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1. 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

2. 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。

3. 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。

4. 发明授权

US07745198B2 Method of producing macrolide compound 失效
标题翻译：大环内酯类化合物的制备方法
公开(公告)号：US07745198B2
公开(公告)日：2010-06-29
申请号：US10532412
申请日：2003-11-27
申请人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
发明人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
IPC分类号： C12N1/20 , A01N43/02
CPC分类号： C07D407/06 , A61K31/336 , C12P17/162
摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured myceha and oxygen, and then 11107D substance which is a target material is collected from the treating solution.
摘要翻译：本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的肌肉和氧的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。

5. 发明申请

US20060141589A1 Method of producing macrolide compound 失效
标题翻译：大环内酯类化合物的制备方法
公开(公告)号：US20060141589A1
公开(公告)日：2006-06-29
申请号：US10532412
申请日：2003-11-27
申请人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
发明人： Akifumi Okuda , Satoshi Yamamoto , Takashi Sakai , Susumu Takeda , Takashi Nakashima , Katsura Kaneko , Tomohiro Sameshima , Taira Kato , Naoto Kawamura
IPC分类号： C12P17/02 , C12N1/21
CPC分类号： C07D407/06 , A61K31/336 , C12P17/162
摘要： The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus Mortierella, the genus Streptomyces or the family Micromonosporaceae (for example, Streptomyces sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured mycelia and oxygen, and then 11107D substance which is a target material is collected from the treating solution.
摘要翻译：本发明提供了通过生物转化制备具有抗肿瘤活性的12元环大环内酯化合物11107D的新方法。作为式（I）所示的12元环大环内酯化合物11107B的起始原料在属于被孢霉属（Mortierella），链霉菌属（Streptomyces）属或小单孢菌属（Micromonosporaceae）的菌株（例如，链霉菌属AB-1704 菌株（FERM BP-8551）），其各自具有将12元环大环内酯化合物11107B转化为由式（II）表示的11107D物质或其培养的菌丝体和氧气的制剂的能力，然后将11107D 从处理液中收集作为目标物质的物质。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明申请

US20130331576A1 Novel Compound, Novel Ligand, Novel Transition Metal Complex, and Catalyst Including Novel Transition Metal Complex 有权
标题翻译：新型配体，新型配体，新型过渡金属络合物和包含新型过渡金属络合物的催化剂
公开(公告)号：US20130331576A1
公开(公告)日：2013-12-12
申请号：US13985378
申请日：2012-02-16
申请人： Toshinobu Korenaga , Takashi Sakai , Aram Ko
发明人： Toshinobu Korenaga , Takashi Sakai , Aram Ko
IPC分类号： C07F9/58 , B01J31/24 , C07F15/00 , C07F11/00 , C07F17/02 , C07F9/6558
CPC分类号： C07F9/58 , B01J31/2295 , B01J31/2404 , B01J31/2409 , B01J31/2452 , B01J31/2457 , B01J2231/346 , B01J2231/4205 , B01J2231/4255 , B01J2231/643 , B01J2531/0205 , B01J2531/0216 , B01J2531/0266 , B01J2531/64 , B01J2531/822 , B01J2531/824 , B01J2531/828 , B01J2531/842 , B01J2540/10 , B01J2540/22 , B01J2540/225 , B01J2540/40 , B01J2540/444 , B01J2540/62 , C07F9/5027 , C07F9/65522 , C07F9/65586 , C07F11/00 , C07F15/006 , C07F15/0073 , C07F15/008 , C07F15/0093 , C07F17/02
摘要： The invention provides novel ligands for transition metal complexes which exhibit high coordination power with respect to metals by being free of substituents at the positions ortho to phosphorus or arsenic and which have electron-withdrawing power comparable to the highest level known in conventional ligands. A ligand of the invention includes a compound represented by General Formula (1): R1R2R3A or General Formula (2): R1R2A-Y-AR3R4 and having a total of 15 to 110 carbon atoms. In the formulae, A is phosphorus or arsenic; R1, R2, R3 and R4 are each independently a substituted pyridyl group having optionally different electron-withdrawing groups bonded to the positions meta to the atom A as well as hydrogen atoms bonded to the positions ortho to the atom A; and Y is a divalent group derived from a C2-20, optionally substituted and optionally heteroatom-containing, aliphatic, alicyclic or aromatic compound or from ferrocene.
摘要翻译：本发明提供了用于过渡金属配合物的新型配体，其通过在磷或砷邻位置没有取代基而具有相对于金属的高配位力，并且具有与常规配体中已知的最高水平相当的吸电能力。本发明的配体包括由通式（1）表示的化合物：R1R2R3A或通式（2）：R1R2A-Y-AR3R4，总共具有15至110个碳原子。在配方中，A是磷或砷; R 1，R 2，R 3和R 4各自独立地为具有与位于原子A的位置键合的任意不同的吸电子基团的取代的吡啶基以及与原子A的邻位键合的氢原子; 并且Y是衍生自C2-20，任选取代的和任选地含杂原子的脂族，脂环族或芳族化合物或二茂铁的二价基团。

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