Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
申请人:Teranishi Hirotaka
公开号:US20060166899A1
公开(公告)日:2006-07-27
The present invention provides pyrazole derivatives represented by the general formula:
wherein R
1
represents H, an optionally substituted C
1-6
alkyl group etc.; one of Q and T represents a group represented by the general formula:
or a group represented by the general formula:
while the other represents an optionally substituted C
1-6
alkyl group etc.; R
2
represents H, a halogen atom, OH, an optionally substituted C
1-6
alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C
1-6
alkylene group etc.; Z represents CO or SO
2
; R
4
and R
5
represent H, an optionally substituted C
1-6
alkyl group etc.; and R
3
, R
6
and R
7
represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
本发明提供了由下式表示的吡唑衍生物:
其中,R1代表H、可选取代的C1-6烷基等;Q和T中的一个代表由下式表示的基团:
另一个代表可选取代的C1-6烷基等;R2代表H、卤素原子、OH、可选取代的C1-6烷基等;X代表单键、O或S;Y代表单键、C1-6烷基亚基等;Z代表CO或SO2;R4和R5代表H、可选取代的C1-6烷基等;R3、R6和R7代表H、卤素原子等,其药学上可接受的盐或前药,具有在人类SGLT1中出色的抑制活性,并且作为预防或治疗与高血糖相关的疾病,如糖尿病、糖尿病并发症或肥胖症的药物,以及包含它们的制药组合物、制药用途和制备它们的中间体。