申请人:Takeda Chemical Industries, Ltd.
公开号:EP0260121A2
公开(公告)日:1988-03-16
Disclosed is a novel inosose compound represented by the general formula:
wherein X¹ and X² are both halogen; X¹ is hydrogen and X² is halogen; or X¹ is -SQ¹ and X² is -SQ² (each of Q¹ and Q² is lower alkyl or Q¹ and Q² may form lower alkylene), R¹ is a protective group for hydroxyl and Y is =O, =N-Z (Z is hydroxyl which may be protected) or
HA (A is hydrogen or an amine residue), particulaly to the compound wherein the symbol Y is oxygen.
The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent α-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.
本发明公开了一种由通式表示的新型肌苷化合物:
其中X¹和X²均为卤素;X¹为氢,X²为卤素;或X¹为-SQ¹,X²为-SQ²(Q¹和Q²各自为低级烷基或Q¹和Q²可形成低级亚烷基),R¹为羟基的保护基团,Y为=O、=N-Z(Z为羟基,可被保护)或
HA(A 为氢或胺残基),特别是符号 Y 为氧的化合物。
肌苷化合物可作为生产缬氨醇胺及其 N-取代衍生物的中间体,这些衍生物具有强效的 α-葡萄糖苷酶抑制活性,可用于预防或治疗人和动物的高血糖症状以及由此引发的各种疾病,如糖尿病、肥胖症和高脂血症。