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1. 发明申请

US20080227815A1 Crystal of Indole Derivative Having Piperidine Ring and Process for Production Thereof 审中-公开
标题翻译：具有哌啶环的吲哚衍生物的晶体及其制备方法
公开(公告)号：US20080227815A1
公开(公告)日：2008-09-18
申请号：US11913931
申请日：2006-05-11
申请人： Takahisa Sakaguchi , Yuichi Suzuki , Koichi Ito , Jun Niijima , Mamoru Miyazawa , Toshikazu Shimizu , Masaharu Gotoda , Naoko Suzuki , Takashi Hasebe
发明人： Takahisa Sakaguchi , Yuichi Suzuki , Koichi Ito , Jun Niijima , Mamoru Miyazawa , Toshikazu Shimizu , Masaharu Gotoda , Naoko Suzuki , Takashi Hasebe
IPC分类号： A61K31/454 , C07D405/14 , A61P25/18 , A61P25/30
CPC分类号： C07D405/14
摘要： A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
摘要翻译： 1- [1- [2-（7-甲氧基-2,2-二甲基-4-氧代色满-8-基） - 乙基]哌啶-4-基] -N-甲基-1H-吲哚-6- 富马酸甲酰胺，在13 C固体NMR光谱中具有约124.0ppm和约26.8ppm的化学位移的峰。

2. 发明申请

US20090192316A1 PROCESS FOR PREPARATION OF WATER-SOLUBLE AZOLE PRODRUGS 有权
标题翻译：水溶性AZOLE PRODRUGS的制备方法
公开(公告)号：US20090192316A1
公开(公告)日：2009-07-30
申请号：US12097244
申请日：2006-12-20
申请人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
发明人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
IPC分类号： C07F9/6539
CPC分类号： C07F9/65583
摘要： An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
摘要翻译：本发明的目的是提供一种适于工业化有效的脱保护反应而不使用有毒溶剂的方法，以及提供一种制备水溶性唑类药物的方法等。。本发明提供由式（I）表示的盐的制备方法。（其中X表示在苯基的第4位或第5位键合的氟原子），包括以下步骤：（a）进行式（II）表示的化合物的脱保护反应; （其中X表示在苯基的4位或5位键合的氟原子）在碳阳离子清除剂存在下进行。

3. 发明授权

US07803949B2 Process for preparation of water-soluble azole prodrugs 有权
标题翻译：制备水溶性唑前体药物的方法
公开(公告)号：US07803949B2
公开(公告)日：2010-09-28
申请号：US12097244
申请日：2006-12-20
申请人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
发明人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
IPC分类号： C07F9/06
CPC分类号： C07F9/65583
摘要： An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
摘要翻译：本发明的目的是提供一种适于工业化有效的脱保护反应而不使用有毒溶剂的方法，以及提供一种制备水溶性唑类药物的方法等。。本发明提供由式（I）表示的盐的制备方法。（其中X表示在苯基的第4位或第5位键合的氟原子），包括以下步骤：（a）进行式（II）表示的化合物的脱保护反应; （其中X表示在苯基的4位或5位键合的氟原子）在碳阳离子清除剂存在下进行。

4. 发明授权

US08410277B2 Method for manufacturing heterocycle substituted pyridine derivatives 失效
标题翻译：制备杂环取代吡啶衍生物的方法
公开(公告)号：US08410277B2
公开(公告)日：2013-04-02
申请号：US12809011
申请日：2008-12-25
申请人： Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
发明人： Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
IPC分类号： C07D413/14
CPC分类号： C07D498/04 , C07D213/46 , C07D213/643 , C07D413/04 , C07D413/14 , Y02P20/55
摘要： It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.; R represents a hydrogen atom or a C1-6 alkyl group, etc.; R3 represents a hydrogen atom or a halogen atom, etc.; and R4 represents a hydrogen atom or a halogen atom; provided that when Z represents a single bond, or when R3 represents a hydrogen atom, then R1, R2, and R4 cannot all be a hydrogen atom at the same time.
摘要翻译：本发明的目的是提供一种制备杂环取代的吡啶衍生物的有效方法。本发明提供下述式（I）表示的化合物的制造方法：使下述式（III）表示的化合物与下述式（II）所示的化合物反应的方法：在溶剂和在钯催化剂和碱的存在下，其中R1表示氢原子等; R2表示氢原子，C1-6烷基，可被保护基保护的氨基等; X和Y中的一个表示氮原子，另一个表示氮原子或氧原子; Q表示离去组; 环A表示可具有一个或两个卤素原子或C 1-6烷基的5-或6-元杂芳环或苯环; Z表示单键，亚甲基，亚乙基，氧原子等; R表示氢原子或C 1-6烷基等; R3表示氢原子或卤素原子等; R4代表氢原子或卤原子; 条件是当Z表示单键时，或当R3表示氢原子时，则R1，R2和R4不能同时为氢原子。

5. 发明授权

US08058444B2 Heterocycle-substituted pyridine derivative's salt or crystal thereof 有权
标题翻译：杂环取代的吡啶衍生物的盐或其结晶
公开(公告)号：US08058444B2
公开(公告)日：2011-11-15
申请号：US12109959
申请日：2008-04-25
申请人： Jun Niijima , Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Eiichi Yamamoto , Takuma Minamisono
发明人： Jun Niijima , Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Eiichi Yamamoto , Takuma Minamisono
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.
摘要翻译：提供了杂环取代的吡啶衍生物的盐或其结晶。本发明提供3-（3-（4-（吡啶-2-基氧基甲基） - 苄基） - 异恶唑-5-基） - 吡啶-2-基胺或其结晶的酸加成盐以及生产相同。

6. 发明申请

US20110263845A1 METHOD FOR MANUFACTURING HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVES 失效
标题翻译：制备杂环取代的吡啶衍生物的方法
公开(公告)号：US20110263845A1
公开(公告)日：2011-10-27
申请号：US12809011
申请日：2008-12-25
申请人： Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
发明人： Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
IPC分类号： C07D498/04 , C07D413/04 , C07F5/02 , C07D213/64 , C07D413/14 , C07F5/04
CPC分类号： C07D498/04 , C07D213/46 , C07D213/643 , C07D413/04 , C07D413/14 , Y02P20/55
摘要： It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.; R represents a hydrogen atom or a C1-6 alkyl group, etc.; R3 represents a hydrogen atom or a halogen atom, etc.; and R4 represents a hydrogen atom or a halogen atom; provided that when Z represents a single bond, or when R3 represents a hydrogen atom, then R1, R2, and R4 cannot all be a hydrogen atom at the same time.
摘要翻译：本发明的目的是提供一种制备杂环取代的吡啶衍生物的有效方法。本发明提供下述式（I）表示的化合物的制造方法：使下述式（III）表示的化合物与下述式（II）所示的化合物反应的方法：在溶剂和在钯催化剂和碱的存在下，其中R1表示氢原子等; R2表示氢原子，C1-6烷基，可被保护基保护的氨基等; X和Y中的一个表示氮原子，另一个表示氮原子或氧原子; Q表示离去组; 环A表示可具有一个或两个卤素原子或C 1-6烷基的5-或6-元杂芳环或苯环; Z表示单键，亚甲基，亚乙基，氧原子等; R表示氢原子或C 1-6烷基等; R3表示氢原子或卤素原子等; R4代表氢原子或卤原子; 条件是当Z表示单键时，或当R3表示氢原子时，则R1，R2和R4不能同时为氢原子。

7. 发明授权

US07256178B2 Physiologically active substances 有权
标题翻译：生理活性物质
公开(公告)号：US07256178B2
公开(公告)日：2007-08-14
申请号：US10522731
申请日：2003-07-31
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
IPC分类号： A01N43/04 , A61K31/70 , A61K39/00 , A61K39/38 , A61K39/40
CPC分类号： C07D407/06 , C07D313/00 , C12P17/08 , C12P17/16 , C12P17/162
摘要： Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
摘要翻译：由以下通式（I）表示的化合物，其药学上可接受的盐或其水合物：其中W表示和R 3，R 7，R 7， SUP> 16，R 17，R 20，R 21和R 21'是相同或不同，各自表示氢等。由于抑制血管生成并抑制VEGF的产生，特别是在缺氧中，化合物（I）可用作固体癌症的补救措施。

8. 发明授权

US07893068B2 Physiologically active substances 有权
标题翻译：生理活性物质
公开(公告)号：US07893068B2
公开(公告)日：2011-02-22
申请号：US11927564
申请日：2007-10-29
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： A61K31/496 , A61K31/365 , C07D313/00 , C07D405/12 , A61P19/02 , A61P29/00 , A61P35/00 , A61P9/10
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
摘要翻译：本发明涉及由式（I）表示的化合物：其中R3，R6，R7和R21彼此相同或不同，各自表示羟基等），其药理学上可接受的盐或它们的水合物。本发明的化合物（I）抑制血管生成，特别是在缺氧条件下抑制VEGF的产生，可用作治疗实体癌的治疗剂。

9. 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。

10. 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。

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