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    Therapeutic agent for thrombocytopenia and indolocarbazole derivatives
    3.
    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。

    Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that stimulate platelet production
    4.
    发明授权
    Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that stimulate platelet production 失效
    刺激血小板生成的烷基和芳烷基取代的吡咯并咔唑衍生物

    公开(公告)号：US5728709A

    公开(公告)日：1998-03-17

    申请号：US737194

    申请日：1996-11-08

    申请人： Yoji Ikuina ,  Chikara Murakata ,  Yutaka Saitoh ,  Yukimasa Shiotsu ,  Takako Iida ,  Tatsuya Tamaoki ,  Kinya Yamashita ,  Shiro Akinaga

    发明人： Yoji Ikuina ,  Chikara Murakata ,  Yutaka Saitoh ,  Yukimasa Shiotsu ,  Takako Iida ,  Tatsuya Tamaoki ,  Kinya Yamashita ,  Shiro Akinaga

    IPC分类号： C07D487/04 ,  A61K31/41 ,  A61K31/44

    CPC分类号： C07D487/04

    摘要： Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10, or OR.sup.11 ; R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 --; and when R.sup.1 is benzyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen. A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.

    摘要翻译： PCT No.PCT / JP96 / 00557 Sec。 371日期：1996年11月8日 102（e）1996年11月8日PCT PCT 1996年3月7日PCT公布。 公开号WO96 / 28447 日本1996年9月19日描述了具有下式（I）的吡咯并咔唑衍生物及其药学上可接受的盐：其中R 1是低级烷基或芳烷基; R2是氢，取代或未取代的低级烷基，低级链烯基或取代或未取代的芳烷基; R 3，R 4，R 5，R 6和R 7可以相同或不同，为氢，卤素，硝基，取代或未取代的低级烷酰基，NR 9 R 10或OR 11; R8是氢或与R3结合形成-CONR 12 - ; 当R1为苄基时; R2，R3，R4，R5，R6，R7和R8不同时为氢。 本发明的化合物刺激血小板产生，并且可用于治疗血小板减少症。

    Radicicol derivatives
    6.
    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
    7.
    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。

    Remedy for hormone-dependent cancer
    8.
    发明申请
    Remedy for hormone-dependent cancer 审中-公开
    补充激素依赖性癌症

    公开(公告)号：US20060035875A1

    公开(公告)日：2006-02-16

    申请号：US10531099

    申请日：2003-10-09

    申请人： Yukimasa Shiotsu ,  Hiroyuki Ishida ,  Chikara Murakata ,  Hideaki Kusaka ,  Shiro Akinaga

    发明人： Yukimasa Shiotsu ,  Hiroyuki Ishida ,  Chikara Murakata ,  Hideaki Kusaka ,  Shiro Akinaga

    IPC分类号： A61K31/56

    CPC分类号： A61K31/567 ,  A61K45/06 ,  A61K2300/00

    摘要： A therapeutic agent for a hormone-dependent cancer, which comprises (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy, which may be administered together or separately at an interval, is provided. A method for treating a hormone-dependent cancer, which comprises administering (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy together or separately at an interval, is also provided. A steroid-sulfatase inhibitor which is used in combination with an agent for hormone therapy and/or an agent for chemotherapy, and which is administered together therewith or separately therefrom at an interval, is also provided. A kit for treating a hormone-dependent cancer, which comprises a first component comprising (a) a steroid-sulfatase inhibitor and a second component comprising (b) an agent for hormone therapy and/or an agent for chemotherapy, is also provided. A pharmaceutical composition, which comprises (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy, is also provided. Further, use of (a) a steroid-sulfatase inhibitor and (b) an agent for hormone therapy and/or an agent for chemotherapy for the manufacture of a therapeutic agent for a hormone-dependent cancer is provided.

    摘要翻译： 提供激素依赖性癌症的治疗剂，其包含（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗药物和/或化疗药剂，其可以一个或一个间隔一起施用或分开施用 。 还提供了一种用于治疗激素依赖性癌症的方法，其包括一次或一次间隔地施用（a）类固醇 - 硫酸酯酶抑制剂和（b）用于激素治疗的药剂和/或化学药剂。 还提供了与激素治疗药物和/或化学药剂组合使用的类固醇 - 硫酸酯酶抑制剂，并且其间隔一起或与其一起施用。 还提供了一种用于治疗激素依赖性癌症的试剂盒，其包含第一组分，其包含（a）类固醇 - 硫酸酯酶抑制剂和第二组分，所述第二组分包含（b）激素治疗剂和/或化学药剂。 还提供了一种药物组合物，其包含（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗剂和/或化疗剂。 此外，提供了（a）类固醇 - 硫酸酯酶抑制剂和（b）激素治疗剂和/或化疗剂用于制造激素依赖性癌症治疗剂的用途。

    Radicicol derivatives
    9.
    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。

    PHARMACEUTICAL COMPOSITION
    10.
    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。