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    Staurosporin derivatives
    1.
    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。

    Radicicol derivatives
    2.
    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。

    Radicicol derivatives
    3.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号：US06239168B1

    公开(公告)日：2001-05-29

    申请号：US09513472

    申请日：2000-02-25

    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： A61K31335

    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 CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl; R7 represents hydroxyl, substituted lower alkyl), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, X represents halogen.

    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R1和R2相同或不同，并且各自表示氢，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; R3表示Y-R5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 6 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; R 7表示羟基，取代的低级烷基），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，X表示 卤素。

    Radicicol derivatives
    4.
    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。

    Therapeutic agent for thrombocytopenia and indolocarbazole derivatives
    9.
    发明授权
    Therapeutic agent for thrombocytopenia and indolocarbazole derivatives 失效
    血小板减少症和吲哚并咔唑衍生物的治疗剂

    公开(公告)号：US5629304A

    公开(公告)日：1997-05-13

    申请号：US637590

    申请日：1996-04-25

    申请人： Chikara Murakata ,  Fumihiko Kanai ,  Yutaka Saitoh ,  Yukimasa Shiotsu ,  Takako Shiraki ,  Tatsuya Tamaoki ,  Shiro Akinaga ,  Masami Okabe

    发明人： Chikara Murakata ,  Fumihiko Kanai ,  Yutaka Saitoh ,  Yukimasa Shiotsu ,  Takako Shiraki ,  Tatsuya Tamaoki ,  Shiro Akinaga ,  Masami Okabe

    IPC分类号： A61K31/40 ,  A61K31/404 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  C07D403/14 ,  C07D487/14 ,  C07D487/12

    CPC分类号： C07D403/14 ,  A61K31/40 ,  A61K31/404 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  C07D487/14

    摘要： The present invention provides a method of treating thrombocytopenia, which comprises administering to a patient suffering from thrombocytopenia, an effective amount of an indolocarbazole derivative represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group or a tetrahydropyranyl group; R.sup.2A and R.sup.3A, which may be the same or different, each represent a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkenyl group, a substituted or unsubstituted aralkyl group or a monosaccharide residue where a hydroxyl group at the anomer position is removed; R.sup.4A and R.sup.5A, which may be the same or different, each represent a hydrogen atom, a formyl group, a hydroxyl group or a halogen atom; W.sup.A1 and W.sup.A2 represent hydrogen atoms or are combined together to form an oxygen atom; and X.sup.A1 and X.sup.A2 represents two hydrogen atoms or are combined together to form a single bond, provided that when X.sup.A forms a single bond, then R.sup.1, R.sup.2A, R.sup.3A, R.sup.4A, R.sup.5A, and W.sup.A do not simultaneously represent a hydrogen atom, or a pharmaceutically acceptable salt.

    摘要翻译： 本发明提供一种治疗血小板减少症的方法，其包括向患有血小板减少症的患者施用有效量的由式（I）表示的吲哚并咔唑衍生物：其中R 1表示氢原子，取代或 未取代的低级烷基，取代或未取代的芳烷基或四氢吡喃基; R2A和R3A可以相同或不同，分别表示氢原子，取代或未取代的低级烷基，低级链烯基，取代或未取代的芳烷基或单末端残基，其中前体位置的羟基为 删除 R4A和R5A可以相同或不同，分别表示氢原子，甲酰基，羟基或卤素原子; WA1和WA2表示氢原子，或者组合在一起形成氧原子; 并且XA1和XA2表示两个氢原子，或者组合在一起形成单键，条件是当XA形成单键时，则R1，R2A，R3A，R4A，R5A和WA不同时表示氢原子，或 药学上可接受的盐。