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    2-substituted-6-heterocyclic pyrimidone derivatives as tau protein kinase 1 inhibitors
    1.
    发明授权
    2-substituted-6-heterocyclic pyrimidone derivatives as tau protein kinase 1 inhibitors 失效
    作为tau蛋白激酶1抑制剂的2-取代-6-杂环嘧啶酮衍生物

    公开(公告)号：US08592417B2

    公开(公告)日：2013-11-26

    申请号：US12518997

    申请日：2007-12-26

    申请人： Kazutoshi Watanabe ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Fumiaki Uehara

    发明人： Kazutoshi Watanabe ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Fumiaki Uehara

    IPC分类号： A61K31/535 ,  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 each R1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C3-C7 cycloalkyl group, a C6-C10 aryl group or a heterocyclic group; R6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R2 represents hydrogen atom or the like, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中每个R 1表示氢原子等; X表示氧原子等; A表示C 3 -C 7环烷基，C 6 -C 10芳基或杂环基; R6表示卤素原子等; s表示0或1〜5的整数， Q表示可以被取代或嘧啶环的吡啶环; R2代表氢原子等，其用于预防和/或治疗由tau蛋白激酶1的异常活性引起的疾病，例如神经变性疾病（例如阿尔茨海默病）。

    2-(cyclic amino)-pyrimidone derivatives
    3.
    发明授权
    2-(cyclic amino)-pyrimidone derivatives 失效
    2-（环状氨基） - 嘧啶酮衍生物

    公开(公告)号：US08569294B2

    公开(公告)日：2013-10-29

    申请号：US12282396

    申请日：2007-03-14

    申请人： Kenji Fukunaga ,  Toshiyuki Kohara ,  Kazutoshi Watanabe ,  Yoshihiro Usui ,  Fumiaki Uehara ,  Satoshi Yokoshima ,  Daiki Sakai ,  Shin-ichi Kusaka ,  Kazuki Nakayama

    发明人： Kenji Fukunaga ,  Toshiyuki Kohara ,  Kazutoshi Watanabe ,  Yoshihiro Usui ,  Fumiaki Uehara ,  Satoshi Yokoshima ,  Daiki Sakai ,  Shin-ichi Kusaka ,  Kazuki Nakayama

    IPC分类号： A61K31/535

    CPC分类号： C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D493/04

    摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, 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）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数， Z表示氮原子，CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数， X表示键，CH2，氧原子，NH等; R 5和R 6，R 5和R 4，R 6和R 4，X和R 5，X和R 4，X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环，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。

    2-morpholino-4-pyrimidone compound
    5.
    发明授权
    2-morpholino-4-pyrimidone compound 有权
    2-吗啉代-4-嘧啶酮化合物

    公开(公告)号：US08106045B2

    公开(公告)日：2012-01-31

    申请号：US11573476

    申请日：2005-09-09

    申请人： Kazutoshi Watanabe ,  Fumiaki Uehara ,  Shinsuke Hiki ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Satoshi Yokoshima

    发明人： Kazutoshi Watanabe ,  Fumiaki Uehara ,  Shinsuke Hiki ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Satoshi Yokoshima

    IPC分类号： A61K31/535 ,  A61K31/54 ,  C07D413/00 ,  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。

    2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHIBITORS
    8.
    发明申请
    2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHIBITORS 失效
    2-取代的6-杂环基吡啶酮衍生物作为TAU蛋白激酶1抑制剂

    公开(公告)号：US20100113775A1

    公开(公告)日：2010-05-06

    申请号：US12518997

    申请日：2007-12-26

    申请人： Kazutoshi Watanabe ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Fumiaki Uehara

    发明人： Kazutoshi Watanabe ,  Toshiyuki Kohara ,  Kenji Fukunaga ,  Fumiaki Uehara

    IPC分类号： 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 each R1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C3-C7 cycloalkyl group, a C6-C10 aryl group or a heterocyclic group; R6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R2 represents hydrogen atom or the like, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中每个R 1表示氢原子等; X表示氧原子等; A表示C 3 -C 7环烷基，C 6 -C 10芳基或杂环基; R6表示卤素原子等; s表示0或1〜5的整数， Q表示可以被取代或嘧啶环的吡啶环; R2代表氢原子等，其用于预防和/或治疗由tau蛋白激酶1的异常活性引起的疾病，例如神经变性疾病（例如阿尔茨海默病）。

    2-amino-3-(alkyl)-pyrimidone derivatives
    10.
    发明申请
    2-amino-3-(alkyl)-pyrimidone derivatives 失效
    2-氨基-3-（烷基） - 嘧啶酮衍生物

    公开(公告)号：US20050130998A1

    公开(公告)日：2005-06-16

    申请号：US11035264

    申请日：2005-01-13

    申请人： Antonio Almario Carcia ,  Ryoichi Ando ,  Keiichi Arimoto ,  Fumiaki Uehara ,  Adrien Li ,  Aya Shoda ,  Jonathan Frost ,  Kazutoshi Watanabe

    发明人： Antonio Almario Carcia ,  Ryoichi Ando ,  Keiichi Arimoto ,  Fumiaki Uehara ,  Adrien Li ,  Aya Shoda ,  Jonathan Frost ,  Kazutoshi Watanabe

    IPC分类号： A61K31/505 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/02 ,  A61P17/14 ,  A61P19/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  A61K31/513 ,  C07D43/02

    CPC分类号： A61K31/505 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

    摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β such as Alzheimer's disease.

    摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示氢原子或可以被C 6-10取代的C 1-6烷基， / SUB>芳基; R 2表示可以被取代的C 1-10烷基，可以被取代的C 2-6亚烷基，C 3-6亚烷基， 可以被取代的亚炔基，可被取代的C 3-6亚烷基或可以被取代的C 6〜6-亚芳基; 或者R 1和R 2一起形成可以被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - （CH 2 CH 2）2 - （CH 2）2 - 或 - （CH 2）2 -X-（CH 2）3 - - 其中X表示 氧原子，硫原子或可被取代的氮原子; R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 并且R 4表示任选被羟基，氨基，C 1-6 - 单烷基氨基，C 2-12-12任意取代的C 1-10烷基。 >可以被取代的二烷基氨基或C 6,10 芳基。 以及包含所述衍生物或其盐作为活性成分的药物，其用于由GSK3β如阿尔茨海默氏病的异常活性引起的神经变性疾病的预防和/或治疗性治疗。