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    Amide derivatives or salts thereof
    1.
    发明授权
    Amide derivatives or salts thereof 有权
    酰胺衍生物或其盐

    公开(公告)号：US06346532B1

    公开(公告)日：2002-02-12

    申请号：US09529096

    申请日：2000-04-07

    申请人： Tatsuya Maruyama ,  Takayuki Suzuki ,  Kenichi Onda ,  Masahiko Hayakawa ,  Hiroyuki Moritomo ,  Tetsuya Kimizuka ,  Tetsuo Matsui

    发明人： Tatsuya Maruyama ,  Takayuki Suzuki ,  Kenichi Onda ,  Masahiko Hayakawa ,  Hiroyuki Moritomo ,  Tetsuya Kimizuka ,  Tetsuo Matsui

    IPC分类号： A61K31495

    CPC分类号： C07D231/12 ,  C07D213/30 ,  C07D213/56 ,  C07D213/81 ,  C07D215/48 ,  C07D233/26 ,  C07D235/16 ,  C07D235/30 ,  C07D239/26 ,  C07D241/12 ,  C07D257/04 ,  C07D277/36 ,  C07D277/82 ,  C07D401/04 ,  C07D513/04

    摘要： Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—. The compounds are useful as a diabetes remedy which not only functions to both accelerate the secretion of insulin and enhance insulin sensitivity but has an antiobestic action and an antihyperlipemic action based on its selective stimulative action on a &bgr;3 receptor.

    摘要翻译： 由通式（I）表示的酰胺衍生物或其盐，其中每个符号具有以下含义：环B：任选地与苯环稠合的任选取代的杂芳基; X：任选被羟基或低级烷基取代的低级亚烷基或低级亚烯基，羰基或由-NH-表示的基团（当X为任选被低级烷基取代的低级烷基时，该低级烷基可以键合到与 环B的构成碳原子形成低级亚烷基，从而形成环）; A：低级亚烷基或由 - （低级亚烷基）-O-表示的基团。 R1a和R1b：相同或不同，各个氢或低级烷基; R2：氢或卤素; 和Z：氮或由= CH-表示的基团。 该化合物可用作糖尿病药物，其不仅可以加速胰岛素的分泌并增强胰岛素敏感性，而且具有基于其对β3受体的选择性刺激作用的抗胆碱作用和抗高脂血症作用。

    Amide derivatives and medicinal compositions thereof
    2.
    发明授权
    Amide derivatives and medicinal compositions thereof 失效
    酰胺衍生物及其药用组合物

    公开(公告)号：US06177454B1

    公开(公告)日：2001-01-23

    申请号：US09514637

    申请日：2000-02-29

    申请人： Tatsuya Maruyama ,  Kenichi Onda ,  Masahiko Hayakawa ,  Takumi Takahashi ,  Takayuki Suzuki ,  Tetsuo Matsui

    发明人： Tatsuya Maruyama ,  Kenichi Onda ,  Masahiko Hayakawa ,  Takumi Takahashi ,  Takayuki Suzuki ,  Tetsuo Matsui

    IPC分类号： A61K314184

    CPC分类号： C07D233/64 ,  C07C217/16 ,  C07C271/16 ,  C07C271/20 ,  C07D235/16 ,  C07D249/12 ,  C07D277/30 ,  C07D277/40 ,  C07D277/42 ,  C07D285/12 ,  C07D471/04

    摘要： An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.

    摘要翻译： 由以下通式（I）表示的酰胺衍生物或其盐和含有酰胺衍生物和药学上可接受的载体的药物组合物。式中的符号具有以下含义：A：亚杂芳基; X：键，O，S， -NR5-，-NR5CO-，-NR5CONH-，-NR5SO2-或-NR5C（= NH）NH-; R1：-H，可选取代的低级烷基， - 取代的芳基， - 取代的杂芳基或 - 取代的环烷基 ; R 2a，R 2b：-H或 - 低级烷基，其可以相同或不同; R 3：-H或 - 低级烷基; R 4a，R 4b：-H或-OH，其可以相同，或者R 4a和R 4b 一起形成= O或= NO-低级烷基; 和R5：-H或 - 低级烷基。