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    Novel platinum complexes
    1.
    发明公开
    Novel platinum complexes 失效
    新型铂系复合物

    公开(公告)号：EP0454042A3

    公开(公告)日：1993-02-24

    申请号：EP91106490.5

    申请日：1991-04-23

    申请人： Nippon Kayaku Kabushiki Kaisha

    发明人： Kogawa, Osamu ,  Iwata, Kenji ,  Ekimoto, Hisao ,  Ishii, Tadashi ,  Takada, Kimihiko

    IPC分类号： C07F15/00 ,  A61K31/28

    CPC分类号： C07F15/0093

    摘要： A platinum (II) complex represented by the general formula:

    [wherein A's are each ammonia or two A's jointly represent 1,2-diaminocyclohexane, 1-amino-1-aminomethylcyclohexane or 1,4-diamino-2-methylbutane; and B's may be same or different and represent

    (wherein m is 0, 1 or 2; n is 0 or 1; R₁ is a C₃-C₆ alkyl group substituted with one or two hydroxyl groups) or two B's jointly represent

    (wherein R₂ is a C₂-C₅ alkyl group substituted with one hydroxyl group)]. These platinum (II) complexes have high potencies for use as an antitumor agent.

    Novel organic selenium compounds
    4.
    发明公开
    Novel organic selenium compounds 失效
    有机硒 - 维生素

    公开(公告)号：EP0222414A2

    公开(公告)日：1987-05-20

    申请号：EP86115853.3

    申请日：1986-11-14

    申请人： NIPPON KAYAKU KABUSHIKI KAISHA

    发明人： Ekimoto, Hisao ,  Suzuki, Masanobu ,  Izawa, Takao ,  Takahashi, Katsutoshi ,  Nakatani, Tokuji ,  Fujii, Akio

    IPC分类号： C07D213/06 ,  C07D213/61 ,  C07D213/85 ,  C07D213/84 ,  C07D213/79 ,  C07D213/22 ,  C07D207/20 ,  C07D215/06 ,  C07D471/04 ,  C07D213/73 ,  C07D213/64

    CPC分类号： C07D213/06 ,  C07D207/20 ,  C07D213/22 ,  C07D213/61 ,  C07D213/64 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D213/89 ,  C07D215/06 ,  C07D215/18 ,  C07D215/233 ,  C07D215/24 ,  C07D217/02 ,  C07D231/12 ,  C07D233/56 ,  C07D233/68 ,  C07D235/06 ,  C07D235/08 ,  C07D249/08 ,  C07D471/04 ,  C07D473/08 ,  C07D473/10 ,  C07D473/12 ,  C07F9/11

    摘要： This invention relates to the novel selenium compounds which are useful as an antineoplastic agent. The compounds are represented by the general formula (1):
    wherein R, X, A and Y represent the groups specified below, a represents a number of 0 or 1, b represents a number of 0, 1 or 2, and (1) when a is 0 and b is also 0, c is 4, n is 1 or 2 and m is 0, (2) when a is 1 and b is 0, c is 2, n is 1 or 2 and m is 0 or 1, and (3) when b is 1 or 2, c, n and m are all 0;

    (i) when b is 2, R represents (1) a C 4-10 alkoxy group substituted with a halogen atom, (2) a lower alkoxyl group substituted with a halogen atom and a phenyl group, or (3) a cycloalkyloxy group substituted with a halogen atom, and (ii) when b is 1, R represents a group represented by the formula
    (wherein R o is a C 2-6 alkyl group);
    X represents a halogen atom;
    A represents caffeine, theophylline, N-benzyltheophylline, N-benzyltheobromine, 2,2'-biquinoline, 1,6-naphthylidine, 1,10-phenanthroline, or a compound represented by the formula
    or
    (wherein R, and R 2 may be the same or different and represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a halogen atom, a phenyl group, a cyano group, a lower alkoxycarbonyl group, a phenoxycarbonyl group, an amino group (to which a lower alkyl, lower alkylaminocarbonyl, lower halogenoalkylaminocarbonyl or lower alkoxycarbonyl group may be bonded), a benzoyl group, a loweralkoxyl group, a carbamyl group or an allyloxycarbonyl group; R 3 represents a C 1-10 alkyl group or a benzyl group; R. and R 5 represent independently a hydrogen atom, a halogen atom or an alkyl group, or R 4 and R 5 may represent
    in combination; R 6 represents a lower alkoxyl group, a phenyl group or a phenoxy group; R 7 represents a hydrogen atom, a lower alkyl group or a group represented by the formula
    (wherein R 9 represents an amino group or a lower alkoxyl group); R 10 represent a hydrogen atom or a nitro group; and one of B and D represents nitrogen and the other represents ≥C-H or ≥C-OH); and
    Y represents H 2 O or an alcohol represented by the formula R 8 -OH [wherein R 8 represents a benzyl (which may be substituted with a lower alkoxy group) or alkyl group];
    wherein when X is chlorine atom and m is 0, R 1 and R 10 represent an atom or a group other than hydrogen atom.

    摘要翻译： 本发明涉及可用作抗肿瘤剂的新型硒化合物。 这些化合物由通式（I）表示：Se（O）a（R）b（X）c（A）n（Y）m（I）其中R，X，A和Y表示下面规定的基团， a表示0或1的数，b表示0,1或2的数，以及（1）当a为0且b为0时，c为4，n为1或2，m为0，（2） ）当a为1且b为0时，c为2，n为1或2，m为0或1，（3）当b为1或2时，c，n和m均为0; （i）当b为2时，R表示（1）被卤素原子取代的C 4-10烷氧基，（2）被卤素原子和苯基取代的低级烷氧基，或（3）取代的环烷氧基 和（ii）当b为1时，R表示由式（IMAGE）表示的基团（其中R 0为C 2-6烷基）; X表示卤原子; A表示由式“IMAGE”表示的化合物（其中R 1和R 2可以相同或不同，表示氢原子，羟基，低级烷基，卤素原子，苯基，氰基， 低级烷氧基羰基，苯氧基羰基，氨基（低级烷基，低级烷基氨基羰基，低级卤代烷基氨基羰基或低级烷氧基羰基可键合），苯甲酰基，低级烷氧基，氨基甲酰基或烯丙氧基羰基; R7表示 氢原子，低级烷基或下式表示的基团（其中R9表示氨基或低级烷氧基）; Y表示H 2 O.

    Antineoplastic agent
    5.
    发明公开
    Antineoplastic agent 失效
    Antitoplastisches Mittel。

    公开(公告)号：EP0182317A2

    公开(公告)日：1986-05-28

    申请号：EP85114557.3

    申请日：1985-11-16

    申请人： NIPPON KAYAKU KABUSHIKI KAISHA

    发明人： Suzuki, Masanobu ,  Izawa, Takao ,  Ekimoto, Hisao ,  Takahashi, Katsutoshi ,  Nakatani, Tokuji ,  Fujii, Akio

    IPC分类号： A61K31/095 ,  A61K33/04

    CPC分类号： A61K33/04 ,  A61K31/095

    摘要： The present invention relates to an antineoplastic agent containing a selenium compound of the general formula:
    wherein R, represents a halogen atom, a phenyl group, a lower alkoxy group or a halogen-substituted lower alkoxy group, R 2 represents a halogen atom, a hydroxy group, a lower alkoxy group or a halogen-substituted lower alkoxy group or R 1 and R 2 together form a group of the formula:
    or
    (in which R 3 and R 4 each represent a hydrogen atom or a lower alkyl group), X represents pyridine, quinoline, isoquinoline or dioxane and represents an integer of 0 to 2,
    wherein Hal represents a halogen atom, Y represents pyridine and m represents 0 or 2.

    摘要翻译： 本发明涉及含有以下通式的硒化合物的抗肿瘤剂：R1-S @ -R2。（X）n其中R1表示卤素原子，苯基，低级烷氧基或卤素取代的低级烷氧基 基团，R 2表示卤素原子，羟基，低级烷氧基或卤素取代的低级烷氧基，或者R 1和R 2一起形成下式的基团：其中R 3和R 4各自表示氢原子 或低级烷基），X表示吡啶，喹啉，异喹啉或二恶烷，n表示0〜2的整数，Se（Hal）4（Y）m其中Hal表示卤素原子，Y表示吡啶，m表示0 或2。

    Process for preparing benzo[C]phenanthridinium derivatives, and novel compounds prepared by said process
    7.
    发明公开
    Process for preparing benzo[C]phenanthridinium derivatives, and novel compounds prepared by said process 失效
    一种用于苯并的制备方法[C] phenanthridiniumderivaten和通过该方法获得的化合物。

    公开(公告)号：EP0487930A1

    公开(公告)日：1992-06-03

    申请号：EP91118676.5

    申请日：1991-11-01

    申请人： NIPPON KAYAKU KABUSHIKI KAISHA

    发明人： Suzuki, Masanobu ,  Nakanishi, Takeshi ,  Kogawa, Osamu ,  Ishikawa, Keizou ,  Kobayashi, Fumiko ,  Ekimoto, Hisao

    IPC分类号： C07D221/18 ,  C07D491/04 ,  A61K31/435

    CPC分类号： C07D491/04 ,  C07D221/18 ,  Y02P20/55

    摘要： The present invention relates to a process for preparing benzo[c]phenanthridinium derivatives of the general formula A:

    wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X⁻ represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group. This process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. Also, it has been found that certain novel benzo[c]phenanthridinium derivatives, prepared by the present process, have not only an antitumor activity but also an inhibition activity on blood platelet aggregation. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating into phamaceutical preparations.

    摘要翻译： 本发明涉及一种用于制备苯并[c]通式A的菲啶鎓衍生物： worin M和N分别独立地表示羟基或低级烷氧基，或M和N同时表示氢原子或一起形成 亚甲二氧基，X < - >酸残基或氢酸残基，R的darstellt darstellt低级烷基。 该工艺具有良好的重复性和可温和的条件下进行，并且，过程，因此实用价值。 所以，已经发现没有某些新颖苯并[c]菲啶鎓衍生物，由本发明方法制备的，不仅对的抗肿瘤活性，但这样对血小板聚集抑制活性。 此外，本发明化合物的氢盐具有增强的稳定性在，所有这些是有利的在配制成phamaceutical制剂。