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    DC 107 DERIVATIVES (1)
    4.
    发明公开
    DC 107 DERIVATIVES (1) 失效
    DC 107 DERIVATE（1）

    公开(公告)号：EP0918058A1

    公开(公告)日：1999-05-26

    申请号：EP97947916.9

    申请日：1997-12-12

    申请人： KYOWA HAKKO KOGYO CO., Ltd.

    发明人： ARAI, Hitoshi ,  KANDA, Yutaka ,  YAMAGUCHI, Hiroyuki ,  ASHIZAWA, Tadashi ,  MURAKATA, Chikara ,  IKEDA, Shun-ichi ,  TAMAOKI, Tatsuya

    IPC分类号： C07D513/18 ,  C07D519/00 ,  C07H15/26 ,  A61K31/425 ,  A61K31/70

    CPC分类号： C07D513/18 ,  C07H15/26

    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 hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR 4 , or the like; R 2 represents hydrogen or COR 6 ; R 3 represents -CH 2 OCOR 7 , phthalimidomethyl, or the like; and W represents oxygen or NR 8 (wherein R 8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).

    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表示氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR 4等; R 2表示氢或COR 6; R 3表示-CH 2 OCOR 7，邻苯二甲酰亚氨基甲基等; W表示氧或NR 8（其中R 8表示羟基，低级烷氧基，低级烯氧基，芳烷氧基，取代或未取代的芳基磺酰基氨基或低级烷氧基羰基氨基）。

    LK6-A DERIVATIVES
    5.
    发明公开
    LK6-A DERIVATIVES 有权
    LK6-A-衍生物

    公开(公告)号：EP1097934A1

    公开(公告)日：2001-05-09

    申请号：EP99929753.4

    申请日：1999-07-08

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： AKAMA, Tsutomu ,  NAGATA, Hiroyuki ,  HASEGAWA, Atsuhiro ,  UE, Harumi ,  TAKAHASHI, Isami ,  SAITOH, Yutaka ,  MOCHIDA, Kenichi ,  IKEDA, Shun-ichi ,  KANDA, Yutaka

    IPC分类号： C07D471/06 ,  A61K31/47

    CPC分类号： C07D471/06

    摘要： LK6-A derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, which exhibit immunosuppressive, cytostatic and antitumor effects and so on, wherein R 1 is a lower alkanoyl or acryloyl group which may be substituted with, e.g., lower alkoxy, or the like; R 2 is hydrogen, halogeno or the like; R 2' is hydrogen, or R 2' together with R 3 forms a bond; R 3 is optionally substituted lower alkanoyl, or R 3 together with R 2' forms a bond; R 4 and R 5 are each hydrogen, optionally substituted lower alkanoyl or the like; R 6 is hydrogen or the like; and R 7 and R 8 are each hydrogen, optionally substituted lower alkanoyl or the like, with the proviso that LK6-A corresponding to a compound of general formula (I) where R 1 is (E)-methoxyacryloyl; R 2 , R 4 , R 5 , R 6 and R 7 are each hydrogen; R 8 is acetyl; and R 2' and R 3 together form a bond is excepted.

    摘要翻译： 具有通式（I）表示的LK6-A衍生物及其药理学上可接受的盐，其具有免疫抑制，细胞抑制和抗肿瘤作用等，其中R 1为低级烷酰基或丙烯酰基，其可被例如较低级 烷氧基等; R 2是氢，卤素等; R 2是氢，或R 2与R 3一起形成键; R 3是任选取代的低级烷酰基，或R 3与R 2'一起形成键; R 4和R 5各自为氢，任选取代的低级烷酰基等; R 6是氢等; R 7和R 8各自为氢，任选取代的低级烷酰基等，条件是对应于通式（I）的化合物的LK6-A，其中R 1为（E） - 甲氧基丙烯酰基 ; R 2，R 4，R 5，R 6和R 7各自为氢; R 8是乙酰基; 和R 2'和R 3一起形成键。

    DC107 DERIVATIVES
    6.
    发明公开
    DC107 DERIVATIVES 失效
    推出冯DC 107

    公开(公告)号：EP0786462A1

    公开(公告)日：1997-07-30

    申请号：EP96917696.5

    申请日：1996-06-14

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： KANDA, Yutaka ,  SAITOH, Yutaka ,  SAITO, Hiromitsu ,  ASHIZAWA, Tadashi ,  SUGIYAMA, Kazuyo ,  GOMI, Katsushige ,  KAKITA, Shingo ,  TAKAHASHI, Yuichi ,  MURAKATA, Chikara

    IPC分类号： C07D513/08 ,  A61K31/425

    CPC分类号： C07D513/08

    摘要： DC107 derivatives represented by the formula (I):
    or pharmacologically acceptable slats thereof,
    [wherein R 1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR 4 or the like; R 2 represents hydrogen or COR 5 ; R 3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R 3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR 6 , with the proviso that the compound wherein R 1 , R 2 and Z each represents hydrogen, R 3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.]

    摘要翻译： 由式（I）代表的DC107衍生物：其或其药理学上可接受的板条，其中R 1是氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR 4等; R 2表示氢或COR 5; R 3表示低级烷基，低级烯基，可被取代或未取代的芳基取代的芳烷基，低级烷氧基烷基，芳烷氧基烷基，取代或未取代的芳氧基烷基，低级烷氧基羰基烷基，低级烷酰氧基烷基，脂环族烷酰氧基烷基等，或与Y键合以表示 单一债券 Y与R 3键合以表示单键，或与Z键合以表示单键; Z表示氢或与Y键合以表示单键; W表示氧或NR 6，条件是其中R 1，R 2和Z各自表示氢，R 3与Y键合以表示单键，W表示氧（DC107 ）被排除在外

    DC 107 DERIVATIVES (2)
    7.
    发明公开
    DC 107 DERIVATIVES (2) 失效
    DC 107-DERIVATE

    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

    申请人： Kyowa Hakko Kogyo Co., Ltd.

    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。

    FARNESYLTRANSFERASE INHIBITOR
    8.
    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.