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    N'-(pyridin-3-yl)-(4-phenylpiperazin-1-yl)-carboxyimidamide and -iminothiolate derivatives for the treatment of tumors
    2.
    发明公开
    N'-(pyridin-3-yl)-(4-phenylpiperazin-1-yl)-carboxyimidamide and -iminothiolate derivatives for the treatment of tumors 审中-公开
    N' - （吡啶-3-基） - （4-苯基哌嗪-1-基） - 羧酰亚胺酰胺和-Iminothiolat衍生物zur Behandlung vom Tumoren

    公开(公告)号：EP1424072A1

    公开(公告)日：2004-06-02

    申请号：EP03078792.3

    申请日：2000-03-03

    申请人： Samjin Pharmaceutical Co., Ltd.

    发明人： Chung, Sung-Gan ,  Lee, Sun-Hwan ,  Lee, Young-Hee ,  Kwon, Ho-Seok ,  Kang, Dong-wook ,  Joo, Jeong-Ho

    IPC分类号： A61K31/496 ,  C07D213/75

    CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D241/20 ,  C07D295/215

    摘要： The present invention relates to a novel compound of the general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antimumor activities and very low toxicity.
    wherein R 1 and R 2 are independently hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkylcarboxyl, C 1 -C 4 alkylcarbonyl, C 1 -C 4 alkoxy, C 1 -C 4 hydroxyalkyl, C 1 -C 4 aminoalkyl or C 1 -C 4 hydroxyiminoalkyl, or R 1 and R 2 are fused to form C 3 -C 4 unsaturated ring;
    R 3 , R 4 , R 5 , R 6 and R 7 are independently hydrogen, halogen, hydroxy, nitro, amino, C 1 -C 4 alkyl, C 1 -C 4 alkylcarboxyl, C 1 -C 4 alkylcarbonyl, C 1 -C 4 alkoxy or C 1 -C 4 thioalkoxy;
    Y is amino, substituted amino or C 1 -C 4 thioalkyl;
    Z is C 1 -C 4 alkoxy, C 1 -C 4 alkyl, C 1 -C 4 alkylamino or C 1 -C 4 thioalkoxy;
    X 1 is CH and X 2 is nitrogen;

    摘要翻译： 本发明涉及一种新型的通式（I）化合物及其药学上可接受的酸加成盐及其制备方法，其具有强的抗肿瘤活性和极低的毒性。 其中R1和R2独立地是氢，C1-C4烷基，C1-C4烷基羧基，C1-C4烷基羰基，C1-C4烷氧基，C1-C4羟基烷基，C1-C4氨基烷基或C1-C4羟基亚氨基烷基，或R1和R2 融合形成C3-C4不饱和环; R3，R4，R5，R6和R7独立地是氢，卤素，羟基，硝基，氨基，C1-C4烷基，C1-C4烷基羧基，C1-C4烷基羰基，C1-C4烷氧基或C1-C4硫代烷氧基; Y是氨基，取代的氨基或C 1 -C 4硫代烷基; Z是C 1 -C 4烷氧基，C 1 -C 4烷基，C 1 -C 4烷基氨基或C 1 -C 4硫代烷氧基; X1是CH，X2是氮;

    9-aminoacridine derivates and process for the preparation thereof
    3.
    发明公开
    9-aminoacridine derivates and process for the preparation thereof 有权
    9-Aminoacridin Derivate und Verfahrenfürihre Herstellung

    公开(公告)号：EP1380574A1

    公开(公告)日：2004-01-14

    申请号：EP03077547.2

    申请日：1999-12-17

    申请人： Samjin Pharmaceutical Co., Ltd.

    发明人： Cho, Eui-Hwan ,  Chung, Sun-Gan ,  Lee, Sun-Hwan ,  Kwon, Ho-Seok ,  Kang, Dong-Wook ,  Joo, Jeong-Ho

    IPC分类号： C07D219/10

    CPC分类号： C07D219/10 ,  Y02P20/55

    摘要： The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrdogen or (II) (wherein X is oxygen or sulfur, R 1 , R 2 , R 3 , R 4 and R 5 are independently ydrogen, halogen, nitro, amino, hydroxy, C 1 -C 4 lower alkylhydroxy, C 1 -C 4 lower alkylamino, C 1 -C 8 alkyl, C 1 -C 4 lower alkoxy or C 1 -C 4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2) , R 6 , R 7 , R 8 and Rg are independently hydrogen, C 1 -C 8 alkyl or C 1 -C 4 lower alkoxy, and Y is -N=CHR' (wherein R' is hydrogen, benzyl, C 1 -C 8 alkyl or C 1 -C 6 lower alkylamino), (III) (wherein R" is hydrogen, benzyl, C 1 -C 8 alkyl or C 1 -C 6 lower alkylamino, and R''' is hydrogen, benzyl, C 1 -C 8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R 1 ', R 2 ', R 3 ', R 4 ' and R 5 ' are independently hydrogen, halogen, nitro, amino, hydroxy, C 1 -C 4 lower alkylhydroxy, C 1 -C 4 lower alkylamino, C 1 -C 8 alkyl, C 1 -C 4 lower alkoxy or C 1 -C 4 lower alkylcarboxy, and q and r are independently an integer of 0, 1 or 2) or its pharmaceutically acceptable salt, and process for the preparation thereof.

    摘要翻译： 本发明涉及通式（I）的新的9-氨基吖啶衍生物，其中A是氢原子或（II）（其中X是氧或硫，R1，R2，R3，R4和R5独立地是氢原子，卤素，硝基， 氨基，羟基，C1-C4低级烷基羟基，C1-C4低级烷基氨基，C1-C8烷基，C1-C4低级烷氧基或C1-C4低级烷氧基羰基，m和n分别为0,1或2的整数），R6， R 7，R 8和R 8独立地是氢，C 1 -C 8烷基或C 1 -C 4低级烷氧基，Y是-N = CHR'（其中R'是氢，苄基，C 1 -C 8烷基或C 1 -C 6低级烷基氨基）， III）（其中R“是氢，苄基，C 1 -C 8烷基或C 1 -C 6低级烷基氨基，R”'是氢，苄基，C 1 -C 8烷基或氨基保护基）或（Ⅳ）（其中X是 如上定义，R1'，R2'，R3'，R4'和R5'独立地是氢，卤素，硝基，氨基，羟基，C1-C4低级烷基羟基，C1-C4低级烷基氨基，C1-C8烷基，C1-C4 低级烷氧基或C1-C4低级烷基羧基，q和r独立地为整数 0,1或2）或其药学上可接受的盐，以及其制备方法。