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    EPOXYCYCLOHEXENEDIONE DERIVATIVE
    1.
    发明授权
    EPOXYCYCLOHEXENEDIONE DERIVATIVE 失效
    环氧环己烯衍生物

    公开(公告)号：EP0670317B1

    公开(公告)日：2000-03-08

    申请号：EP94927068.0

    申请日：1994-09-20

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： KANEKO, Masami ,  SAITOH, Yutaka ,  AKINAGA, Shiro ,  OKABE, Masami ,  AKASAKA, Kazuhito ,  NAKANO, Hirofumi

    IPC分类号： C07D303/36 ,  A61K31/335

    CPC分类号： C07D303/36

    摘要： An epoxycyclohexenedione derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents C10-C25 linear or branched alkanoyl, C10-C25 linear alkenoyl or a group represented by formula (A), wherein n represents an integer of 1 to 4. This compound has antibacterial and antitumoral activities.

    摘要翻译： 通式（I）表示的环氧基环己二酮衍生物或其药理学上允许的盐，式中，R表示碳原子数10〜25的直链状或支链状的烷酰基，碳原子数10〜25的直链烯酰基或式（A）所示的基团， 到4.这种化合物具有抗菌和抗肿瘤活性。

    EPOXYCYCLOHEXENEDIONE DERIVATIVE
    3.
    发明公开
    EPOXYCYCLOHEXENEDIONE DERIVATIVE 失效
    环氧环己烯衍生物

    公开(公告)号：EP0670317A1

    公开(公告)日：1995-09-06

    申请号：EP94927068.0

    申请日：1994-09-20

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： KANEKO, Masami ,  SAITOH, Yutaka ,  AKINAGA, Shiro ,  OKABE, Masami ,  AKASAKA, Kazuhito ,  NAKANO, Hirofumi

    IPC分类号： C07D303/36 ,  A61K31/335

    CPC分类号： C07D303/36

    摘要： An epoxycyclohexenedione derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents C₁₀-C₂₅ linear or branched alkanoyl, C₁₀-C₂₅ linear alkenoyl or a group represented by formula (A), wherein n represents an integer of 1 to 4. This compound has antibacterial and antitumoral activities.

    摘要翻译： 由通式（Ⅰ）表示的环氧环己烯二酮衍生物或其药理学上可接受的盐，其中R代表C 10 -C 25直链或支链烷酰基，C 10 -C 25直链烯酰基或式（A）代表的基团，其中n代表整数1 到4.这种化合物具有抗菌和抗肿瘤活性。

    FARNESYLTRANSFERASE INHIBITOR
    4.
    发明公开
    FARNESYLTRANSFERASE INHIBITOR 失效
    法尼基转移酶抑制剂。

    公开(公告)号：EP0670314A1

    公开(公告)日：1995-09-06

    申请号：EP94927069.8

    申请日：1994-09-20

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： KANDA, Yutaka ,  SAITOH, Yutaka ,  AKASAKA, Kazuhito ,  MIZUKAMI, Tamio ,  NAKANO, Hirofumi

    IPC分类号： C07D241/08 ,  C07D513/08 ,  A61K31/495 ,  A61K31/54

    CPC分类号： C07D513/08 ,  A61K31/495 ,  A61K31/54 ,  C07D241/08

    摘要： A farnesyltransferase inhibitor and an antitumor drug each containing a piperazinedione derivative represented by general formula (I) as the active ingredient, wherein R¹ and R² are the same or different from each other and each represents lower alkyl, lower alkoxyalkyl, or (un)substituted aryl or aralkyl; R³ and R⁴ are the same or different from each other and each represents mercapto, lower alkanoylthio, aroylthio, lower alkoxycarbonylthio or aryloxycarbonylthio, or R³ and R⁴ are combined with each other to represent a disulfide bond; and R⁵ and R⁶ are the same or different from each other and each represents hydrogen, lower alkyl, lower alkoxyalkyl, hydroxyalkyl, lower alkanoyloxyalkyl, aroyloxyalkyl, aralkyloxyalkyl or aralkyl.

    RADICICOL DERIVATIVES
    6.
    发明公开
    RADICICOL DERIVATIVES 失效
    DERIVATE DES RADICICOLS

    公开(公告)号：EP0823429A1

    公开(公告)日：1998-02-11

    申请号：EP96912263.9

    申请日：1996-04-26

    申请人： Kyowa Hakko Kogyo Co., Ltd.

    发明人： AGATSUMA, Tsutomu ,  SAITOH, Yutaka ,  YAMASHITA, Yoshinori ,  MIZUKAMI, Tamio ,  AKINAGA, Shiro ,  GOMI, Katsushige ,  AKASAKA, Kazuhito ,  TAKAHASHI, Isami

    IPC分类号： C07D313/00 ,  C07D493/04 ,  A61K31/365

    CPC分类号： C07D313/00

    摘要： The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof:
    wherein R 1 and R 2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R 4 -O-N (wherein R 4 represents hydrogen or substituted or unsubstituted lower alkyl); and R 3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R 3 are combined with each other to represent a single bond; Y represents R 4B -O-N (wherein R 4B has the same meaning as R 4 ). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.

    摘要翻译： 本发明涉及由下式（I）表示的根赤壳菌素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，各自代表氢，链烷酰基，烯酰基或叔 - 甲基硅烷基; （1）当X表示卤素时，Y表示氧原子或R 4 -O-N（其中R 4表示氢或取代或未取代的低级烷基）; 和R 3代表氢，烷酰基，烯酰基等; 和（2）当X和R 3彼此结合以表示单键时; Y表示R 4B-N-N（其中R 4具有与R 4相同的含义）。 本发明的根皮霉素衍生物显示出酪氨酸激酶抑制活性和药理活性，如抗肿瘤，抗微生物或免疫抑制作用。