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    ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    3.
    发明授权
    ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    抗病毒嘧啶二酮衍生物及其制造方法

    公开(公告)号：EP1100786B1

    公开(公告)日：2004-07-21

    申请号：EP00921122.8

    申请日：2000-04-08

    申请人： Samjin Pharmaceutical Co., Ltd.

    发明人： CHO, Eui-Hwan ,  CHUNG, Sun-Gan ,  LEE, Sun-Hwan ,  KWON, Ho-Seok ,  LEE, Jae-Eung ,  JOO, Jeong-Ho

    IPC分类号： C07D239/54

    CPC分类号： C07D239/54 ,  C07D239/60 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06

    摘要： The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or tri-substituted phenyl with a group selected from hydroxy, C1-C4 alkyl, C1-C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1-C4 alkyl, C1-C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1-C4 alkoxycarbonyl; C1-C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1-C4 alkyl, R2 and R3 represent independently hydrogen or C1-C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

    N'-(pyridin-3-yl)-(4-phenylpiperazin-1-yl)-carboxyimidamide and -iminothiolate derivatives for the treatment of tumors
    4.
    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
    5.
    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。