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    Ab1 KINASE INHIBITORS
    1.
    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
    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
    6.
    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。

    PHARMACEUTICAL COMPOSITION
    8.
    发明申请
    PHARMACEUTICAL COMPOSITION 审中-公开
    药物组合物

    公开(公告)号：US20100098690A1

    公开(公告)日：2010-04-22

    申请号：US12529380

    申请日：2008-03-05

    申请人： Shiro Soga ,  Toshihiko Ishii ,  Takayuki Nakashima ,  Yukimasa Shiotsu ,  Shiro Akinaga

    发明人： Shiro Soga ,  Toshihiko Ishii ,  Takayuki Nakashima ,  Yukimasa Shiotsu ,  Shiro Akinaga

    IPC分类号： A61K31/122 ,  A61K31/216 ,  A61K31/135 ,  A61K31/495 ,  A61K31/445 ,  A61K31/47 ,  A61K31/5375 ,  A61K31/44 ,  A61K31/075 ,  A61K31/165 ,  A61K31/05 ,  A61K31/5377 ,  A61K39/395 ,  A61K31/4965 ,  A61P35/00

    CPC分类号： A61K31/5375 ,  A61K31/198 ,  A61K31/337 ,  A61K31/5377 ,  A61K39/39558 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.

    摘要翻译： 本发明提供了包含Hsp90家族蛋白抑制剂和至少一种化合物的组合的药物组合物，所述药物组合物，其中Hsp 90家族蛋白抑制剂是由式（I）表示的新戊酰化合物：[其中n表示 1〜5的整数; R1表示取代或未取代的低级烷基CONR7R8（其中R7和R8可相同或不同，各自表示氢原子，取代或未取代的低级烷基等）等; R2表示取代或未取代的芳基等; R 3和R 5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; R4表示氢原子，羟基或卤素; R6代表氢原子，卤素，取代或未取代的低级烷基等]或其前药; 或其药学上可接受的盐等。

    AURORA INHIBITORS
    9.
    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。