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公开(公告)号：EP1028111A4
公开(公告)日：2000-12-20
申请号：EP98947894
申请日：1998-10-15
发明人： MARUYAMA TATSUYA , SUZUKI TAKAYUKI , ONDA KENICHI , HAYAKAWA MASAHIKO , MORITOMO HIROYUKI , KIMIZUKA TETSUYA , MATSUI TETSUO
IPC分类号： C07C233/07 , A61K31/16 , A61P3/10 , C07C229/38 , C07C233/65 , C07D213/30 , C07D213/56 , C07D213/81 , C07D215/48 , C07D231/12 , C07D233/26 , C07D233/64 , C07D235/16 , C07D235/30 , C07D239/26 , C07D241/12 , C07D257/04 , C07D277/36 , C07D277/40 , C07D277/82 , C07D401/04 , C07D513/04 , A61K31/425 , C07D217/22 , C07D277/68 , C07D285/08
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-; R?1a 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 β¿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：一个键，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是任选被低级烷基取代的低级烷基时，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。 R 1a和R 1b相同或不同，各个氢或低级烷基; R 2：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，而且具有抗胆碱作用和基于其对β3受体的选择性刺激作用的抗高脂血症作用。 -
公开(公告)号：EP0972769A4
公开(公告)日：2001-04-18
申请号：EP98900698
申请日：1998-01-22
发明人： MARUYAMA TATSUYA , ONDA KENICHI , HAYAKAWA MASAHIKO , TAKAHASHI TAKUMI , SUZUKI TAKAYUKI , MATSUI TETSUO
IPC分类号： A61K31/41 , A61K31/415 , A61K31/425 , A61P3/10 , A61P5/50 , C07C217/16 , C07C271/16 , C07C271/20 , C07D233/54 , C07D233/61 , C07D233/64 , C07D235/16 , C07D249/08 , C07D249/12 , C07D257/04 , C07D277/30 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/46 , C07D285/12 , C07D471/04 , A61K31/44 , C07D277/64 , C07D417/06 , C07D417/12 , C07D513/04
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： Amide derivatives represented by general formula (I), or their salts and medicinal compositions containing these derivatives and pharmaceutically acceptable carriers, wherein each symbol has the following meaning: A: heteroarylene; X: a bond, O, S, -NR?5-, -NR5¿CO-, -NR5CONH-, -NR5SO2- or -NR5C(=NH)NH-; R1: H, optionally substituted lower aryl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted cycloalkyl; R?2a and R2b¿: being the same or different from each other and each representing H or lower alkyl; R3: H or lower alkyl; R?4a and R4b¿: being the same or different from each other and each representing H or OH, or R?4a and R4b¿ forming together =O or =N~O-lower alkyl; and R5: H or lower alkyl. These compounds are useful as remedies for diabetes having an insulin secretion accelerating effect together with an insulin sensitivity increasing effect.
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