GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE THEREFOR
申请人:Kissei Pharmaceutical Co., Ltd.
公开号:EP1400529A1
公开(公告)日:2004-03-24
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula;
the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, -OCH2- or -CH2O-; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.
本发明提供由通式表示的葡萄糖吡喃氧基吡唑衍生物:
其中 R1 是氢原子或羟烷基;Q 和 T 中的一个是通式表示的基团,另一个是任选取代的烷基或环烷基;以及 R2 是卤原子;
R2是卤原子、羟基、任选取代的烷基、任选取代的烷氧基、烷硫基、通式如下的基团:-其中 A 是单键、氧原子、亚甲基、亚乙基、-OCH2- 或 -CH2O-;以及 R3 是环烷基、杂环烷基、任选取代的芳基、任选取代的噻唑基或任选取代的吡啶基、其药学上可接受的盐或其原药,它们对人类 SGLT1 具有极佳的抑制活性,因此可用作预防或治疗与高血糖有关的疾病(如糖尿病、糖尿病并发症或肥胖症)的药物、包含这些药物的药物组合物、其药物用途以及其生产中间体。