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    Indolopyrrolocarbazole derivatives
    32.
    发明授权
    Indolopyrrolocarbazole derivatives 失效
    吲哚并吡咯并咔唑衍生物

    公开(公告)号：US5668271A

    公开(公告)日：1997-09-16

    申请号：US474659

    申请日：1995-06-07

    申请人： Katsuhisa Kojiri ,  Hisao Kondo ,  Hiroharu Arakawa ,  Mitsuru Ohkubo ,  Hiroyuki Suda

    发明人： Katsuhisa Kojiri ,  Hisao Kondo ,  Hiroharu Arakawa ,  Mitsuru Ohkubo ,  Hiroyuki Suda

    IPC分类号： C07H19/044 ,  C07H19/23 ,  C07D273/00

    CPC分类号： C07H19/044

    摘要： Indolopyrrocarbazole derivatives represented by formula (I) and the pharmaceutically acceptable salts thereof have excellent antitumor activity as evidenced by their in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell, ##STR1## wherein R.sup.1 and R.sup.2 independently represent, for example, a hydrogen atom or various hydrocarbon groups which may be substituted or heterocyclic groups which may also be substituted; or a group --Y--R.sup.3 where Y represents a carbonyl group, thiocarbonyl group or sulfonyl group and R.sup.3 represents a hydrogen atom or one of various aliphatic, cycloaliphatic, aryl, nitrogen-containing (e.g. amino, hydrazino, etc) or heterocyclic groups, which groups may be substituted by various substituents; or R.sup.1 and R.sup.2 may combine to represent a lower alkylidene group which may be substituted; or R.sup.1 and R.sup.2, together with the N-atom to which they are bonded form a heterocyclic group which may be substituted;G represents a pentose or hexose group; and X.sup.1 and X.sup.2, independently, represent, for example, hydrogen, halogen, amino, hydroxyl, alkoxy, aryloxy, carboxyl, alkoxycarbonyl or alkyl. These compounds have improved water solubility as compared to rebeccamycin.

    摘要翻译： 由式（I）表示的吲哚并吡咔唑衍生物及其药学上可接受的盐具有优异的抗肿瘤活性，如通过其对小鼠白血病细胞，人胃癌细胞，人肺癌细胞和人结肠癌细胞的体外增殖抑制活性所证明的。 其中R1和R2独立地表示例如氢原子或可以是取代的各种烃基或也可以被取代的杂环基; 或其中Y表示羰基，硫代羰基或磺酰基且R 3表示氢原子或各种脂族，脂环族，芳基，含氮（例如氨基，肼基等）或杂环基之一的基团-Y-R3， 哪些基团可以被各种取代基取代; 或者R 1和R 2可以组合以表示可被取代的低级亚烷基; 或R 1和R 2与它们所键合的N-原子一起形成可被取代的杂环基; G表示戊糖或己糖基团; X 1和X 2独立地表示例如氢，卤素，氨基，羟基，烷氧基，芳氧基，羧基，烷氧基羰基或烷基。 与雷贝卡霉素相比，这些化合物具有改善的水溶性。

    Aminopyridine derivatives having aurora a selective inhibitory action
    34.
    发明授权
    Aminopyridine derivatives having aurora a selective inhibitory action 有权
    具有极光选择性抑制作用的氨基吡啶衍生物

    公开(公告)号：US08367690B2

    公开(公告)日：2013-02-05

    申请号：US13259620

    申请日：2010-03-15

    申请人： Hayley Binch ,  Masaya Hashimoto ,  Michael Mortimore ,  Mitsuru Ohkubo ,  Tomoko Sunami

    发明人： Hayley Binch ,  Masaya Hashimoto ,  Michael Mortimore ,  Mitsuru Ohkubo ,  Tomoko Sunami

    IPC分类号： A01N43/54 ,  A61K31/505

    CPC分类号： A61K31/535 ,  C07D401/14 ,  C07D417/14

    摘要： The present invention relates to a compound of Formula (I): wherein: R1 is H, —NHCOOR1a, C5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R10; R1a is C1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R2 is H, —COOH, —CH2 COOH, —COOR2a, or —CH2COOR2a; R2a is C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R3 is H, C1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R11; R10 is F, Cl, CF3, or C1-2 alkyl; R11 is halogen atom, hydroxy, or cyano; W is selected from: W2a is H, halogen atom, cyano, C1-2 alkyl, or C3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译： 本发明涉及式（I）的化合物：其中：R1是H，-NHCOOR1a，C5-6环烷基或苯基; 其中环烷基和苯基各自独立地可以被一至三个相同或不同的选自R 10的取代基取代; R 1a是可以被一至三个相同或不同的选自F和Cl的取代基取代的C 1-3烷基; R2是H，-COOH，-CH2COOH，-COOR2a或-CH2COOR2a; R2a是C1-2烷基，其中烷基可以被一至三个相同或不同的选自卤素原子的取代基取代; R3是H，C1-6烷基，其中烷基可以被一至三个相同或不同的选自R11的取代基取代; R 10是F，Cl，CF 3或C 1-2烷基; R11是卤素原子，羟基或氰基; W选自：W2a是H，卤素原子，氰基，C1-2烷基或C3-5环烷基，或其药学上可接受的盐或酯。

    Indolopyrrolocarbazole derivatives and anti-tumor agent
    36.
    发明申请
    Indolopyrrolocarbazole derivatives and anti-tumor agent 审中-公开
    吲哚并咔唑衍生物和抗肿瘤剂

    公开(公告)号：US20080113927A1

    公开(公告)日：2008-05-15

    申请号：US12008145

    申请日：2008-01-09

    申请人： Mitsuru Ohkubo ,  Hiroharu Arakawa

    发明人： Mitsuru Ohkubo ,  Hiroharu Arakawa

    IPC分类号： A61K31/7056 ,  C07H19/22

    CPC分类号： A61K31/706 ,  A61K31/7056 ,  C07H17/02

    摘要： The present invention relates to new indolopyrrolocarbazole derivatives of formula (I): wherein R represents an unsubstitued pyridyl, furyl, or thienyl group; m represents an integer of 1 to 3; and G represents a β-D-glucopyranosyl group; and the positions of substitution of the hydroxyl groups on the indolopyrrolocarbazole ring are the 1- and 11-positions, or the 2- and 10-positions.

    摘要翻译： 本发明涉及式（I）的新的吲哚并吡咯并唑衍生物：其中R表示未取代的吡啶基，呋喃基或噻吩基; m表示1〜3的整数， G代表β-D-吡喃葡萄糖基; 并且吲哚吡咯并咔唑环上的羟基的取代位置是1位和11位，或2-和10-位。

    Novel indolopyrrolocarbazole derivative with antitumor activity
    37.
    发明申请
    Novel indolopyrrolocarbazole derivative with antitumor activity 审中-公开
    具有抗肿瘤活性的新型吲哚并吡咯并咔唑衍生物

    公开(公告)号：US20070042975A1

    公开(公告)日：2007-02-22

    申请号：US10571861

    申请日：2004-09-14

    申请人： Koji Yamada ,  Satoshi Sunami ,  Masaaki Hirose ,  Mitsuru Ohkubo ,  Hiroharu Arakawa

    发明人： Koji Yamada ,  Satoshi Sunami ,  Masaaki Hirose ,  Mitsuru Ohkubo ,  Hiroharu Arakawa

    IPC分类号： A61K31/7056 ,  C07H19/22

    CPC分类号： A61K31/7056

    摘要： The present invention relates to a novel indolopyrrolocarbazole derivative which is represented by the formula [I]: wherein: A represents O, NH, or CH2; R1 represents a single bond, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, etc.; R2 represents a phenyl group, a naphthyl group, or a five- or six-membered aromatic or aliphatic heterocyclic ring having at least one atom selected from N, S, or O, wherein the phenyl group, naphthyl group, aromatic or aliphatic heterocyclic ring may be substituted; and G represents a hexose group or a pentose group, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及由式[I]表示的新型吲哚并吡咯并唑衍生物：其中：A表示O，NH或CH 2。 R 1表示单键，低级烷基，低级烯基，低级炔基等; R 2表示具有至少一个选自N，S或O的原子的苯基，萘基或五元或六元芳族或脂族杂环，其中苯基， 萘基，芳族或脂肪族杂环可以被取代; G表示己糖基或戊糖基，或其药学上可接受的盐。

    Indolopyrrolocabazole derivative and antitumor agent
    39.
    发明申请
    Indolopyrrolocabazole derivative and antitumor agent 审中-公开
    吲哚并咔唑衍生物和抗肿瘤剂

    公开(公告)号：US20060189800A1

    公开(公告)日：2006-08-24

    申请号：US10565326

    申请日：2004-07-21

    申请人： Mitsuru Ohkubo ,  Hiroharu Arakawa

    发明人： Mitsuru Ohkubo ,  Hiroharu Arakawa

    IPC分类号： A61K31/7056 ,  C07H19/22

    CPC分类号： C07H19/22

    摘要： The present invention relates to new indolopyrrolocarbazole derivatives of formula (I): wherein R represents an unsubstitued pyridyl, furyl, or thienyl group; m represents an integer of 1 to 3; and G represents a β-D-glucopyranosyl group; and the positions of substitution of the hydroxyl groups on the indolopyrrolocarbazole ring are the 1- and 11-positions, or the 2- and 10-positions.

    摘要翻译： 本发明涉及式（I）的新的吲哚并吡咯并唑衍生物：其中R表示未取代的吡啶基，呋喃基或噻吩基; m表示1〜3的整数， G代表β-D-吡喃葡萄糖基; 并且吲哚吡咯并咔唑环上的羟基的取代位置是1位和11位，或2-和10-位。