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公开(公告)号：US10150735B2
公开(公告)日：2018-12-11
申请号：US14624595
申请日：2015-02-18
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： C07D215/227 , C07D215/22
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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公开(公告)号：US08552188B2
公开(公告)日：2013-10-08
申请号：US13677727
申请日：2012-11-15
发明人： Hidetsugu Tsubouchi , Yoshikazu Haraguchi , Satoshi Hayakawa , Naoto Utsumi , Shinichi Taira , Yoshihisa Tanada , Nobuhisa Fujita , Koichi Shinhama , Kimiyoshi Annaka , Takuya Furuta
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D303/18 , C07D498/04
摘要： The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.
摘要翻译： 本发明提供了一种制备具有高产率和高纯度的2,3-二氢咪唑并[2,1-b]恶唑化合物的新型中间体及其制备方法。 本发明提供由通式（2）表示的环氧化合物：其中，R1表示氢或低级烷基; R 2表示由通式（A1）表示的哌啶基：（其中，R3表示在苯基取代的卤素取代的低级烷氧基的苯氧基等）等。 n表示1〜6的整数，环氧化合物的制造方法和使用环氧方法的恶唑化合物的制造方法。
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公开(公告)号：US20140030523A1
公开(公告)日：2014-01-30
申请号：US13749753
申请日：2013-01-25
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： C07D215/227
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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公开(公告)号：US20130072683A1
公开(公告)日：2013-03-21
申请号：US13677727
申请日：2012-11-15
发明人： Hidetsugu Tsubouchi , Yoshikazu Haraguchi , Satoshi Hayakawa , Naoto Utsumi , Shinichi Taira , Yoshihisa Tanada , Nobuhisa Fujita , Koichi Shinhama , Kimiyoshi Annaka , Takuya Furuta
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D303/18 , C07D498/04
摘要： The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.
摘要翻译： 本发明提供了一种制备具有高产率和高纯度的2,3-二氢咪唑并[2,1-b]恶唑化合物的新型中间体及其制备方法。 本发明提供由通式（2）表示的环氧化合物：其中，R1表示氢或低级烷基; R 2表示由通式（A1）表示的哌啶基：（其中，R3表示在苯基取代的卤素取代的低级烷氧基的苯氧基等）等。 n表示1〜6的整数，环氧化合物的制造方法和使用环氧方法的恶唑化合物的制造方法。
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5.发明授权公开(公告)号：US08993761B2
公开(公告)日：2015-03-31
申请号：US13749753
申请日：2013-01-25
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： C07D403/12 , C07D215/227
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失去其原始溶解度。
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公开(公告)号：US09359302B2
公开(公告)日：2016-06-07
申请号：US14049777
申请日：2013-10-09
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 , C07D215/22 , C07D215/227
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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