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公开(公告)号：EP1999128B1
公开(公告)日：2010-08-04
申请号：EP07739373.4
申请日：2007-03-15
IPC分类号： C07D417/04 , A61K31/4439 , A61P11/00
CPC分类号： A61K31/4436 , C07D417/04
摘要： The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions.
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2.发明授权
公开(公告)号：EP2841431B1
公开(公告)日：2017-01-04
申请号：EP13722129.7
申请日：2013-04-23
发明人： YAMASHITA, Hiroshi , SATO, Tetsuya , MINOWA, Takuya , HOSHIKA, Yusuke , TOYOFUKU, Hidekazu , YAMAGUCHI, Tatsuya , SOTA, Masahiro , KAWANO, Shuuji , NAKAMURA, Takayuki , ETO, Ryohei , IKEBUCHI, Takuma , MORIYAMA, Kei , ITO, Nobuaki
IPC分类号： C07D409/12 , A61K31/4704 , A61P25/00
CPC分类号： C07D409/12
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3.发明授权METHOD FOR PRODUCING BENZO[B] THIOPHENE COMPOUNDS 有权VERFAHREN ZUR HERSTELLUNG VON BENZO [B] THIOPHEN-VERBINDUNGEN
公开(公告)号：EP2736894B1
公开(公告)日：2016-08-31
申请号：EP12748265.1
申请日：2012-07-27
IPC分类号： C07D333/54 , C07D409/12 , C07B61/00
CPC分类号： C07D409/12 , C07D333/54 , Y02P20/55
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公开(公告)号：EP1999128A1
公开(公告)日：2008-12-10
申请号：EP07739373.4
申请日：2007-03-15
IPC分类号： C07D417/04 , A61K31/4439 , A61P11/00
CPC分类号： A61K31/4436 , C07D417/04
摘要： The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions.
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