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1. 发明授权

US09206169B2 Method for producing benzo[b]thiophene compound 有权
标题翻译：苯并[b]噻吩化合物的制备方法
公开(公告)号：US09206169B2
公开(公告)日：2015-12-08
申请号：US14235635
申请日：2012-07-27
申请人： Koichi Shinhama , Naoto Utsumi , Masahiro Sota , Shigeo Fujieda , Shin Ogasawara
发明人： Koichi Shinhama , Naoto Utsumi , Masahiro Sota , Shigeo Fujieda , Shin Ogasawara
IPC分类号： C07D409/12 , C07D333/54
CPC分类号： C07D409/12 , C07D333/54 , Y02P20/55
摘要： The present invention provides a method for producing a compound of Formula (4): wherein R1 is a hydrogen atom etc. by reacting a compound of Formula (2): wherein X1 is a leaving group, with a compound of Formula (3): wherein R1 is as defined above, in the presence of (a) a palladium compound and a tertiary phosphine or (b) a palladium carbene complex, in an inert solvent or without a solvent. The present invention can produce the compound of Formula (4), with high purity and high yield, and by a simple operation.
摘要翻译：本发明提供式（4）的化合物的制备方法：其中，R 1为氢原子等，式（2）的化合物：其中X1为离去基团与式（3）的化合物反应：其中R 1如上定义，在（a）钯化合物和叔膦或（b）钯卡宾络合物的存在下，在惰性溶剂中或不用溶剂存在下进行。本发明可以通过简单的操作制备高纯度和高收率的式（4）化合物。

2. 发明授权

US08703773B2 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof 有权
公开(公告)号：US08703773B2
公开(公告)日：2014-04-22
申请号：US13476773
申请日：2012-05-21
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： A61K31/497 , C07D401/12
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.

3. 发明授权

US08598358B2 Synthetic intermediate of oxazole compound and method for producing the same 有权
标题翻译：恶唑化合物的合成中间体及其制造方法
公开(公告)号：US08598358B2
公开(公告)日：2013-12-03
申请号：US13574546
申请日：2011-01-28
申请人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
发明人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
IPC分类号： C07D211/46 , C07D405/12 , C07D498/04
CPC分类号： C07D211/46 , C07D405/12 , C07D498/04
摘要： An object of the present invention is to provide a method for producing an oxazole compound in a high yield.The object can be achieved by a compound represented by Formula (11): wherein R1 is a hydrogen atom or lower-alkyl group; R2 is a 1-piperidyl group substituted at the 4-position with a substituent selected from (A1a) a phenoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1b) a phenoxy-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkyl groups, (A1c) a phenyl-substituted lower-alkoxy lower-alkyl group substituted on the phenyl moiety with halogen, (A1d) a phenyl-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1e) an amino group substituted with a phenyl group substituted with one or more halogen-substituted lower-alkoxy groups, and a lower-alkyl group, and (A1f) a phenyl-substituted lower-alkoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups; n is an integer from 1 to 6; and X3 is an organic sulfonyloxy group.
摘要翻译：本发明的目的是提供以高产率制备恶唑化合物的方法。该目的可以通过式（11）表示的化合物来实现：其中R1是氢原子或低级烷基; R2是在4-位被取代基取代的1-哌啶基，该取代基选自（A1a）苯基部分被一个或多个卤素取代的低级烷氧基取代的苯氧基，（A1b）苯氧基取代的低级烷氧基，在苯基部分上被一个或多个卤素取代的低级烷基取代的烷基（A1c）在苯基部分被卤素取代的苯基取代的低级烷氧基低级烷基，（A1d）苯基取代的低级烷基，在苯基部分被一个或多个卤素取代的低级烷氧基取代的烷基，（A1e）被被一个或多个卤素取代的低级烷氧基取代的苯基取代的氨基和低级烷基，和（A1f）在苯基部分上被一个或多个卤素取代的低级烷氧基取代的苯基取代的低级烷氧基; n是1至6的整数; X3是有机磺酰氧基。

4. 发明授权

US08399469B2 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof 有权
公开(公告)号：US08399469B2
公开(公告)日：2013-03-19
申请号：US11790604
申请日：2007-04-26
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： C07D401/12 , A61K31/497
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.

5. 发明申请

US20120316180A1 LOW HYGROSCOPIC ARIPIPRAZOLE DRUG SUBSTANCE AND PROCESSES FOR THE PREPARATION THEREOF 有权
标题翻译：低剂量阿维替唑药物及其制备方法
公开(公告)号：US20120316180A1
公开(公告)日：2012-12-13
申请号：US13476773
申请日：2012-05-21
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： C07D401/12 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/16 , A61P25/20 , A61P15/00 , A61P25/30 , A61P1/08 , A61P3/04 , A61P25/06 , A61P25/32 , A61K31/496
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
摘要翻译：本发明提供低吸湿形式的阿立哌唑及其制备方法，即使当含有无水阿立哌唑晶体的药物制剂长时间储存时，其也不会转化为水合物或丧失其原始溶解度。

6. 发明申请

US20120316179A1 LOW HYGROSCOPIC ARIPIPRAZOLE DRUG SUBSTANCE AND PROCESSES FOR THE PREPARATION THEREOF 有权
公开(公告)号：US20120316179A1
公开(公告)日：2012-12-13
申请号：US13476758
申请日：2012-05-21
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Misanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Misanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： C07D401/12 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/06 , A61P25/16 , A61P25/32 , A61P25/30 , A61P1/08 , A61P3/04 , A61K31/496 , A61P25/28
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.

7. 发明申请

US20120130082A1 1-Substituted-4-Nitroimidazole Compound and Method for Preparing the Same 审中-公开
标题翻译： 1-取代的4-硝基咪唑化合物及其制备方法
公开(公告)号：US20120130082A1
公开(公告)日：2012-05-24
申请号：US13362646
申请日：2012-01-31
申请人： Fumitaka GOTO , Noriaki Takemura , Tadaaki Otani , Takeshi Hasegawa , Hidetsugu Tsubouchi , Naoto Utsumi , Shigekazu Fujita , Hideaki Kuroda , Takuya Shitsuta , Hirofumi Sasaki
发明人： Fumitaka GOTO , Noriaki Takemura , Tadaaki Otani , Takeshi Hasegawa , Hidetsugu Tsubouchi , Naoto Utsumi , Shigekazu Fujita , Hideaki Kuroda , Takuya Shitsuta , Hirofumi Sasaki
IPC分类号： C07D405/06 , C07D233/92 , C07D233/84
CPC分类号： C07D233/92
摘要： The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.
摘要翻译：本发明涉及由通式（1）表示的1-取代-4-硝基咪唑化合物或其盐（其中R是氢原子，低级烷氧基取代的低级烷基，苯基 - 低级烷氧基取代基的低级烷基，氰基取代的低级烷基，可以具有低级烷氧基作为苯环中的取代基的苯基 - 低级烷基或式-CH2RA的基团; X是卤素原子或基团-S（O）n -R1）及其制备方法。式（1）的化合物是用作合成各种药用和农药的中间体的有用化合物，特别是作为抗结核剂的中间体。

8. 发明申请

US20120077821A1 LOW HYGROSCOPIC ARIPIPRAZOLE DRUG SUBSTANCE AND PROCESSES FOR THE PREPARATION THEREOF 有权
标题翻译：低剂量阿维替唑药物及其制备方法
公开(公告)号：US20120077821A1
公开(公告)日：2012-03-29
申请号：US13217636
申请日：2011-08-25
申请人： Takuji BANDO , Satoshi AOKI , Junichi KAWASAKI , Makoto ISHIGAMI , Youichi TANIGUCHI , Tsuyoshi YABUUCHI , Kiyoshi FUJIMOTO , Yoshihiro NISHIOKA , Noriyuki KOBAYASHI , Tsutomu FUJIMURA , Masanori TAKAHASHI , Kaoru ABE , Tomonori NAKAGAWA , Koichi SHINHAMA , Naoto UTSUMI , Michiaki TOMINAGA , Yoshihiro OOI , Shohei YAMADA , Kenji TOMIKAWA
发明人： Takuji BANDO , Satoshi AOKI , Junichi KAWASAKI , Makoto ISHIGAMI , Youichi TANIGUCHI , Tsuyoshi YABUUCHI , Kiyoshi FUJIMOTO , Yoshihiro NISHIOKA , Noriyuki KOBAYASHI , Tsutomu FUJIMURA , Masanori TAKAHASHI , Kaoru ABE , Tomonori NAKAGAWA , Koichi SHINHAMA , Naoto UTSUMI , Michiaki TOMINAGA , Yoshihiro OOI , Shohei YAMADA , Kenji TOMIKAWA
IPC分类号： A61K31/496 , A61P25/00 , A61P25/24 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/20 , A61P25/30 , A61P25/32 , A61P1/08 , A61P3/04 , A61P25/06 , B29C67/24 , C07D401/12
CPC分类号： C07D215/227
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the aripiprazole anhydride crystals is stored for an extended period.
摘要翻译：本发明提供低吸湿形式的阿立哌唑及其制备方法，即使当含有阿立哌唑酐晶体的药物制剂长时间储存时，其也不会转化为水合物或丧失其原始溶解度。

9. 发明申请

US20120016123A1 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof 有权
标题翻译：低吸湿性阿立哌唑药物及其制备方法
公开(公告)号：US20120016123A1
公开(公告)日：2012-01-19
申请号：US13067750
申请日：2011-06-23
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： C07D401/12
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
摘要翻译：本发明提供低吸湿形式的阿立哌唑及其制备方法，即使当含有无水阿立哌唑晶体的药物制剂长时间储存时，其也不会转化为水合物或丧失其原始溶解度。

10. 发明申请

US20120000998A1 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof 有权
公开(公告)号：US20120000998A1
公开(公告)日：2012-01-05
申请号：US13067838
申请日：2011-06-29
申请人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
发明人： Takuji Bando , Satoshi Aoki , Junichi Kawasaki , Makoto Ishigami , Youichi Taniguchi , Tsuyoshi Yabuuchi , Kiyoshi Fujimoto , Yoshihiro Nishioka , Noriyuki Kobayashi , Tsutomu Fujimura , Masanori Takahashi , Kaoru Abe , Tomonori Nakagawa , Koichi Shinhama , Naoto Utsumi , Michiaki Tominaga , Yoshihiro Ooi , Shohei Yamada , Kenji Tomikawa
IPC分类号： B02C23/18
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.

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