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    Indazole derivatives
    4.
    发明申请
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US20070117856A1

    公开(公告)日：2007-05-24

    申请号：US10548475

    申请日：2004-07-30

    申请人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    发明人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56

    摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    摘要翻译： 本发明提供由式（I）表示的化合物：[其中R 1表示CONR 1a 1b 1b（其中R 1a） R 1b和R 1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基， 或R 1a和R 1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R 2 O， >表示氢原子，其中R 2a，R 2b和R 2b可以相同或不同， 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 2b和R 2b >与t结合在一起 它与氮原子相邻以形成取代或未取代的杂环基），NR 2c R 2d（其中R 2c和R 2d） 取代或未取代的低级烷酰基，取代或未取代的芳酰基，取代或未取代的杂芳酰基，取代或未取代的芳烷基，取代或未取代的低级烷基磺酰基或 取代或未取代的低级芳基磺酰基等）。

    Indazole derivatives
    5.
    发明授权
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US07919517B2

    公开(公告)日：2011-04-05

    申请号：US12275614

    申请日：2008-11-21

    申请人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    发明人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56

    摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    摘要翻译： 本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的 芳基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳基或取代或未取代的杂环基，或者R 2a和R 2b与相邻的氮原子一起形成取代基 或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同 取代或未取代的杂芳酰基，取代或未取代的芳酰基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等，其中R 1表示氢原子，取代或未取代的低级烷基，取代或未取代的低级烷酰基，取代或未取代的芳酰基， 。

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

    公开(公告)号：US20090082348A1

    公开(公告)日：2009-03-26

    申请号：US12275614

    申请日：2008-11-21

    申请人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    发明人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC分类号： A61K31/5377 ,  A61K31/416 ,  A61K31/496 ,  A61K31/454 ,  A61K31/506 ,  A61K31/4439 ,  A61P35/00

    CPC分类号： C07D231/56

    摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    摘要翻译： 本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的 芳基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳基或取代或未取代的杂环基，或者R 2a和R 2b与相邻的氮原子一起形成取代基 或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同 取代或未取代的芳酰基，取代或未取代的芳酰基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等。 。

    Indazole derivatives
    7.
    发明授权
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US07470717B2

    公开(公告)日：2008-12-30

    申请号：US10548475

    申请日：2004-07-30

    申请人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    发明人： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56

    摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    摘要翻译： 本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的 芳烷基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 2a和R 2b与相邻的氮原子一起形成取代基 或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同 取代或未取代的杂芳酰基，取代或未取代的芳烷基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等，其中R 1代表氢原子，取代或未取代的低级烷基，取代或未取代的低级烷酰基，取代或未取代的芳酰基， 。

    AURORA INHIBITORS
    8.
    发明申请
    AURORA INHIBITORS 审中-公开
    AURORA抑制剂

    公开(公告)号：US20090209537A1

    公开(公告)日：2009-08-20

    申请号：US12305120

    申请日：2007-06-29

    申请人： Yukimasa Shiotsu ,  Kenichi Ishii ,  Hiroshi Umehara

    发明人： Yukimasa Shiotsu ,  Kenichi Ishii ,  Hiroshi Umehara

    IPC分类号： A61K31/5377 ,  A61P35/00

    CPC分类号： C07D403/10 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D231/56 ,  C07D401/06

    摘要： The present invention provides an Aurora inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group) or a pharmaceutically acceptable salt thereof, an Aurora inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (Ia) [wherein R2 represents CONR4aR4b (wherein R4a and R4b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like, or R4a and R4b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, and R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof, and the like.

    摘要翻译： 本发明提供一种Aurora抑制剂，其包含作为活性成分的由式（I）表示的吲唑衍生物（其中R 1表示取代或未取代的芳基或取代或未取代的杂环基）或其药学上可接受的盐，极光抑制剂 其包含作为活性成分的由式（Ia）表示的吲唑衍生物[其中R2表示CONR4aR4b（其中R4a和R4b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等， 或R4a和R4b与相邻的氮原子一起形成取代或未取代的杂环基）等，R 3表示氢原子，取代或未取代的低级烷基等]或其药学上可接受的盐， 等等。

    Ab1 KINASE INHIBITORS
    9.
    发明申请
    Ab1 KINASE INHIBITORS 审中-公开
    Ab1激酶抑制剂

    公开(公告)号：US20120329794A1

    公开(公告)日：2012-12-27

    申请号：US12305146

    申请日：2007-06-29

    申请人： Yukimasa Shiotsu ,  Kenichi Ishii ,  Hiroshi Umehara ,  Shiro Akinaga

    发明人： Yukimasa Shiotsu ,  Kenichi Ishii ,  Hiroshi Umehara ,  Shiro Akinaga

    IPC分类号： A61K31/416 ,  A61K31/4439 ,  C12N9/99 ,  A61K31/454 ,  A61P35/00 ,  A61P35/02 ,  A61K31/5377 ,  A61K31/496

    CPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D401/06 ,  C07D403/10 ,  C07D413/12

    摘要： The present invention provides an Abelson kinase (Abl kinase) inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group) or a pharmaceutically acceptable salt thereof,an Abl kinase inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (Ia) [wherein R2 represents CONR4aR4b (wherein R4a and R4b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like, or R4a and R4b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, and R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof, and the like.

    摘要翻译： 本发明提供了一种Abelson激酶（Abl激酶）抑制剂，其包含式（I）表示的吲唑衍生物作为活性成分（其中R 1表示取代或未取代的芳基或取代或未取代的杂环基）或其药学上可接受的盐 其包含作为活性成分的由式（Ia）表示的吲唑衍生物（其中R 2表示CONR 4 aR 4 b（其中R 4a和R 4b可以相同或不同，各自表示氢原子，取代或未取代的低级）的Abl激酶抑制剂 烷基等，或者R4a和R4b与相邻的氮原子一起形成取代或未取代的杂环基）等，R 3表示氢原子，取代或未取代的低级烷基等，或 其药学上可接受的盐等。

    Radicicol derivatives
    10.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号：US06635662B2

    公开(公告)日：2003-10-21

    申请号：US09791602

    申请日：2001-02-26

    申请人： Yoji Ino ,  Nobuyoshi Amishiro ,  Mayumi Miyata ,  Chikara Murakata ,  Harumi Ogawa ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Shiro Soga ,  Yukimasa Shiotsu

    发明人： Yoji Ino ,  Nobuyoshi Amishiro ,  Mayumi Miyata ,  Chikara Murakata ,  Harumi Ogawa ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Shiro Soga ,  Yukimasa Shiotsu

    IPC分类号： A61K3144

    CPC分类号： C07D493/04 ,  C07D313/00

    摘要： Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR5R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like} and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.

    摘要翻译： 由下式（I）表示的具有酪氨酸激酶抑制活性的衍生物衍生物或其药理学上可接受的盐：其中R 1和R 2相同或不同，各自表示氢，链烷酰基，烯酰基，叔丁基二苯基甲硅烷基或 叔丁基二甲基甲硅烷基; R 3表示Y-R 5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 5 R 7（其中R 6表示氢，羟基，取代或未取代的低级烷基，取代或未取代的高级烷基等; R 7表示羟基，取代的低级 烷基等），CO 2 R 12（其中R 12表示取代的低级烷基，取代或未取代的高级烷基等）等}等; X表示卤素或与R 4结合以表示单键;并且R 4与X一起组合以表示单键，或表示氢，烷酰基等。