Amide derivatives or salts thereof
    26.
    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

    IPC分类号: A61K31495

    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。

    Pyrimidine derivative condensed with a non-aromatic ring
    29.
    发明授权
    Pyrimidine derivative condensed with a non-aromatic ring 失效
    与非芳香环稠合的嘧啶衍生物

    公开(公告)号:US07947690B2

    公开(公告)日:2011-05-24

    申请号:US11577648

    申请日:2005-10-17

    摘要: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.

    摘要翻译: 本发明提供由式(I)表示的稠合嘧啶化合物或其药学上可接受的盐:其中A表示环,其中所述环中至少一个碳原子任选被一个或多个选自以下的基团取代:低级烷基 ,-O-(低级烷基),卤素原子,羧基,-CO 2 - (低级烷基)和氨基甲酰基,R 1表示:(1)被至少三个卤素原子取代的苯基,其可以具有至少一个另外的取代基,或 (2)环丙基,环丁基,环戊基,环己基或环庚基,其各自任选被取代; 并且R 2表示由式(II)表示的基团或任选取代的环状氨基:其中R 21和R 22可以相同或不同,并且各自表示-H,低级烷基,低级烯基,低级炔基,环烷基,苯基,杂芳基, 芳族杂环基或-O-(低级烷基),其各自任选被取代。