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    INDOLINE DERIVATIVES
    6.
    发明申请
    INDOLINE DERIVATIVES 失效
    吲哚衍生物

    公开(公告)号：US20110294850A1

    公开(公告)日：2011-12-01

    申请号：US13148011

    申请日：2010-02-03

    申请人： Hachiro Sugimoto ,  Jun Takahashi ,  Takashi Takahashi ,  Ichiro Hijikuro

    发明人： Hachiro Sugimoto ,  Jun Takahashi ,  Takashi Takahashi ,  Ichiro Hijikuro

    IPC分类号： A61K31/475 ,  C07D403/06 ,  C07D405/12 ,  C07D401/12 ,  A61P25/00 ,  C07D403/12 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/454 ,  A61P25/28 ,  C07D209/08 ,  C07D401/06

    CPC分类号： C07D405/14 ,  C07D209/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.

    摘要翻译： 本发明提供具有优异的丁酰胆碱酯酶抑制活性的新型二氢吲哚衍生物或其药理学上可接受的盐或其由下式（1）表示的衍生物或其盐的溶剂合物。 在该式中，R 1表示烷基，环烷基，杂环烷基，芳基，杂芳基，芳烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基，二氢呋喃基烷基，烯基， 四氢萘基或茚满基; R2表示氢原子，烷基，芳基烷基，环烷基烷基，杂芳基烷基，杂环烷基烷基，芳基或酰基; R3各自独立地表示氢原子，烷基或二烷基氨基羰基; R4各自独立地表示氢原子或烷基; R 5表示氢原子或烷基。 每个官能团可以具有取代基。

    Indoline derivatives
    8.
    发明授权
    Indoline derivatives 失效
    二氢吲哚衍生物

    公开(公告)号：US08686024B2

    公开(公告)日：2014-04-01

    申请号：US13148011

    申请日：2010-02-03

    申请人： Hachiro Sugimoto ,  Jun Takahashi ,  Takashi Takahashi ,  Ichiro Hijikuro

    发明人： Hachiro Sugimoto ,  Jun Takahashi ,  Takashi Takahashi ,  Ichiro Hijikuro

    IPC分类号： A61K31/404 ,  C07D209/10

    CPC分类号： C07D405/14 ,  C07D209/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.

    摘要翻译： 本发明提供具有优异的丁酰胆碱酯酶抑制活性的新型二氢吲哚衍生物或其药理学上可接受的盐或其由下式（1）表示的衍生物或其盐的溶剂合物。 在该式中，R 1表示烷基，环烷基，杂环烷基，芳基，杂芳基，芳烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基，二氢呋喃基烷基，烯基， 四氢萘基或茚满基; R2表示氢原子，烷基，芳基烷基，环烷基烷基，杂芳基烷基，杂环烷基烷基，芳基或酰基; R3各自独立地表示氢原子，烷基或二烷基氨基羰基; R4各自独立地表示氢原子或烷基; R 5表示氢原子或烷基。 每个官能团可以具有取代基。

    LOW-VISCOSITY LIQUID CRYSTAL COMPOUND
    9.
    发明申请
    LOW-VISCOSITY LIQUID CRYSTAL COMPOUND 有权
    低粘度液晶化合物

    公开(公告)号：US20120264923A1

    公开(公告)日：2012-10-18

    申请号：US13518932

    申请日：2010-12-27

    申请人： Yutaka Ikeda ,  Jun Yamashita ,  Ichiro Hijikuro ,  Satoshi Imuta ,  Yasuhiro HIroki ,  Takashi Takahashi

    发明人： Yutaka Ikeda ,  Jun Yamashita ,  Ichiro Hijikuro ,  Satoshi Imuta ,  Yasuhiro HIroki ,  Takashi Takahashi

    IPC分类号： C07C57/03 ,  C07H15/10

    CPC分类号： A61K47/14 ,  A61K9/0019 ,  A61K9/0024 ,  A61K47/08 ,  A61K47/10 ,  A61K47/22 ,  A61K47/26 ,  C07H15/10 ,  C09K19/06

    摘要： The present invention relates to a liquid crystal compound that can be used as a base for injection formulations. The present invention provides an amphipathic compound having the following general formula (I): wherein X and Y each denotes a hydrogen atom or together denote an oxygen atom, n denotes an integer from 0 to 2, m denotes the integer 1 or 2, and R denotes a hydrophilic group generated by removal of one hydroxyl group from any one selected from the group consisting of glycerol, erythritol, pentaerythritol, diglycerol, triglycerol, xylose, sorbitol, ascorbic acid, glucose, galactose, mannose, dipentaerythritol, maltose, mannitol, and xylitol; as well as a base for injection formulations and depot formulation comprising the same.

    摘要翻译： 本发明涉及可用作注射制剂的基质的液晶化合物。 本发明提供具有以下通式（I）的两亲化合物：其中X和Y各自表示氢原子或一起表示氧原子，n表示0至2的整数，m表示整数1或2，并且 R表示通过从选自甘油，赤藓糖醇，季戊四醇，双甘油，三甘油，木糖，山梨醇，抗坏血酸，葡萄糖，半乳糖，甘露糖，二季戊四醇，麦芽糖，甘露糖醇，甘露糖醇， 和木糖醇; 以及用于注射制剂的基料和包含其的包含药剂的制剂。

    Low-viscosity liquid crystal compound
    10.
    发明授权
    Low-viscosity liquid crystal compound 有权
    低粘度液晶复合物

    公开(公告)号：US08703922B2

    公开(公告)日：2014-04-22

    申请号：US13518932

    申请日：2010-12-27

    申请人： Yutaka Ikeda ,  Jun Yamashita ,  Ichiro Hijikuro ,  Satoshi Imuta ,  Yasuhiro Hiroki ,  Takashi Takahashi

    发明人： Yutaka Ikeda ,  Jun Yamashita ,  Ichiro Hijikuro ,  Satoshi Imuta ,  Yasuhiro Hiroki ,  Takashi Takahashi

    IPC分类号： C07H15/00 ,  C07H15/04 ,  A61K31/70 ,  A61K31/7028 ,  C07C57/03

    CPC分类号： A61K47/14 ,  A61K9/0019 ,  A61K9/0024 ,  A61K47/08 ,  A61K47/10 ,  A61K47/22 ,  A61K47/26 ,  C07H15/10 ,  C09K19/06

    摘要： The present invention relates to a liquid crystal compound that can be used as a base for injection formulations. The present invention provides an amphipathic compound having the following general formula (I): wherein X and Y each denotes a hydrogen atom or together denote an oxygen atom, n denotes an integer from 0 to 2, m denotes the integer 1 or 2, and R denotes a hydrophilic group generated by removal of one hydroxyl group from any one selected from the group consisting of glycerol, erythritol, pentaerythritol, diglycerol, triglycerol, xylose, sorbitol, ascorbic acid, glucose, galactose, mannose, dipentaerythritol, maltose, mannitol, and xylitol; as well as a base for injection formulations and depot formulation comprising the same.

    摘要翻译： 本发明涉及可用作注射制剂的基质的液晶化合物。 本发明提供具有以下通式（I）的两亲化合物：其中X和Y各自表示氢原子或一起表示氧原子，n表示0至2的整数，m表示整数1或2，并且 R表示通过从选自甘油，赤藓糖醇，季戊四醇，双甘油，三甘油，木糖，山梨醇，抗坏血酸，葡萄糖，半乳糖，甘露糖，二季戊四醇，麦芽糖，甘露糖醇，甘露糖醇， 和木糖醇; 以及用于注射制剂的基料和包含其的包含药剂的制剂。