INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
    3.
    发明申请
    INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
    用于合成药物代理的中间体化合物及其生产方法

    公开(公告)号:US20110251385A1

    公开(公告)日:2011-10-13

    申请号:US13169782

    申请日:2011-06-27

    IPC分类号: C07D413/14

    CPC分类号: C07D265/30 C07D265/32

    摘要: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification.The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification.According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

    摘要翻译: 本发明涉及由式10表示的光学活性吗啉化合物的制备方法,其包括以下步骤:其中各符号如说明书中所定义。 本发明还涉及由式55表示的化合物的制备方法,其包括以下步骤:其中每个符号如说明书中所定义。 根据本发明的制备方法,光学活性2-芳基取代的吗啉化合物和3-氧代-3-(嘧啶-4-基)丙酸酯作为合成2-(2-芳基吗啉) -4-基)-1-甲基-1H- [4,4']二嘧啶基-6-酮,其具有tau蛋白激酶1抑制活性,可用作阿尔茨海默氏病等的治疗药物,可以以高 通过工业上有利的方法得到。

    INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF

    公开(公告)号:US20110257392A1

    公开(公告)日:2011-10-20

    申请号:US13169799

    申请日:2011-06-27

    IPC分类号: C07D413/14

    CPC分类号: C07D265/30 C07D265/32

    摘要: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification.The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification.According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

    2-MORPHOLINO-4-PYRIMIDONE COMPOUND
    7.
    发明申请
    2-MORPHOLINO-4-PYRIMIDONE COMPOUND 有权
    2-吗啉-4-基吡啶酮化合物

    公开(公告)号:US20090124618A1

    公开(公告)日:2009-05-14

    申请号:US11573476

    申请日:2005-09-09

    IPC分类号: A61K31/5377 C07D413/14

    CPC分类号: C07D413/14

    摘要: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R′ represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译: 由式(I)表示的化合物,其光学活性异构体或其药学上可接受的盐:其中X表示CH或N; 表示C1-C12烷基; R2表示氢原子等; R'表示C1-C6烷基等; q表示0或1〜7的整数, Y表示C1-C6烷基等; p表示0或1〜5的整数, R表示2,3-二氢吲哚基等,其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病(例如阿尔茨海默病)引起的疾病。