PHENOXYACETIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    2.
    发明公开
    PHENOXYACETIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权
    PHENOXYESSIGSÄURE-VERBINDUNGEN UND MEDISINISCHE ZUSAMMENSETZUNGEN,DIEE ENTHALTEN

    公开(公告)号:EP1095932A1

    公开(公告)日:2001-05-02

    申请号:EP99926928.5

    申请日:1999-07-05

    摘要: The present invention provides novel phenoxyacetic acid derivatives represented by the general formula:
    [wherein R 1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, or a mono or di(lower alkyl)amino group; one of R 2 and R 3 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, while the other is a hydrogen atom; R 4 represents a halogen atom, a lower alkyl group, a halo(lower alkyl)group, a hydroxy group, a lower alkoxy group, an aralkoxy group, a cyano group, a nitro group, an amino group, a mono or di(lower alkyl)amino group, a carbamoyl group, a mono or di(lower alkyl)carbamoyl group or a group represented by the general formula:

            -NHCOR 5

    (wherein R 5 represents a hydrogen atom or a lower alkyl group); the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have excellent β 3 -adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of biliary tract.

    摘要翻译: 本发明提供由以下通式表示的新型苯氧基乙酸衍生物:其中R 1表示羟基,低级烷氧基,芳烷氧基,氨基或单或二(低级烷基)氨基 组; R 2和R 3之一是氢原子,卤素原子,低级烷基或低级烷氧基,而另一个是氢原子; R 4表示卤素原子,低级烷基,卤代(低级烷基),羟基,低级烷氧基,芳烷氧基,氰基,硝基,氨基,单或者 二(低级烷基)氨基,氨基甲酰基,一或二(低级烷基)氨基甲酰基或由通式-NHCOR 5表示的基团(其中R 5表示氢原子或低级烷基 组); 用(R)标记的碳原子表示R构型的碳原子; 标记有(S)的碳原子表示S构型中的碳原子及其药学上可接受的盐,其具有优异的β3肾上腺素能受体刺激作用,并且可用作预防或治疗肥胖,高血糖,由 肠蠕动过多,尿频,尿失禁,抑郁症,胆道结石或胆汁运动障碍引起的疾病。