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1. 发明申请

US20100217001A1 METHOD FOR PRODUCING PYRAZOLE FUSED RING DERIVATIVE 审中-公开
标题翻译：用于生产吡唑熔融衍生物的方法
公开(公告)号：US20100217001A1
公开(公告)日：2010-08-26
申请号：US12738514
申请日：2008-10-17
申请人： Keizo Sato , Kazumasa Nara , Naoyuki Shimomura
发明人： Keizo Sato , Kazumasa Nara , Naoyuki Shimomura
IPC分类号： C07D471/04 , C07F5/02
CPC分类号： C07D471/04 , C07F5/025
摘要： Disclosed is a commercially advantageous method for producing a pyrazole fused ring derivative (such as a 7-phenylpyrazolo[1,5-a]pyridine derivative). Specifically disclosed is a method for producing a compound (I) represented by the formula (I) below or a salt thereof, which comprises a step A wherein a hydroxy group in a compound (IV) represented by the formula (IV) below is converted into a methoxy group, thereby obtaining a compound (I) or a salt thereof:
摘要翻译：公开了用于制备吡唑稠环衍生物（如7-苯基吡唑并[1,5-a]吡啶衍生物）的商业上有利的方法。具体公开的是制备下述式（I）表示的化合物（I）或其盐的方法，其包括步骤A，其中由下式（IV）表示的化合物（IV）中的羟基转化为形成甲氧基，从而得到化合物（I）或其盐：

2. 发明授权

US06333322B1 Nitrogen-containing tricyclic compounds and drugs containing the same 失效
标题翻译：含氮三环化合物和含有这些化合物的药物
公开(公告)号：US06333322B1
公开(公告)日：2001-12-25
申请号：US09125451
申请日：1998-09-21
申请人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Makoto Kaino , Masayuki Tanaka , Motohiro Soejima , Katsuhiro Moriya , Yoshinori Sakuma , Koji Yamada , Kokichi Harada , Yukio Nishizawa , Seiichi Kobayashi , Makoto Okita , Koichi Katayama
发明人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Makoto Kaino , Masayuki Tanaka , Motohiro Soejima , Katsuhiro Moriya , Yoshinori Sakuma , Koji Yamada , Kokichi Harada , Yukio Nishizawa , Seiichi Kobayashi , Makoto Okita , Koichi Katayama
IPC分类号： A61K315415
CPC分类号： C07D417/06 , C07D279/22 , C07D279/24 , C07D417/12 , C09B21/00 , C09B57/08
摘要： A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
摘要翻译：苯并噻嗪，吖啶酮肟，吖啶酮肟，腙酮腙和二苯并二氮杂衍生物，其对组胺，白细胞三烯等参与并有效预防或治疗化学介质如组胺和白三烯参与的疾病有效，例如哮喘，过敏性鼻炎，特应性皮炎，荨麻疹，花粉症，胃肠道过敏和食物过敏。

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. 发明申请

US20090149647A1 PROCESS FOR PRODUCTION OF LIPID A ANALOGUE 审中-公开
标题翻译：生产脂类似物的方法
公开(公告)号：US20090149647A1
公开(公告)日：2009-06-11
申请号：US12064450
申请日：2006-08-29
申请人： Katsuya Tagami , Keizo Sato , Kimihiro Matsuo , Taichi Abe , Toyokazu Haga
发明人： Katsuya Tagami , Keizo Sato , Kimihiro Matsuo , Taichi Abe , Toyokazu Haga
IPC分类号： C07H1/00
CPC分类号： C07H15/04 , C07H1/02
摘要： Discloses is a process for producing α-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-β-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source.
摘要翻译：公开了制备α-D-吡喃葡萄糖，3-O-癸基-2-脱氧-6-O- [2-脱氧-3-O - [（3R）-3-甲氧基癸基] -6-O-甲基 -2 - [（11Z）-1-氧代-11-十八碳烯基]氨基] -4-O-膦酰基-β-D-吡喃葡萄糖基] -2 - [（1,3-二氧代十四烷基）氨基] - 或1- 磷酸盐）四钠盐，其可用作其合成的药物或中间体的活性成分，其环境友好并且安全性，操作性和再现性优异。一种制备由式（I）表示的化合物的方法，包括以下步骤：使式（VIII）表示的化合物与钯催化剂在一种核仁类药剂的存在下反应并用钠源处理该产物。

5. 发明授权

US06795834B2 Apparatus, method, and storage medium for file management 失效
标题翻译：用于文件管理的装置，方法和存储介质
公开(公告)号：US06795834B2
公开(公告)日：2004-09-21
申请号：US09748372
申请日：2000-12-27
申请人： Yasuyuki Higashiura , Takumi Kishino , Seigo Kotani , Takashi Yoshioka , Keizo Sato , Hiroki Inoue
发明人： Yasuyuki Higashiura , Takumi Kishino , Seigo Kotani , Takashi Yoshioka , Keizo Sato , Hiroki Inoue
IPC分类号： G06F1200
CPC分类号： G06F11/14 , G06F11/1451 , Y10S707/99953 , Y10S707/99955
摘要： When a sweeping process and a backup process are performed on an electronic library file in an electronic library, a file storing a history of the sweeping process or a history of a backup process is generated, and the sweeping and the backup processes are managed. Thus, a user can easily manage as to which medium an original document has been swept to or where a backup copy of the original document is. If the uniqueness of the original document shown in a sweep history and a backup history can be secured, the problem that there can be a plurality of original documents on the storage media of a plurality of electronic libraries can be avoided.
摘要翻译：当在电子图书馆的电子图书馆文件中执行扫描处理和备份处理时，生成存储扫描处理的历史或备份处理的历史的文件，并且管理扫描和备份处理。因此，用户可以容易地管理原始文档被扫描到哪个媒体或原始文档的备份副本的位置。如果可以确保扫描历史和备份历史中所示的原始文档的唯一性，则可以避免在多个电子图书馆的存储介质上存在多个原始文档的问题。

6. 发明授权

US06583138B1 Heterocyclic-ring condensed benzothiazine compound 失效
标题翻译：杂环稠合苯并噻嗪化合物
公开(公告)号：US06583138B1
公开(公告)日：2003-06-24
申请号：US09622458
申请日：2001-01-04
申请人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Motohiro Soejima , Takashi Sato , Koichi Kikuchi , Hiroyuki Yoshimura , Katsuhiro Moriya , Yoshinori Sakuma , Shigeru Akasofu , Koji Yamada
发明人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Motohiro Soejima , Takashi Sato , Koichi Kikuchi , Hiroyuki Yoshimura , Katsuhiro Moriya , Yoshinori Sakuma , Shigeru Akasofu , Koji Yamada
IPC分类号： C07D51304
CPC分类号： C07D513/04
摘要： The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula: In the formula, the ring Het represents an unsaturated heterocyclic ring; R1 and R2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula —NR20R2 (in the formula, R20 and R21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R20 and R21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.
摘要翻译：本发明提供一种新颖的杂环稠合苯并噻嗪化合物，其对组胺，白细胞三烯等参与的疾病的预防或治疗有效。本发明的杂环稠合苯并噻嗪化合物或其药理学上可接受的盐对于预防或治疗其中化学介质如组胺，白三烯等参与的疾病是有效的，例如哮喘，过敏性鼻炎，特应性皮炎，荨麻疹，花粉症，胃肠道过敏，食物过敏等。此外，本发明的杂环稠合苯并噻嗪化合物，其药理学上可接受的盐或其水合物由下式表示：式中，环Het表示不饱和杂环; R1和R2彼此相同或不同，各自表示卤素原子，可以被卤素原子取代的低级烷基，可被卤素原子取代的低级烷氧基，低级烷基低级烷氧基基团，氰基; D表示可以具有取代基的低级亚烷基等; Q表示例如式-NR20R2（式中，R20和R21彼此相同或不同，各自表示氢原子，可被卤素原子取代的低级烷基，芳基可以具有取代基的芳基烷基，可以具有取代基的芳基烷基，可以具有取代基的杂芳基或可以具有取代基的杂芳基烷基，或者R20和R21可以与氮原子）; x表示1〜2的整数。

7. 发明申请

US20080214564A1 MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
标题翻译：固体形式的MACROLIDE化合物，其制备方法和含有该化合物的药物组合物
公开(公告)号：US20080214564A1
公开(公告)日：2008-09-04
申请号：US12021184
申请日：2008-01-28
申请人： Hiroshi ISHIHARA , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
发明人： Hiroshi ISHIHARA , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
IPC分类号： A61K31/497 , C07D405/12
CPC分类号： C07D407/06
摘要： The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.
摘要翻译：本发明提供了固体形式的式（I）化合物，其作为药物制造的大量药物是均匀的，具有高纯度，并且易于加工。本发明还提供了制备该化合物的方法和含有该化合物的药物组合物。（8E，12E，14E）-7 - {（4-环庚基哌嗪-1-基）羰基}氧-3,6,16,21-四羟基-6,10,12,16,20-五甲基 - 开发了具有统一规格并且易于使用的18,19-环氧树脂-8,12,14-三烯-11-硼化物。

8. 发明授权

US06489336B2 Nitrogen-containing tricyclic compounds and drugs containing the same 失效
标题翻译：含氮三环化合物和含有这些化合物的药物
公开(公告)号：US06489336B2
公开(公告)日：2002-12-03
申请号：US09985416
申请日：2001-11-02
申请人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Makoto Kaino , Masayuki Tanaka , Motohiro Soejima , Katsuhiro Moriya , Yoshinori Sakuma , Koji Yamada , Kokichi Harada , Yukio Nishizawa , Seiichi Kobayashi , Makoto Okita , Koichi Katayama
发明人： Mitsuaki Miyamoto , Tatsuya Yoshiuchi , Keizo Sato , Makoto Kaino , Masayuki Tanaka , Motohiro Soejima , Katsuhiro Moriya , Yoshinori Sakuma , Koji Yamada , Kokichi Harada , Yukio Nishizawa , Seiichi Kobayashi , Makoto Okita , Koichi Katayama
IPC分类号： A61K31473
CPC分类号： C07D417/06 , C07D279/22 , C07D279/24 , C07D417/12 , C09B21/00 , C09B57/08
摘要： A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
摘要翻译：苯并噻嗪，吖啶酮肟，吖啶酮肟，腙酮腙和二苯并二氮杂衍生物，其对组胺，白细胞三烯等参与并有效预防或治疗化学介质如组胺和白三烯参与的疾病有效，例如哮喘，过敏性鼻炎，特应性皮炎，荨麻疹，花粉症，胃肠道过敏和食物过敏。

9. 发明授权

US07790887B2 Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same 失效
标题翻译：固体形式的大环内酯类化合物，其制备方法和含有该化合物的药物组合物
公开(公告)号：US07790887B2
公开(公告)日：2010-09-07
申请号：US12021184
申请日：2008-01-28
申请人： Hiroshi Ishihara , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
发明人： Hiroshi Ishihara , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
IPC分类号： C07D411/14
CPC分类号： C07D407/06
摘要： The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.
摘要翻译：本发明提供了固体形式的式（I）化合物，其作为药物制造的大量药物是均匀的，具有高纯度，并且易于加工。本发明还提供了制备该化合物的方法和含有该化合物的药物组合物。（8E，12E，14E）-7 - {（4-环庚基哌嗪-1-基）羰基}氧-3,6,16,21-四羟基-6,10,12,16,20-五甲基 - 开发了具有统一规格并且易于使用的18,19-环氧树脂-8,12,14-三烯-11-硼化物。

10. 发明申请

US20100094001A1 COMPOSITION CONTAINING STABILITY-IMPROVED CHLOROMETHYL PHOSPHATE DERIVATIVE AND PROCESS FOR PRODUCING SAME 审中-公开
标题翻译：包含稳定性改进的氯代氯代磷酸酯衍生物的组合物及其生产方法
公开(公告)号：US20100094001A1
公开(公告)日：2010-04-15
申请号：US12526905
申请日：2008-03-05
申请人： Keizo Sato , Shinya Abe , Kazuhiro Yoshizawa , Kazunori Wakasugi , Shigeto Negi , Mamoru Miyazawa
发明人： Keizo Sato , Shinya Abe , Kazuhiro Yoshizawa , Kazunori Wakasugi , Shigeto Negi , Mamoru Miyazawa
IPC分类号： C07D265/30 , C07F9/06
CPC分类号： C07F9/025 , C07F9/091
摘要： The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine, (wherein R1 and R2 are identical or different from each other, and represent a C1-C6 alkyl group, a C2-C6 alkenyl group or a C6-C14 aryl C1-C6 alkyl group which may have a substituent, and R1 and R2 may together form a ring), the process comprising the step of adding the tertiary amine having a boiling point at 1 atmosphere of 150° C. or higher to the compound represented by formula (I).
摘要翻译：本发明提供了用于制备可用于制备水溶性前药的氯甲基磷酸酯衍生物的方法等，从可加工性，操作性和节能性的观点出发，优选。根据本发明，提供一种制备含有下式（I）表示的化合物和叔胺的组合物的方法，其中R1和R2彼此相同或不同，并表示C1-C6 烷基，C 2 -C 6烯基或可以具有取代基的C 6 -C 14芳基C 1 -C 6烷基，R 1和R 2可以一起形成环），该方法包括将具有沸点在由式（I）表示的化合物的150℃以上的1个大气压下进行。

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