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1. 发明授权

US08058432B2 Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of derivatives 有权
标题翻译：制备具有喹唑啉二酮骨架的苯丙氨酸衍生物的方法和用于制备衍生物的中间体
公开(公告)号：US08058432B2
公开(公告)日：2011-11-15
申请号：US12470846
申请日：2009-05-22
申请人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
发明人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
IPC分类号： C07D239/96
CPC分类号： C07D239/96 , C07C233/47 , C07C233/87 , C07C237/40 , C07C237/42 , C07C265/12 , C07C271/22 , C07C271/28 , C07C275/42 , Y02P20/55
摘要： The present invention releates to a method for preparing a phenylalanine compound having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof: where R1-R4 are defined herein. The method involves reacting a specified acyl phenylalanine compound with a carbonyl group-introducing reagent and a specified anthranilic acid compound to form a carboxy-asymmetric urea compound which is converted to a quinazoline-dione compound in the presence of a carboxyl group-activating agent.
摘要翻译：本发明涉及制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸化合物或其药学上可接受的盐的方法：其中R1-R4如本文所定义。该方法包括使特定的酰基苯丙氨酸化合物与羰基引入试剂和特定的邻氨基苯甲酸化合物反应，形成羧基不对称脲化合物，其在羧基活化剂存在下转化为喹唑啉二酮化合物。

2. 发明授权

US08546610B2 Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives 有权
标题翻译：制备具有喹唑啉二酮骨架的苯丙氨酸衍生物的方法和用于制备衍生物的中间体
公开(公告)号：US08546610B2
公开(公告)日：2013-10-01
申请号：US13218946
申请日：2011-08-26
申请人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
发明人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
IPC分类号： C07C229/56
CPC分类号： C07D239/96 , C07C233/47 , C07C233/87 , C07C237/40 , C07C237/42 , C07C265/12 , C07C271/22 , C07C271/28 , C07C275/42 , Y02P20/55
摘要： A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3′ which is a group corresponding to R3 is protected. According to this method, there can be obtained a phenylalanine derivative having a quinazoline-dione skeleton in a industrially favorably high yield.
摘要翻译：一种制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸衍生物或其药学上可接受的盐的方法，包括以下步骤（a），（b）和（c）：（a）使酰基由下式（2）表示的苯丙氨酸衍生物：具有羰基导入试剂和特定的邻氨基苯甲酸衍生物，从而形成相应的羧基不对称脲衍生物; （b）在羧基活化剂存在下将羧基不对称脲衍生物转化为相应的喹唑啉二酮衍生物：（c）如果需要，用N-烷基取代与氮原子键合的氢原子存在在使用N-烷基化试剂的喹唑啉二酮衍生物的喹唑啉二酮环中，然后当对应于R3的基团的取代基R3'被保护时，使得到的产物脱保护。根据该方法，可以得到具有喹唑啉二酮骨架的苯丙氨酸衍生物，工业上有利地高产率。

3. 发明申请

US20080108634A1 NOVEL PHENYLALANINE DERIVATIVES 有权
标题翻译：新型苯乙烯胺衍生物
公开(公告)号：US20080108634A1
公开(公告)日：2008-05-08
申请号：US11963144
申请日：2007-12-21
申请人： Kazuyuki SAGI , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
发明人： Kazuyuki SAGI , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
IPC分类号： A61K31/517 , A61P29/00
CPC分类号： C07D239/70 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/96 , C07D401/12 , C07D401/14 , C07D403/04 , C07D471/04 , C07D487/04
摘要： Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译：具体的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。它们被用作关于α4整联蛋白的各种疾病的治疗剂。

4. 发明授权

US07345049B2 Phenylalanine derivatives 有权
标题翻译：苯丙氨酸衍生物
公开(公告)号：US07345049B2
公开(公告)日：2008-03-18
申请号：US11018226
申请日：2004-12-22
申请人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
发明人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
IPC分类号： A61K31/517 , A61K31/519 , C07D239/70 , C07D239/95
CPC分类号： C07D239/70 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/96 , C07D401/12 , C07D401/14 , C07D403/04 , C07D471/04 , C07D487/04
摘要： Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译：具体的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。它们被用作关于α4整联蛋白的各种疾病的治疗剂。

5. 发明授权

US08309561B2 Phenylalanine derivatives 有权
标题翻译：苯丙氨酸衍生物
公开(公告)号：US08309561B2
公开(公告)日：2012-11-13
申请号：US11963144
申请日：2007-12-21
申请人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
发明人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
IPC分类号： A61K31/517 , A61K31/519 , C07D239/70 , C07D239/95
CPC分类号： C07D239/70 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/96 , C07D401/12 , C07D401/14 , C07D403/04 , C07D471/04 , C07D487/04
摘要： Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译：特定的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。它们被用作关于α4整联蛋白的各种疾病的治疗剂。

6. 发明申请

US20050222141A1 Novel phenylalanine derivatives 有权
标题翻译：新型苯丙氨酸衍生物
公开(公告)号：US20050222141A1
公开(公告)日：2005-10-06
申请号：US11018226
申请日：2004-12-22
申请人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
发明人： Kazuyuki Sagi , Tatsuya Okuzumi , Tatsuhiro Yamada , Shunsuke Kageyama , Yoichiro Shima , Tadakiyo Nakagawa , Munetaka Tokumasu , Masayuki Sugiki , Hajime Ito , Itsuya Tanabe , Tamotsu Suzuki , Akira Nakayama , Kazuyuki Ubukata , Kenji Shinkai , Yasuhiro Tanaka , Misato Noguchi , Ayatoshi Andou , Yoriko Yamamoto , Noriyasu Kataoka , Koichi Fujita
IPC分类号： A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/541 , C07D239/70 , C07D239/96 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/02 , C07D417/02 , C07D471/04 , C07D487/04 , C07D43/02
CPC分类号： C07D239/70 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/96 , C07D401/12 , C07D401/14 , C07D403/04 , C07D471/04 , C07D487/04
摘要： Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译：具体的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。它们被用作关于α4整联蛋白的各种疾病的治疗剂。

7. 发明授权

US08268844B2 Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-l-phenylalanine hydrochloride, production method thereof and use thereof 有权
标题翻译： N-（2,6-二氯苯甲酰基）-4- [6-（甲基氨基）甲基-1-甲基-2,4-二氧代-1,4-二氢喹唑啉-3（2H） - 基] -1的异丙酯的晶体苯丙氨酸盐酸盐，其制备方法和用途
公开(公告)号：US08268844B2
公开(公告)日：2012-09-18
申请号：US12885936
申请日：2010-09-20
申请人： Koichi Fujita , Shinichiro Takahashi , Tatsuya Okuzumi , Tatsuhiro Yamada , Kotaro Okado , Noriyasu Kataoka , Haruko Hirashima , Hideyuki Yamaguchi
发明人： Koichi Fujita , Shinichiro Takahashi , Tatsuya Okuzumi , Tatsuhiro Yamada , Kotaro Okado , Noriyasu Kataoka , Haruko Hirashima , Hideyuki Yamaguchi
IPC分类号： A61K31/517
CPC分类号： C07D239/96
摘要： Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride: are useful as α4 integrin inhibitors.
摘要翻译： N-（2,6-二氯苯甲酰基）-4- [6-（甲基氨基）甲基-1-甲基-2,4-二氧代-1,4-二氢喹唑啉-3（2H） - 基] -L-异丙基酯的晶体苯丙氨酸盐酸盐：可用作α4整联蛋白抑制剂。

8. 发明授权

US07842700B2 Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride, production method thereof and use thereof 有权
标题翻译： N-（2,6-二氯苯甲酰基）-4- [6-（甲基氨基）甲基-1-甲基-2,4-二氧代-1,4-二氢喹唑啉-3（2H） - 基] -L- 苯丙氨酸盐酸盐，其制备方法和用途
公开(公告)号：US07842700B2
公开(公告)日：2010-11-30
申请号：US11963192
申请日：2007-12-21
申请人： Koichi Fujita , Shinichiro Takahashi , Tatsuya Okuzumi , Tatsuhiro Yamada , Kotaro Okado , Noriyasu Kataoka , Haruko Hirashima , Hideyuki Yamaguchi
发明人： Koichi Fujita , Shinichiro Takahashi , Tatsuya Okuzumi , Tatsuhiro Yamada , Kotaro Okado , Noriyasu Kataoka , Haruko Hirashima , Hideyuki Yamaguchi
IPC分类号： A61K31/517
CPC分类号： C07D239/96
摘要： Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as α4 integrin inhibitors.
摘要翻译： N-（2,6-二氯苯甲酰基）-4- [6-（甲基氨基）甲基-1-甲基-2,4-二氧代-1,4-二氢喹唑啉-3（2H） - 基] -L- 苯丙氨酸盐酸盐可用作α4整联蛋白抑制剂。

9. 发明申请

US20090018161A1 METHOD FOR PROMOTING GASTROINTESTINAL FUNCTION AND METHOD FOR SCREENING FOR PROMOTER OF GASTROINTESTINAL FUNCTION 审中-公开
标题翻译：促进胃肠功能的方法和筛查胃肠功能促进剂的方法
公开(公告)号：US20090018161A1
公开(公告)日：2009-01-15
申请号：US12114125
申请日：2008-05-02
申请人： Tatsuro Tanaka , Hisayuki Uneyama , Shinichi Fujita , Saori Ogawa , Yusuke Amino , Seiji Shiraishi , Koichi Fujita , Tatsuhiro Yamada , Takashi Yamamoto , Takeshi Aihara , Manabu Suzuki
发明人： Tatsuro Tanaka , Hisayuki Uneyama , Shinichi Fujita , Saori Ogawa , Yusuke Amino , Seiji Shiraishi , Koichi Fujita , Tatsuhiro Yamada , Takashi Yamamoto , Takeshi Aihara , Manabu Suzuki
IPC分类号： A61K31/47 , A61K31/16 , A61K31/164 , A61K31/343 , A61K31/4439 , G01N33/53 , A61P1/00 , C12Q1/02 , A61K31/221 , A61K31/357 , A61K31/44
CPC分类号： A61K31/36 , A23L33/10 , A61K31/165 , A61K31/166 , A61K31/343
摘要： The present invention provides a more effective gastrointestinal function promoter. The present invention also provides a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like. The present invention also provides a method for screening for a substance capable of promoting a gastrointestinal function. The present invention provides a gastrointestinal function promoter containing a T1R agonist as an active ingredient and a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like by administering a T1R agonist. The present invention also provides a method of screening for a substance capable of promoting a gastrointestinal function which method uses a cell expressing T1R receptor.
摘要翻译：本发明提供了更有效的胃肠功能促进剂。本发明还提供了预防或改善功能性胃肠道疾病的方法，食欲调节方法等。本发明还提供了筛选能够促进胃肠功能的物质的方法。本发明提供了含有T1R激动剂作为活性成分的胃肠功能促进剂和通过施用T1R激动剂来预防或改善功能性胃肠道疾病的方法，食欲调节方法等。本发明还提供一种筛选能够促进胃肠功能的方法，该方法使用表达T1R受体的细胞。

10. 发明授权

US08907424B2 Protection diode 有权
标题翻译：保护二极管
公开(公告)号：US08907424B2
公开(公告)日：2014-12-09
申请号：US13739042
申请日：2013-01-11
申请人： Koichi Fujita
发明人： Koichi Fujita
IPC分类号： H01L23/62 , H01L27/02
CPC分类号： H01L29/7808 , H01L27/0248 , H01L27/0255
摘要： A protection diode includes: a semiconductor substrate; a well region of a first conductivity type in the semiconductor substrate; a gate side diffusion region of a second conductivity type in the semiconductor substrate and joined to the well region; a grounding side diffusion region of the second conductivity type in the semiconductor substrate, separated from the gate side diffusion region, and joined to the well region; a gate side electrode connected between a gate of a transistor and the gate side diffusion region; and a grounding electrode connected to the grounding side diffusion region. Dopant impurity concentration in the grounding side diffusion region is lower than dopant impurity concentration in the gate side diffusion region.
摘要翻译：保护二极管包括：半导体衬底; 半导体衬底中的第一导电类型的阱区; 半导体衬底中的第二导电类型的栅极侧扩散区，并连接到阱区; 半导体衬底中的与栅极侧扩散区分离的第二导电类型的接地侧扩散区，并与阱区连接; 连接在晶体管的栅极和栅极侧扩散区之间的栅极电极; 以及连接到接地侧扩散区的接地电极。接地侧扩散区域中的掺杂剂杂质浓度低于栅极侧扩散区域中的掺杂剂杂质浓度。

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