申请人:Yamanouchi Pharmaceutical Co., Ltd.
公开号:US06346532B1
公开(公告)日:2002-02-12
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.
通用公式(I)表示的酰胺衍生物或其盐,其中每个符号的含义如下:环B:可选地取代的杂环芳基,可选地与苯环融合;X:键,较低的烷基或烯基,可选地取代为羟基或较低的烷基,酰基,或由—NH—表示的基团(当X为较低的烷基时,可选地取代为较低的烷基,可能与环B上的一个碳原子上的氢原子结合以形成较低的烷基从而形成一个环);A:较低的烷基或由-(较低的烷基)—O—表示的基团;R1a和R1b:相同或不同,各为氢或较低的烷基;R2:氢或卤素;Z:氮或由═CH—表示的基团。这些化合物可用作糖尿病疗法,不仅能加速胰岛素的分泌和增强胰岛素敏感性,还具有抗肥胖作用和抗高脂血症作用,这是基于其对β3受体的选择性刺激作用。