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    INDOLINE DERIVATIVES
    1.
    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
    2.
    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。