公开(公告)号：US20140228567A1

公开(公告)日：2014-08-14

申请号：US14128305

申请日：2012-06-29

申请人： Takuji Bando ,  Katsuhiko Yano ,  Makoto Fukana ,  Satoshi Aoki

发明人： Takuji Bando ,  Katsuhiko Yano ,  Makoto Fukana ,  Satoshi Aoki

IPC分类号： C07D215/22

CPC分类号： C07D215/22

摘要： The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.

摘要翻译： 本发明提供了一种制备阿立哌唑酐晶体B的微粒的新方法。阿立哌唑酐晶体B的微粒的制造方法包括以下步骤：（1）将阿立哌唑粗制物加热溶解在低级醇中， 得到的混合物沉淀出晶体，得到阿立哌唑低级醇溶剂化物晶体; （2）使阿立哌唑低级醇溶剂化物的晶体以含有低级醇的浆液的形式进行湿磨; 和（3）将经湿磨的晶体的分散液进行固液分离，得到晶体，并加热晶体。

公开(公告)号：US09278934B2

公开(公告)日：2016-03-08

申请号：US14128305

申请日：2012-06-29

申请人： Takuji Bando ,  Katsuhiko Yano ,  Makoto Fukana ,  Satoshi Aoki

发明人： Takuji Bando ,  Katsuhiko Yano ,  Makoto Fukana ,  Satoshi Aoki

IPC分类号： C07D401/12 ,  C07D403/02 ,  C07D215/22

CPC分类号： C07D215/22

摘要： The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.

摘要翻译： 本发明提供了一种制备阿立哌唑酐晶体B的微粒的新方法。阿立哌唑酐晶体B的微粒的制造方法包括以下步骤：（1）将阿立哌唑粗制物加热溶解在低级醇中， 得到的混合物沉淀出晶体，得到阿立哌唑低级醇溶剂化物晶体; （2）使阿立哌唑低级醇溶剂化物的晶体以含有低级醇的浆液的形式进行湿磨; 和（3）将经湿磨的晶体的分散液进行固液分离，得到晶体，并加热晶体。

公开(公告)号：US08703772B2

公开(公告)日：2014-04-22

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： A61K31/497 ,  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。

公开(公告)号：US07910589B2

公开(公告)日：2011-03-22

申请号：US11790606

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： 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.

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。

公开(公告)号：US20070213343A1

公开(公告)日：2007-09-13

申请号：US11790603

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： A61K31/496 ,  C07D401/10

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 aripiprazole anhydride crystals is stored for an extended period.

公开(公告)号：US08901130B2

公开(公告)日：2014-12-02

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 ,  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 ,  C07D401/14 ,  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丧失其原始溶解度。

公开(公告)号：US08642760B2

公开(公告)日：2014-02-04

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。

公开(公告)号：US20070213344A1

公开(公告)日：2007-09-13

申请号：US11790606

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： 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 aripiprazole anhydride crystals is stored for an extended period.

公开(公告)号：US20070203151A1

公开(公告)日：2007-08-30

申请号：US11797024

申请日：2007-04-30

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 aripiprazole anhydride crystals is stored for an extended period.

公开(公告)号：US08901303B2

公开(公告)日：2014-12-02

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： C07D401/06 ,  C07D215/227 ,  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.