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    Ab1 KINASE INHIBITORS
    41.
    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。

    Staurosporin derivatives
    47.
    发明授权
    Staurosporin derivatives 失效
    星孢菌素衍生物

    公开(公告)号：US06806266B1

    公开(公告)日：2004-10-19

    申请号：US10030618

    申请日：2002-01-11

    申请人： Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

    发明人： Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

    IPC分类号： C07D49822

    CPC分类号： C07D498/22 ,  A61K31/553

    摘要： The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.

    摘要翻译： 本发明提供包含星形孢菌素衍生物或其药学上可接受的盐作为活性成分的抗肿瘤剂，其由通式（I）表示：其中R 1表示氢，羟基或低级烷氧基，R 2 和R 3相同或不同，表示氢，取代或未取代的烷基，取代或未取代的低级烯基，取代或未取代的低级炔基，取代或未取代的芳基，取代或未取代的杂环基，卤素，硝基，甲酰基， 等等，R 4表示氢等，R 5表示NR 11A R 12A（其中R 11A和R 12A表示氢，取代或未取代的低级烷基等）， 条件是R 2和R 3不同时为氢。

    2-piperidone compounds
    48.
    发明授权
    2-piperidone compounds 失效
    2-哌啶酮化合物

    公开(公告)号：US06492392B1

    公开(公告)日：2002-12-10

    申请号：US09481542

    申请日：2000-01-12

    申请人： Yutaka Kanda ,  Rieko Tanaka ,  Mitsunobu Hara ,  Jun Eishima ,  Shiro Akinaga ,  Tadashi Ashizawa

    发明人： Yutaka Kanda ,  Rieko Tanaka ,  Mitsunobu Hara ,  Jun Eishima ,  Shiro Akinaga ,  Tadashi Ashizawa

    IPC分类号： A61K31445

    CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D405/14 ,  C07D409/14

    摘要： The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I): wherein R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.

    摘要翻译： 本发明提供了具有抑制肿瘤细胞增殖的有效活性的2-哌啶酮化合物或其药学上可接受的盐，因此可用作药物，以及含有这些化合物的抗肿瘤剂。 2-哌啶酮化合物由下式（I）表示：其中R1表示 - （CH2）nR1a {其中n为0-5的整数，R1a表示氨基，低级烷基氨基，二（低级烷基）氨基，取代的 或未取代的芳基，或取代或未取代的杂环基}，R2和R3独立地表示可以被低级烷氧基羰基取代的低级烷基; 可被取代或未取代的芳基或取代或未取代的杂环基取代的低级烯基，芳烷基或低级炔基; 取代或未取代的芳基; 或取代或未取代的杂环基。

    Radicicol derivatives
    49.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号：US06316491B1

    公开(公告)日：2001-11-13

    申请号：US09091752

    申请日：1998-06-24

    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： A61K3135

    CPC分类号： C07D493/04 ,  C07D313/00

    摘要： Radioicol 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 CONR6R7 (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： 由具有酪氨酸激酶抑制活性的下式（I）表示的放射性标记衍生物或其药理学上可接受的盐：其中R1和R2相同或不同，并且各自表示氢，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; R3表示Y-R5（其中Y表示取代或未取代的亚烷基; R5表示CONR6R7（其中R6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; R7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 4一起表示单键; 并且R 4与X结合以表示单键，或表示氢，烷酰基等。