2-methylpropionic acid derivatives and pharmaceutical compositions comprising the same
申请人:KISSEI PHARMACEUTICAL CO., LTD.
公开号:US20030166719A1
公开(公告)日:2003-09-04
The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula:
1
(wherein R
1
represents a hydroxy group, a lower alkoxy group or an aralkyl group; R
2
represents a hydroxy group, a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino 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 &bgr;
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.
本发明提供了一种新的2-甲基丙酸衍生物,其通式表示为:1(其中R1代表一个羟基、一个较低的烷氧基或一个芳基烷基;R2代表一个羟基、一个较低的烷基或一个卤原子;A代表一个氧原子或一个亚胺基;标有(R)的碳原子代表R构型中的一个碳原子;标有(S)的碳原子代表S构型中的一个碳原子),以及其药学上可接受的盐,具有优异的β3-肾上腺素受体刺激效应,可用作预防或治疗肥胖、高血糖、由肠道过度运动引起的疾病、尿频、尿失禁、抑郁症或胆结石或胆道过度运动引起的疾病的药剂。