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1. 发明授权

US07816401B2 Process for total synthesis of pladienolide B and pladienolide D 失效
标题翻译：丙二烯内酯B和普拉二烯内酯D的全合成方法
公开(公告)号：US07816401B2
公开(公告)日：2010-10-19
申请号：US11580047
申请日：2006-10-13
申请人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： A61K31/335 , A61K31/16
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.
摘要翻译：一种制备由式（11）表示的化合物的方法：其中P1，P7，P8，P9和R1与本文所定义的相同，其特征在于包括使由式（12）表示的化合物与式（12）表示的化合物 13）：在催化剂存在下。

2. 发明授权

US07884128B2 Process for total synthesis of pladienolide B and pladienolide D 失效
标题翻译：丙二烯内酯B和普拉二烯内酯D的全合成方法
公开(公告)号：US07884128B2
公开(公告)日：2011-02-08
申请号：US12764336
申请日：2010-04-21
申请人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： A61K31/36
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
摘要翻译：制备式的化合物的方法：其中P2，P3和R2与下文定义相同，其特征在于包括使由式（7）表示的化合物反应：其中P3表示羟基的保护基; 和Het表示1-苯基-1H-四唑-5-基与式（8）表示的化合物：其中P2表示羟基的保护基; 并且R 2表示在碱的存在下可被取代的苯基。

3. 发明申请

US20100204490A1 PROCESS FOR TOTAL SYNTHESIS OF PLADIENOLIDE B AND PLADIENOLIDE D 失效
标题翻译： PLADIENOLIDE B和PLADENENOL D的合成方法D
公开(公告)号：US20100204490A1
公开(公告)日：2010-08-12
申请号：US12764336
申请日：2010-04-21
申请人： Regina Mikie KANADA , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Mikie KANADA , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： C07D493/04
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
摘要翻译：制备式的化合物的方法：其中P2，P3和R2与下文定义相同，其特征在于包括使由式（7）表示的化合物反应：其中P3表示羟基的保护基; 和Het表示1-苯基-1H-四唑-5-基与式（8）表示的化合物：其中P2表示羟基的保护基; 并且R 2表示在碱的存在下可被取代的苯基。

4. 发明申请

US20080021226A1 Process for total synthesis of pladienolide B and pladienolide D 失效
标题翻译：丙二烯内酯B和普拉二烯内酯D的全合成方法
公开(公告)号：US20080021226A1
公开(公告)日：2008-01-24
申请号：US11580047
申请日：2006-10-13
申请人： Regina Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： C07D313/00 , C07D303/02
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： [Problems to be Solved]To provide an effective process for total synthesis of pladienolide B and pladienolide D having excellent anti-tumor activity and to provide useful intermediates in the above-described process. [Measure for Solving the Problem]A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined below, characterized by including reacting a compound represented by Formula (12): wherein P7 means a hydrogen atom or a protecting group for hydroxy group; R1 means a hydrogen atom or a hydroxy group, with a compound represented by Formula (13): wherein P1 means a hydrogen atom or a protecting group for hydroxy group; P8 means a hydrogen atom, an acetyl group or a protecting group for hydroxy group; P9 means a hydrogen atom or a protecting group for hydroxy group; or P8 and P9 may form together a group represented by a formula: wherein R5 means a phenyl group which may have a substituent, in the presence of a catalyst.
摘要翻译： [待解决的问题]为了提供具有优异的抗肿瘤活性的普拉二烯内酯B和普拉二烯内酯D的全合成的有效方法，并且在上述方法中提供有用的中间体。 [解决问题的措施]制备由式（11）表示的化合物的方法：其中P 1，P 2，P 3，，其中P 9和R 12与下述定义相同，其特征在于包括使由式（12）表示的化合物：其中P 是指氢原子或羟基的保护基; R 1表示氢原子或羟基，与式（13）表示的化合物：其中P 1是氢原子或羟基的保护基; “8”表示氢原子，乙酰基或羟基保护基; “9”表示氢原子或羟基的保护基; 或者P 9和P 9可以一起形成由下式表示的基团：其中R 5表示可以具有取代基的苯基，在催化剂存在下。

5. 发明授权

US07667052B2 Bioactive substance 有权
标题翻译：生物活性物质
公开(公告)号：US07667052B2
公开(公告)日：2010-02-23
申请号：US11213962
申请日：2005-08-30
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： C07D313/00 , C07D407/06 , A61K31/365
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.
摘要翻译：本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法。

6. 发明申请

US20060079572A1 Novel bioactive substance 有权
标题翻译：新型生物活性物质
公开(公告)号：US20060079572A1
公开(公告)日：2006-04-13
申请号：US11213962
申请日：2005-08-30
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： A61K31/365 , C07D313/00
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.
摘要翻译：本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法。

7. 发明授权

US07026352B1 Physiologically active substances 有权
标题翻译：生理活性物质
公开(公告)号：US07026352B1
公开(公告)日：2006-04-11
申请号：US10470806
申请日：2002-02-01
申请人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
发明人： Yoshiharu Mizui , Takashi Sakai , Satoshi Yamamoto , Keisuke Komeda , Masanori Fujita , Akifumi Okuda , Kumiko Kishi , Jun Niijima , Mitsuo Nagai , Kiyoshi Okamoto , Masao Iwata , Yoshihiko Kotake , Toshimitsu Uenaka , Naoki Asai , Motoko Matsufuji , Tomohiro Sameshima , Naoto Kawamura , Kazuyuki Dobashi , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Susumu Takeda , Tomonari Yamada , Koji Norihisa , Takao Yamori
IPC分类号： A61K31/365 , C07D313/00
CPC分类号： C07D405/14 , A61K31/335 , A61K31/336 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/74 , C07D313/00 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C12P17/02
摘要： The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it
摘要翻译：本发明提供了具有抗肿瘤活性的新型生物活性物质及其制造方法及其医疗用途。即，它提供了由下列公式表示的12元环大环内酯化合物，其由Streptomyces sp。梅尔 11107或其变体，其药理学上可接受的盐或它们的水合物及其制备方法

8. 发明申请

US20110065202A1 Method for Examination of Alzheimer's Disease 审中-公开
标题翻译：阿尔茨海默病检查方法
公开(公告)号：US20110065202A1
公开(公告)日：2011-03-17
申请号：US12992309
申请日：2009-06-11
申请人： Khin Than Myint , Yoshiya Oda , Naoki Asai
发明人： Khin Than Myint , Yoshiya Oda , Naoki Asai
IPC分类号： G01N33/53 , G01N27/26 , G01N30/02 , H01J49/26
CPC分类号： G01N33/9453 , G01N30/72 , G01N33/9486 , G01N2800/2821 , Y10T436/174614
摘要： A method for examining Alzheimer's disease comprising (1) the measurement step of measuring an amount of lidocaine or a metabolite thereof in a cerebrospinal fluid derived from a lidocaine-administered test subject, and (2) the determination step of determining whether the test subject has Alzheimer's disease or not on the basis of the measured amount.
摘要翻译：一种检查阿尔茨海默氏病的方法，其特征在于，包括：（1）测定利多卡因或其代谢物在来自利多卡因的测试对象的脑脊液中的量的测定步骤，以及（2）阿尔茨海默氏病或不是基于测量量。

9. 发明授权

US5789727A Integrated method and apparatus for reading mier code and printing 失效
标题翻译：用于读取微码和打印的集成方法和装置
公开(公告)号：US5789727A
公开(公告)日：1998-08-04
申请号：US544528
申请日：1995-10-18
申请人： Mitsuaki Teradaira , Tsutomu Momose , Kenji Komatsu , Eizo Takahashi , Akira Koyabu , Naoki Asai
发明人： Mitsuaki Teradaira , Tsutomu Momose , Kenji Komatsu , Eizo Takahashi , Akira Koyabu , Naoki Asai
IPC分类号： B41J3/44 , B41J3/60 , B41J11/48 , B41J11/50 , B41J13/10 , G06K1/12 , G06K7/08 , G06K17/00
CPC分类号： G06Q20/042 , B41J11/48 , B41J11/50 , B41J13/10 , B41J3/44 , B41J3/60 , G06K1/125 , G06K17/00 , G06K7/084 , Y10S271/902
摘要： Printing to aNd MICR code reading from a cut-sheet form imprinted with an MICR code, such as personal checks, are continuously accomplished by a single apparatus, thereby simplifying processing and reducing the required installation space. A magnetic head and a magnet for reading the MICR code are disposed on the slope of a paper path provided in a printer housing. A personal check in paper path is held by cut-sheet form loading rollers and/or transportation rollers which operate at a synchronized speed, and is passed over the magnetic head for MICR code reading. Thereafter, the personal check is held by the loading rollers and/or the transportation rollers for endorsement printing by the print head.
摘要翻译：通过单个设备连续地进行打印到由打印有MICR码（例如个人检查）的单张纸形式读取的MICR代码，从而简化处理并减少所需的安装空间。用于读取MICR码的磁头和磁铁设置在设置在打印机壳体中的纸路的斜面上。纸张通行的个人检查由以同步速度操作的片状加载辊和/或输送辊保持，并且通过用于MICR代码读取的磁头。此后，个人支票由装载辊和/或输送辊保持，用于由打印头进行背书印刷。

10. 发明授权

US06328490B1 Winding shaft and a printer using the same 有权
标题翻译：绕线轴和使用其的打印机
公开(公告)号：US06328490B1
公开(公告)日：2001-12-11
申请号：US09583190
申请日：2000-05-30
申请人： Hiroshi Narita , Masahiko Yamada , Naoki Asai , Kenichiro Arai
发明人： Hiroshi Narita , Masahiko Yamada , Naoki Asai , Kenichiro Arai
IPC分类号： B41J1126
CPC分类号： B65H75/24 , B65H18/04 , B65H75/242
摘要： A winding shaft, for use in a printer allows a wound recording paper to be easily removed therefrom. The winding shaft includes a shaft main body, a winding portion and a support-removing member. The winding portion, which sandwiches the shaft main body, winds the recording paper therearound. The shaft main body includes a pair of support-removing members, which respectively project from the shaft main body. The two support-removing members are respectively supported on the two side portions of the shaft main body in such a manner that they can be freely rotated about their respective support shafts. A tension-coiled spring is bridgingly disposed between the two support-removing members, so that the two support-removing members remain in standing positions when no external force is applied to them. If the recording paper is lightly rotated in a direction opposite to the winding direction of the recording paper, then the two support-removing members are brought down in the same direction due to an external force applied thereto from the innermost peripheral recording paper. As a result, the innermost peripheral recording paper is loosened, that is, is caused to float loosely from the outer peripheral surface of the shaft main body, thereby enabling the removal of the recording paper from the winding shaft.
摘要翻译：用于打印机中的卷绕轴允许容易地从其上移除卷绕的记录纸。卷绕轴包括轴主体，卷绕部分和支撑件移除部件。卷绕轴主体的卷绕部分绕着记录纸卷绕。轴主体包括分别从轴主体突出的一对支撑移除构件。两个支撑移除部件分别支撑在轴主体的两个侧部上，使得它们能够绕其各自的支撑轴自由旋转。张紧螺旋弹簧桥接地布置在两个支撑移除构件之间，使得当没有施加外力时，两个支撑件移除构件保持在竖立位置。如果记录纸在与记录纸的卷绕方向相反的方向上轻微旋转，则两个支撑件移除部件由于从最内侧的周边记录纸施加到其上的外力而沿同一方向下降。结果，最内侧的周边记录纸被松动，从而从轴主体的外周表面松动地浮动，从而能够从卷轴移除记录纸。

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