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    신규한 벤즈아미딘 유도체, 그의 제조방법 및 이를포함하는 약학 조성물
    3.
    发明公开
    신규한 벤즈아미딘 유도체, 그의 제조방법 및 이를포함하는 약학 조성물 失效
    新颖的苯扎明衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：KR1020070079043A

    公开(公告)日：2007-08-03

    申请号：KR1020070009859

    申请日：2007-01-31

    Applicant: 동화약품주식회사

    Inventor： 유제만 ,  이진수 ,  진영구 ,  이기영 ,  박재훈 ,  황연하 ,  구세광

    IPC: C07D277/22 ,  C07D413/04 ,  C07D401/04 ,  A61P19/10

    CPC classification number: C07D417/04 ,  C07D277/28 ,  C07D417/12

    Abstract: A novel benzamidine derivative is provided to effectively inhibit osteoclast differentiation at an extremely low concentration, and significantly increase the trabecular bone volume, thereby being used for preventing and treating osteoporosis. The benzamidine derivative is represented by the formula(1), wherein R1 is C1-6 alkyl which is unsubstituted or substituted with one group selected from pyridine and a group represented by the structural formula(1-a), C3-6 cycloalkyl, phenyl, benzyl; pyridinyl which is unsubstituted or substituted with C1-6 alkyl, guanidino, NR6R7, a group represented by the structural formula(1-b); or a group represented by the structural formula(1-a) which is unsubstituted or substituted with C1-6 alkyl; R2 is a primary or secondary amine, which is NR8R9, a compound represented by the structural formula(1-c), pyrrolidine, piperidine or imidazole, each R3 and R4 is independently H, halogen, hydroxy, C1-6 alkyl which is unsubstituted or substituted with halogen, C3-6 cycloalkylamino, C1-6 alkoxy, C1-6 alkanoyloxy, C2-6 alkenyloxy, phenyl-C1-6 alkoxy, phenoxy, C2-6 alkenoyloxy or phenyl-C1-6 alkanoyloxy, or C3-6 cycloalkyloxy which is substituted with one group selected from carboxy, esterified carboxy and amidated carboxy or aminooxy; R5 is H or hydroxy group; each X1 and X3 is independently O, S, NH, or N-C1-6 alkyl, N-C3-6 cycloalkyl, N-benzyl or N-phenyl; X2 is C3-7 alkylene, C1-3 alkylene-C2-7 alkenylene-C1-3 alkylene, C1-3 alkylene-O-C1-3 alkylene, C1-3 alkylene-S-C1-3 alkylene, C1-3 alkylene-NH-C1-3 alkylene, C1-3 alkylene-phenylene-C1-3 alkylene, C1-3 alkylene-pyridylene-C1-3 alkylene or C1-3 alkylene-naphthylene-C1-3 alkylene, C3-7 alkylene which is substituted with C1-3 alkyl and hydroxyl, C3-7 alkylene carbonyl, or C3-7 alkylene which is interrupted by piperazine; Q is CH or carbonyl; and n is an integer of 0 to 6..

    Abstract translation: 提供了一种新颖的苯甲脒衍生物，以极低浓度有效抑制破骨细胞分化，并显着增加小梁骨体积，从而用于预防和治疗骨质疏松症。 苯甲脒衍生物由式（1）表示，其中R 1是未被取代或被一个选自吡啶和由结构式（1-a）表示的基团，C 3-6环烷基，苯基 ，苄基; 吡啶基，其未被取代或被C 1-6烷基，胍基，NR 6 R 7，被结构式（1-b）表示的基团取代; 或由未被取代或被C 1-6烷基取代的结构式（1-a）表示的基团; R2是伯或仲胺，其为NR8R9，由结构式（1-c）表示的化合物，吡咯烷，哌啶或咪唑，每个R 3和R 4独立地为H，卤素，羟基，未被取代的C 1-6烷基 或被卤素取代，C 3-6环烷基氨基，C 1-6烷氧基，C 1-6烷酰氧基，C 2-6烯氧基，苯基-C 1-6烷氧基，苯氧基，C 2-6烯酰氧基或苯基-C 1-6烷酰氧基或C 3-6 被一个选自羧基，酯化的羧基和酰胺化的羧基或氨氧基的基团取代的环烷氧基; R5为H或羟基; 每个X 1和X 3独立地是O，S，NH或N-C 1-6烷基，N 3 -C 6环烷基，N-苄基或N-苯基; X2是C3-7亚烷基，C1-3亚烷基-C2-7亚烯基C1-3亚烷基，C1-3亚烷基-O-C1-3亚烷基，C1-3亚烷基-S-C1-3亚烷基，C1-3亚烷基 -NH-C 1-3亚烷基，C 1-3亚烷基 - 亚苯基-C 1-3亚烷基，C 1-3亚烷基 - 亚吡啶基-C 1-3亚烷基或C 1-3亚烷基 - 亚萘基-C 1-3亚烷基， 被C 1-3烷基和羟基取代，C 3-7亚烷基羰基或被哌嗪中断的C 3-7亚烷基; Q是CH或羰基; n为0〜6的整数。

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