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1. 发明授权

US5674867A Indolocarbazole derivatives and therapeutic method for stimulating megakaicyocyte production 失效
标题翻译：吲哚咯唑衍生物和刺激巨核细胞产生的治疗方法
公开(公告)号：US5674867A
公开(公告)日：1997-10-07
申请号：US244111
申请日：1994-05-18
申请人： Tatsuya Tamaoki , Yukimasa Shiotsu , Chikara Murakata , Shiro Akinaga , Masami Okabe , Yutaka Saito , Junichi Watanabe , Takako Shiraki
发明人： Tatsuya Tamaoki , Yukimasa Shiotsu , Chikara Murakata , Shiro Akinaga , Masami Okabe , Yutaka Saito , Junichi Watanabe , Takako Shiraki
IPC分类号： C07D498/22 , C07H9/06 , C07H19/044 , A61K31/55
CPC分类号： C07D498/22 , C07H19/044 , C07H9/06
摘要： The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives. ##STR1##
摘要翻译： PCT No.PCT / JP93 / 01346 Sec。 371日期：1994年5月18日 102（e）日期1994年5月18日PCT提交1993年9月20日PCT公布。第WO94 / 06799号公报日期：1994年3月3日本发明涉及血小板减少症治疗剂，其含有下述式（I）表示的吲哚并咔唑衍生物或其药学上可接受的盐作为活性成分，以及新的吲哚并咔唑衍生物。（一）

2. 发明授权

US5604219A Indolocarbazole derivatives that stimulate platelet production 失效
标题翻译：刺激血小板生成的吲哚咔唑衍生物
公开(公告)号：US5604219A
公开(公告)日：1997-02-18
申请号：US404961
申请日：1995-03-16
申请人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
发明人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
IPC分类号： C07D498/22 , C07H9/06 , A61K31/55
CPC分类号： C07D498/22 , C07H9/06
摘要： Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents substituted or unsubstituted lower alkyl, R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, R.sup.3 and R.sup.4 are the same or different, and represent hydrogen, nitro, NR.sup.5 R.sup.6, OR.sup.9, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, or CH.dbd.NNR.sup.10 R.sup.11, W represents two hydrogen atoms or oxygen, and Me represents methyl, provided that when R.sup.1 is unsubstituted lower alkyl, R.sup.3 and R.sup.4 are not simultaneously hydrogen.
摘要翻译：公开了下式（I）表示的吲哚咔唑衍生物或其药学上可接受的盐：其中R 1表示取代或未取代的低级烷基，R 2表示氢，取代或未取代的低级烷基，R 3和R 4 代表氢，硝基，NR5R6，OR9，取代或未取代的低级烷基，取代或未取代的低级链烯基或CH = NNR10R11，W代表两个氢原子或氧，Me代表甲基，条件是当R 1 未取代的低级烷基，R3和R4不同时为氢。

3. 发明授权

US5629304A Therapeutic agent for thrombocytopenia and indolocarbazole derivatives 失效
标题翻译：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。

4. 发明授权

US5728709A Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that stimulate platelet production 失效
标题翻译：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。

5. 发明授权

US5344926A Process for producing staurosporine derivatives 失效
标题翻译：生产星形孢菌素衍生物的方法
公开(公告)号：US5344926A
公开(公告)日：1994-09-06
申请号：US79560
申请日：1993-06-22
申请人： Chikara Murakata , Toshimitsu Takiguchi , Shigeo Katsumata , Akira Mihara , Keiichi Takahashi , Hiromitsu Saito , Shiro Akinaga , Masami Okabe , Yutaka Saito
发明人： Chikara Murakata , Toshimitsu Takiguchi , Shigeo Katsumata , Akira Mihara , Keiichi Takahashi , Hiromitsu Saito , Shiro Akinaga , Masami Okabe , Yutaka Saito
IPC分类号： C07D498/22 , C07H9/06 , C07H19/04
CPC分类号： C07D498/22 , C07H19/04 , C07H9/06
摘要： Disclosed is a process for producing a staurosporine derivative represented by Formula (I): Q is defined as in specification: ##STR1## The staurosporine derivative (I-1) possesses selective protein kinase C-inhibitory and cell growth-inhibiting activities, and platelet-increasing activity.
摘要翻译：（I）星形孢菌素衍生物（I-1）具有选择性蛋白激酶C抑制和细胞生长抑制活性的方法，，血小板增多活性。

6. 发明授权

US06635662B2 Radicicol derivatives 失效
标题翻译：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。

7. 发明授权

US06316491B1 Radicicol derivatives 失效
标题翻译：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。

8. 发明申请

US20060035875A1 Remedy for hormone-dependent cancer 审中-公开
标题翻译：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。

9. 发明授权

US06239168B1 Radicicol derivatives 失效
标题翻译：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。

10. 发明申请

US20100098690A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：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。

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