以相同或彼此不同，并且各自表示氢原子，苯环上可具有取代基的苄基，可在苯环上具有取代基的二苯甲基或三苯甲基在苯环上具有取代基，R 3表示氰基，羧基，烷氧基羰基，烷硫基羰基或可具有取代基的氨基甲酰基，或其盐，其包括使式通过式（II-a）表示：其中符号具有与上述相同的含义或其盐进行环转化。

6. 发明授权

US07439368B2 Process for producing 3-acylaminobenzofuran-2-carboxylic acid derivative 失效
标题翻译： 3-酰氨基苯并呋喃-2-羧酸衍生物的制备方法
公开(公告)号：US07439368B2
公开(公告)日：2008-10-21
申请号：US10561180
申请日：2004-06-29
申请人： Masahiko Seki , Shin-ichi Yoshida , Nobuhiro Yagi , Masanori Hatsuda , Mayumi Kimura , Kazuhiko Kondo
发明人： Masahiko Seki , Shin-ichi Yoshida , Nobuhiro Yagi , Masanori Hatsuda , Mayumi Kimura , Kazuhiko Kondo
IPC分类号： C07D405/14 , C07D405/12
CPC分类号： C07D405/14 , C07C253/14 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/85 , C07D265/32 , C07D295/192 , C07D333/62 , C07D333/68 , C07D405/12 , C07C255/50 , C07C255/51 , C07C255/53 , C07C255/54 , C07C255/56 , C07C255/57
摘要： The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: —N═ or —CH═; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of activated blood coagulation factor X.
摘要翻译：本发明提供制备式[I]化合物的方法：其中X是下式的基团：-N-或-CH-; R 1是氢原子，卤素原子，低级烷基，低级烷氧基，氰基或任选被低级烷基取代的氨基; 环A是含氮杂环基; 环B是任选取代的苯环或任选取代的吡啶环; R 3是氢原子或低级烷基或其药学上可接受的盐，其可用作活化凝血因子X的抑制剂。

7. 发明申请

US20060173188A1 Process for producing 3-acylaminobenzofuran-2-carboxylic acid derivative 失效
标题翻译： 3-酰氨基苯并呋喃-2-羧酸衍生物的制备方法
公开(公告)号：US20060173188A1
公开(公告)日：2006-08-03
申请号：US10561180
申请日：2004-06-29
申请人： Masahiko Seki , Shin-chi Yoshida , Nobuhiro Yagi , Masanori Hatsuda
发明人： Masahiko Seki , Shin-chi Yoshida , Nobuhiro Yagi , Masanori Hatsuda
IPC分类号： C07D405/14 , C07D405/02 , C07D307/87
CPC分类号： C07D405/14 , C07C253/14 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/85 , C07D265/32 , C07D295/192 , C07D333/62 , C07D333/68 , C07D405/12 , C07C255/50 , C07C255/51 , C07C255/53 , C07C255/54 , C07C255/56 , C07C255/57
摘要： The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: —N═ or —CH═; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of activated blood coagulation factor X.
摘要翻译：本发明提供制备式[I]化合物的方法：其中X是下式的基团：-N-或-CH-; R 1是氢原子，卤素原子，低级烷基，低级烷氧基，氰基或任选被低级烷基取代的氨基; 环A是含氮杂环基; 环B是任选取代的苯环或任选取代的吡啶环; R 3是氢原子或低级烷基或其药学上可接受的盐，其可用作活化凝血因子X的抑制剂。

8. 发明授权

US07799929B2 Biotin intermediate and process for preparing the same 有权
标题翻译：生物素中间体及其制备方法
公开(公告)号：US07799929B2
公开(公告)日：2010-09-21
申请号：US12007118
申请日：2008-01-07
申请人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
发明人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
IPC分类号： C07D235/00 , C07D233/34 , C07D233/28
CPC分类号： C07F3/06 , C07D233/34 , C07D495/04 , C07F3/02
摘要： The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): 1 wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): 2 wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
摘要翻译：本发明提供一种制备在工业上有利的生物素的合成中间体的方法，并公开了制备由式（I）表示的化合物的方法：其中R1和R2可以相同或不同，各自表示氢原子，苯环上可具有取代基的苄基，可在苯环上具有取代基的二苯甲基或可具有取代基的三苯甲基（s ），R3表示氰基，羧基，烷氧基羰基，烷硫基羰基或可具有取代基的氨基甲酰基，或其盐，其包括使由式（II-a）表示的化合物 2，其中符号具有与上述相同的含义或其盐进行环转化。

9. 发明申请

US20080119655A1 Biotin intermediate and process for preparing the same 有权
标题翻译：生物素中间体及其制备方法
公开(公告)号：US20080119655A1
公开(公告)日：2008-05-22
申请号：US12007118
申请日：2008-01-07
申请人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
发明人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
IPC分类号： C07D277/04 , C07D235/00
CPC分类号： C07F3/06 , C07D233/34 , C07D495/04 , C07F3/02
摘要： The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): 1 wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): 2 wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
摘要翻译：本发明提供一种制备在工业上有利的生物素的合成中间体的方法，并公开了由式（I）表示的化合物的制备方法：其中R 1和R 2， SUP> 2可以相同或不同，各自表示氢原子，苯环上可以具有取代基的苄基，可具有取代基的二苯甲基，或在苯环上可具有取代基的三苯甲基，R 3表示氰基，羧基，烷氧基羰基，烷硫基羰基或氨基甲酰基其可以具有取代基，或其盐，其包括使由式（II-a）表示的化合物：其中符号具有与上述相同的含义，或其盐进行环转化。

10. 发明授权

US07335778B2 Intermediate for biotin and process for producing the same 失效
标题翻译：生物素的中间体及其制备方法
公开(公告)号：US07335778B2
公开(公告)日：2008-02-26
申请号：US10496660
申请日：2002-12-04
申请人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
发明人： Masahiko Seki , Toshiaki Shimizu , Shin-ichi Yoshida , Masanori Hatsuda
IPC分类号： C07D233/20 , C07D277/10
CPC分类号： C07F3/06 , C07D233/34 , C07D495/04 , C07F3/02
摘要： The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
摘要翻译：本发明提供一种制备在工业上有利的生物素的合成中间体的方法，并公开了制备由式（I）表示的化合物的方法：其中R 1和R 2 > 2个彼此可以相同或不同，并且各自表示氢原子，苯环上可具有取代基的苄基，可以具有取代基的二苯甲基苯环或在苯环上可具有取代基的三苯甲基，R 3表示氰基，羧基，烷氧基羰基，烷硫基羰基或氨基甲酰基，其中可以具有取代基或其盐，其包括使由式（II-a）表示的化合物：其中符号具有与上述相同的含义或其盐进行环转化。

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