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公开(公告)号：EP0788501B1
公开(公告)日：2002-06-05
申请号：EP95937391.1
申请日：1995-10-04
发明人： LEWIS, Michael, E. , KAUER, James, C. , NEFF, Nicola , GLICKSMAN, Marcie , ROBERTS-LEWIS, Jill , MURAKATA, Chikara , SAITO, Hiromitsu , MATSUDA, Yuzuru , KANAI, Fumihiko , KANEKO, Masami
IPC分类号： C07D498/22 , A61K31/55 , C07D487/14 , A61K31/40
CPC分类号： C07D487/14 , A61K31/407 , A61K31/5377 , A61K31/553 , A61K31/7056 , A61K2300/00
摘要： The invention features novel derivatives of K-252a e.g. (II-4) as well as novel bis-N-substituted derivatives of staurosporine of Formula (I). The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a. In the formula (I): [Stau] -N(CH3)-W-N(CH3)-[Stau], [Stau] represents a residue of formula (a) and W represents a radical of the formula: -C(=Y)-NH-W'-NH-C(=Y)- where W' is a hydrocarbylene radical of 2-20 carbon atoms and Y is O or S. In formula (II-4) R?1, R2, Z1, and Z2¿ are each H; X is CH¿2?OH; and R is OCH3.
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公开(公告)号：EP0630898B1
公开(公告)日：2001-11-28
申请号：EP93919687.9
申请日：1993-09-20
发明人： TAMAOKI, Tatsuya , SHIOTSU, Yukimasa , MURAKATA, Chikara , AKINAGA, Shiro , OKABE, Masami , SAITOH, Yutaka , WATANABE, Junichi , SHIRAKI, Takako
IPC分类号： C07D487/14 , C07D498/22 , C07H19/23 , A61K31/55 , A61K31/40
CPC分类号： C07D498/22 , C07H9/06 , C07H19/044
摘要： A thrombocytopenia remedy containing an indolocarbazole derivative represented by general formula (I) or a pharmacologically acceptable salt thereof as the active ingredient, and a novel indolocarbazole derivative.
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公开(公告)号：EP0717045B1
公开(公告)日：2001-04-04
申请号：EP95923556.5
申请日：1995-06-30
发明人： KINUGAWA, Masahiko , MASUDA, Yoshiaki , MIMURA, Yukiteru , MURAKATA, Chikara , SAITO, Hiromitsu , OGASA, Takehiro , KASAI, Masaji , TOMIOKA, Shinji
IPC分类号： C07D498/22 , A61K31/55
CPC分类号： C07D487/22 , C07D498/22
摘要： A process for producing an indolocarbazole derivative represented by general formula (II) by the acidic treatment of a silylated indolocarbazole derivative represented by general formula (VI) wherein R?1, R2 and R3¿ represent each independently lower alkyl or aryl; and R4 represents lower alkyl.
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公开(公告)号：EP0717045A1
公开(公告)日：1996-06-19
申请号：EP95923556.5
申请日：1995-06-30
发明人： KINUGAWA, Masahiko , MASUDA, Yoshiaki , MIMURA, Yukiteru , MURAKATA, Chikara , SAITO, Hiromitsu , OGASA, Takehiro , KASAI, Masaji , TOMIOKA, Shinji
IPC分类号： C07D498/22 , A61K31/55
CPC分类号： C07D487/22 , C07D498/22
摘要： A process for producing an indolocarbazole derivative represented by general formula (II) by the acidic treatment of a silylated indolocarbazole derivative represented by general formula (VI) wherein R¹, R² and R³ represent each independently lower alkyl or aryl; and R⁴ represents lower alkyl.
摘要翻译： 通过酸处理由通式（Ⅵ）表示的甲硅烷基化的吲哚并咔唑衍生物，其中R 1，R 2和R 3各自代表低级烷基或芳基，制备通式（Ⅱ）代表的吲哚并咔唑衍生物的方法; 而R 4代表低级烷基。
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5.发明公开USE OF INDOLOCARBAZOLE DERIVATIVES TO TREAT A PATHOLOGICAL CONDITION OF THE PROSTATE 失效吲哚咔唑衍生物治疗前列腺疾病的治疗中的应用
公开(公告)号：EP0699204A1
公开(公告)日：1996-03-06
申请号：EP94918168.0
申请日：1994-05-27
CPC分类号： C07D487/14 , A61K31/55 , C07H19/04
摘要： The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.
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公开(公告)号：EP1908755A1
公开(公告)日：2008-04-09
申请号：EP06767189.1
申请日：2006-06-22
IPC分类号： C07D285/135 , A61K31/433 , A61P9/00 , C07D285/12
CPC分类号： A61K31/433 , C07D285/12 , C07D285/135 , C07D417/12 , C07D491/10
摘要： A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof:
[wherein, n represents an integer of 1 to 3, R 0 represents aryl, -NR 1 CONR 2 (wherein R 1 represents a hydrogen atom or the like, and R 2 represents lower alkyl or the like) or the like, R 3 represents lower alkyl, R 4 represents a hydrogen atom or the like, and R 5 represents aryl or the like].摘要翻译： 用于再狭窄的治疗和/或预防剂，其包含由通式（0）表示的噻二唑啉衍生物或其药学上可接受的盐：[其中，n表示1〜3的整数，R 0表示芳基，-NR 1 CONR 2（其中R 1表示氢原子等，R 2表示低级烷基等）等，R 3表示低级烷基，R 4表示氢原子等，R 5表示芳基 等等]。
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公开(公告)号：EP1632484A1
公开(公告)日：2006-03-08
申请号：EP04745927.6
申请日：2004-06-09
发明人： MURAKATA, Chikara , INO, Yoji , KATO, Kazuhiko , YAMAMOTO, Junichiro , KITAMURA, Yuji , NAKAI, Ryuichiro , NAKANO, Tomohisa , TSUJITA, Tetsuya
IPC分类号： C07D285/12 , A61K31/433 , A61P35/00
CPC分类号： C07D285/135
摘要： A thiadiazoline derivative represented by the general formula (I), or a pharmacologically acceptable salt thereof:
[wherein R 1 represents a hydrogen atom and the like, R 2 represents a hydrogen atom, -COR 5 (wherein R 5 represents lower alkyl and the like) and the like, R 3 represents lower alkyl and the like, R 4 represents aryl and the like, A represents -(CH 2 ) n- (wherein n represents an integer of 1 to 6) and the like, and B represents -NR 6 R 7 (wherein R 6 and R 7 are the same or different and represent a hydrogen atom, lower alkyl and the like) and the like] is provided.摘要翻译： 由通式（I）的化合物或其药理学上可接受的盐表示的噻二唑啉衍生物：[其中R1表示氢原子等，R 2表示氢原子，-COR 5（其中R 5表示低级烷基等）和 等，R 3表示低级烷基等，R 4表示芳基等，A表示 - （CH 2）n - （其中n表示1〜6的整数）等，B表示-NR 6 R 7（其中R6和R7 相同或不同，表示氢原子，低级烷基等）等]。
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公开(公告)号：EP0918777B1
公开(公告)日：2002-08-28
申请号：EP97927906.4
申请日：1997-06-02
IPC分类号： C07D498/22 , A61K31/55
CPC分类号： C07D498/22
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公开(公告)号：EP0918777A1
公开(公告)日：1999-06-02
申请号：EP97927906.0
申请日：1997-06-02
CPC分类号： C07D498/22
摘要： Disclosed herein are selected indolocarbazole derivatives which are represented by general formula (I). The compounds are useful for enhancing the function and/or survival of a trophic factor responsive cell. They inhibit interleukin-2 production and have immunosuppressive activity.
摘要翻译： 本文公开了由通式（I）表示的选择的吲哚并咔唑衍生物。 该化合物可用于增强营养因子应答细胞的功能和/或存活。 它们抑制白细胞介素-2的产生并具有免疫抑制活性。
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公开(公告)号：EP0887351A1
公开(公告)日：1998-12-30
申请号：EP97947917.7
申请日：1997-12-12
发明人： KANDA, Yutaka , ARAI, Hitoshi , YAMAGUCHI, Hiroyuki , ASHIZAWA, Tadashi , IKEDA, Shun-ichi , MURAKATA, Chikara , TAMAOKI, Tatsuya
IPC分类号： C07D513/18 , C07D513/20 , C07D519/00 , C07H15/26 , C07H17/00 , A61K31/425 , A61K31/70
CPC分类号： C07D513/08 , C07H15/26 , C07H17/02
摘要： DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided:
wherein R 1 represents CO(CR 4A R 4B ) n1 (O(CH 2 ) p1 ) n2 OR 5 {wherein n1 represents an integer of 1 or 2; R 4A and R 4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R 5 represents hydrogen, lower alkyl, or the like), or
(wherein A 1 , A 2 , A 3 , and A 4 are the same or different, and each represents hydrogen, hydroxy, or the like); R 2 represents hydrogen or COR 6 (wherein R 6 represents lower alkyl, aralkyl, substituted or unsubstituted aryl, or the like); R 3 represents lower alkyl, lower alkenyl, aralkyl having substituted or unsubstituted aryl, alicyclic alkanoyloxyalkyl, -CH 2 OCOR 7 , or the like, or is combined with Y to represent a bond; Y is combined together with R 3 to represent a bond or is combined together with Z to represent a bond; Z represents hydrogen, or is combined together with Y to represent a bond; and W represents oxygen, or NR 8 .摘要翻译： 提供了具有抗微生物活性和抗肿瘤活性的由式（I）表示的DC107衍生物或其药学上可接受的盐：其中R 1表示CO（CR 4 R 4）n1（O（CH 2）p1） ）n2OR <5>其中n1表示1或2的整数; R 4A和R 4B相同或不同，各自表示氢或低级烷基; p1和n2各自表示1〜10的整数， R 5表示氢，低级烷基等）或
（其中A 1，A 2，A 3和A 4相同或不同，各自 表示氢，羟基等）; R 2表示氢或COR 6（其中R 6表示低级烷基，芳烷基，取代或未取代的芳基等）; R 3表示低级烷基，低级烯基，具有取代或未取代的芳基的芳烷基，脂环族烷酰氧基烷基，-CH 2 OCOR 7等，或与Y结合以表示键; Y与R 3结合以表示键或与Z结合以表示键; Z表示氢，或与Y结合表示键; W表示氧，或NR 8。
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