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1. 发明授权

US4877776A K-252 compounds 失效
标题翻译： K-252化合物
公开(公告)号：US4877776A
公开(公告)日：1989-10-31
申请号：US288787
申请日：1988-12-22
申请人： Chikara Murakata , Akira Sato , Masaji Kasai , Eiji Kobayashi , Makoto Morimoto , Shiro Akinaga
发明人： Chikara Murakata , Akira Sato , Masaji Kasai , Eiji Kobayashi , Makoto Morimoto , Shiro Akinaga
IPC分类号： C07D498/22 , A61K31/55 , A61P35/00 , C07H19/23
CPC分类号： C07H19/23
摘要： A K-252 compound represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently H or OH; X represents COOH, COOR or CH.sub.2 OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl has C-kinase inhibitory activity and is expected to be useful as an active ingredient of anti-tumor agents, etc.

2. 发明授权

US4923986A Derivatives of physiologically active substance K-252 失效
标题翻译：生理活性物质K-252的衍生物
公开(公告)号：US4923986A
公开(公告)日：1990-05-08
申请号：US273519
申请日：1988-11-08
申请人： Chikara Murakata , Akira Sato , Mitsuru Takahashi , Eiji Kobayashi , Makoto Morimoto , Shiro Akinaga , Tadashi Hirata , Kenichi Mochida , Hiroshi Kase , Koji Yamada , Kazuyuki Iwashashi
发明人： Chikara Murakata , Akira Sato , Mitsuru Takahashi , Eiji Kobayashi , Makoto Morimoto , Shiro Akinaga , Tadashi Hirata , Kenichi Mochida , Hiroshi Kase , Koji Yamada , Kazuyuki Iwashashi
IPC分类号： A61K31/55 , C07D20060101 , C07D498/22
CPC分类号： C07D498/22
摘要： The present invention relates to novel derivatives of K-252, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H, 11H-2,7b,11a-triazadibenzo[a,g]cycloocta-[c,d,e,]trinden-1-one, and the compounds are represented by formula (I): ##STR1## wherein W.sub.1, W.sub.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y represent various substituents. The compounds are physiologically active substances that inhibit protein kinase C and exhibit an antitumor activity, and are useful as medicines.

3. 发明授权

US06638923B2 Estra-1,3,5(10),16-tetraene derivatives 失效
标题翻译： Estra-1,3,5（10），16-四烯衍生物
公开(公告)号：US06638923B2
公开(公告)日：2003-10-28
申请号：US09859599
申请日：2001-05-18
申请人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
发明人： Yoji Ino , Nobuyoshi Amishiro , Taisuke Nakata , Hiroyuki Ishida , Shiro Akinaga , Chikara Murakata , Pui-Kai Li
IPC分类号： A61K3156
CPC分类号： C07J3/00
摘要： Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 is as defined by the present specification.
摘要翻译：由下式（I）表示的Estra-1,3,5（10），16-四烯衍生物:(其中R 1如本说明书所定义）。

4. 发明授权

US06399595B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
公开(公告)号：US06399595B1
公开(公告)日：2002-06-04
申请号：US09921668
申请日：2001-08-03
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.

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

US06376687B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
标题翻译：类固醇硫酸酯酶抑制剂及其制备和使用方法
公开(公告)号：US06376687B1
公开(公告)日：2002-04-23
申请号：US09490302
申请日：2000-01-24
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： C07J300
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
摘要翻译：公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂化合物。这些化合物通常包含在C17位置取代的类固醇核。还公开了合成这些化合物并将其用于治疗和/或预防性治疗患者的方法。

8. 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。

9. 发明授权

US06288050B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
标题翻译：类固醇硫酸酯酶抑制剂及其制备和使用方法
公开(公告)号：US06288050B1
公开(公告)日：2001-09-11
申请号：US09236842
申请日：1999-01-25
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： A61K3154
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
摘要翻译：公开了可用于治疗雌激素依赖性疾病的硫酸酯酶抑制剂化合物。这些化合物通常包含在C17位置取代的类固醇核。还公开了合成这些化合物并将其用于治疗和/或预防性治疗患者的方法。

10. 发明授权

US06953785B2 Estra-1,3,5(10)-triene derivatives 失效
标题翻译： Estra-1,3,5（10） - 三烯衍生物
公开(公告)号：US06953785B2
公开(公告)日：2005-10-11
申请号：US10258454
申请日：2001-04-24
申请人： Yoji Ino , Nobuyoshi Amishiro , Mayumi Miyata , Tsutomu Agatsuma , Kozue Muramatsu , Takeshi Takahashi , Shiro Akinaga , Chikara Murakata
发明人： Yoji Ino , Nobuyoshi Amishiro , Mayumi Miyata , Tsutomu Agatsuma , Kozue Muramatsu , Takeshi Takahashi , Shiro Akinaga , Chikara Murakata
IPC分类号： A61P5/24 , A61P5/32 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07J41/00 , C07J43/00 , A61K31/56 , A61K31/58 , C07J3/00 , C07J17/00
CPC分类号： C07J43/00 , C07J41/00
摘要： Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.
摘要翻译：提供了类固醇硫酸酯酶抑制剂，其包含作为活性成分的由式（I）表示的雌-1,3,5（10） - 三烯衍生物：其中R 1和R 2 > 2相同或不同，表示氢原子，低级烷基等。 R 3表示氢原子等; R 4表示氢原子等; R 5表示氢原子等; R 6表示氰基，氨基，COR 53（其中R 53表示取代的低级烷基等），取代的或未取代的芳基，取代或未取代的杂环基等）或其药学上可接受的盐。

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