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    TETOMILAST POLYMORPHS
    1.
    发明公开
    TETOMILAST POLYMORPHS 有权
    替托，多形性

    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

    申请人： OTSUKA PHARMACEUTICAL CO., LTD.

    发明人： AOKI, Satoshi ,  NAKAYA, Kenji ,  SOTA, Masahiro ,  ISHIGAMI, Masashi

    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.

    METHOD FOR PRODUCING FINE PARTICLES OF ARIPIPRAZOLE ANHYDRIDE CRYSTALS B
    2.
    发明公开
    METHOD FOR PRODUCING FINE PARTICLES OF ARIPIPRAZOLE ANHYDRIDE CRYSTALS B 审中-公开
    生产ARIPIPRAZOLE ANHYDRIDE晶体的细颗粒的方法B

    公开(公告)号：EP2726461A1

    公开(公告)日：2014-05-07

    申请号：EP12748263.6

    申请日：2012-06-29

    申请人： Otsuka Pharmaceutical Co., Ltd.

    发明人： BANDO, Takuji ,  YANO, Katsuhiko ,  FUKANA, Makoto ,  AOKI, Satoshi

    IPC分类号： C07D215/22 ,  A61K31/4704 ,  A61P25/18

    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： 本发明提供了制备阿立哌唑无水物晶体B微粒的新方法。制备阿立哌唑无水物晶体B微粒的方法包括以下步骤：（1）将粗阿立哌唑加热溶解在低级醇中，随后冷却 得到的混合物沉淀结晶，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合物的晶体以含有低级醇的浆料的形式进行湿磨; （3）将湿磨晶体的分散体进行固液分离以获得晶体，并加热晶体。

    TETOMILAST POLYMORPHS
    3.
    发明授权
    TETOMILAST POLYMORPHS 有权
    替托，多晶型

    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

    申请人： OTSUKA PHARMACEUTICAL CO., LTD.

    发明人： AOKI, Satoshi ,  NAKAYA, Kenji ,  SOTA, Masahiro ,  ISHIGAMI, Masashi

    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.