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    Tetomilast polymorphs
    3.
    发明授权
    Tetomilast polymorphs 有权
    替托司特多晶型物

    公开(公告)号：US09145404B2

    公开(公告)日：2015-09-29

    申请号：US14145260

    申请日：2013-12-31

    申请人： Otsuka Pharmaceutical Co., Ltd.

    发明人： Satoshi Aoki ,  Kenji Nakaya ,  Masahiro Sota ,  Masashi Ishigami

    IPC分类号： C07D417/04

    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 power 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 FIGS. 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.

    摘要翻译： 本发明提供了一种工业上易于大量生产的替托司特晶体。 （1）具有与图1所示的粉末X射线衍射光谱基本相同的功率X射线衍射光谱的替托司他水合物晶体。 2; （2）具有与图1所示的粉末X射线衍射光谱基本相同的粉末X射线衍射光谱的无水替托司特A型晶体。 4; （3）具有粉末X射线衍射光谱的无水替托司特C型晶体，其与图1所示的粉末X射线衍射光谱基本相同。 8; （4）具有粉末X射线衍射光谱的替托司特乙腈溶剂合物晶体，其与图1和图2所示的粉末X射线衍射光谱基本相同。 10; 和（5）由上述无水替托司特A型晶体和无水替托司特B型晶体组成的混合物。 这些晶体对于热和水分是稳定的，并且在片剂的崩解性和溶解性方面也是优异的。 因此，这些晶体优选用作药物组合物。

    Tetomilast polymorphs
    4.
    发明授权
    Tetomilast polymorphs 有权
    替托司特多晶型物

    公开(公告)号：US08993601B2

    公开(公告)日：2015-03-31

    申请号：US13784652

    申请日：2013-03-04

    申请人： Otsuka Pharmaceutical Co., Ltd.

    发明人： Satoshi Aoki ,  Kenji Nakaya ,  Masahiro Sota ,  Masashi Ishigami

    IPC分类号： A61K31/4436 ,  C07D417/04

    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 power 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.

    摘要翻译： 本发明提供了一种工业上易于大量生产的替托司特晶体。 （1）具有与图1所示的粉末X射线衍射光谱基本相同的功率X射线衍射光谱的替托司他水合物晶体。 2; （2）具有与图1所示的粉末X射线衍射光谱基本相同的粉末X射线衍射光谱的无水替托司特A型晶体。 4; （3）粉末X射线衍射光谱与图1所示的粉末X射线衍射光谱基本相同的无水替托司特C型晶体。 8; （4）具有与图1所示的粉末X射线衍射光谱基本相同的粉末X射线衍射光谱的替托司特乙腈溶剂合物晶体。 10; 和（5）由上述无水替托司特A型晶体和无水替托司特B型晶体组成的混合物。 这些晶体对于热和水分是稳定的，并且在片剂的崩解性和溶解性方面也是优异的。 因此，这些晶体优选用作药物组合物。