申请人:Takeda Chemical Industries, Ltd.
公开号:EP1229026A1
公开(公告)日:2002-08-07
A compound represented by the formula
wherein
R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;
Xis a bond, an oxygen atom, a sulfur atom, or a group represented by -CO-, -CS-, -CR6(OR7)- or -NR8- (R6 and R8 are each a hydrogen atom or an optionally substituted hydrocarbon group, and R7 is a hydrogen atom or a hydroxy-protecting group);
nis an integer of 0 to 3;
Yis an oxygen atom, a sulfur atom, or a group represented by -SO-, -SO2-, -NR8-, -CONR8- or -NR8CO- (R8 is a hydrogen atom or an optionally substituted hydrocarbon group);
ring Ais a heterocycle optionally having 1 to 3 additional substituents or a hydrocarbon ring optionally having 1 to 3 additional substituents;
pis an integer of 1 to 8;
R2is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;
qis an integer of 0 to 6;
mis 0 or 1;
R3is a group represented by -OR9 (R9 is a hydrogen, atom or an optionally substituted hydrocarbon group) or -NR10R11 (R10 and R11 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted acyl group, and R10 and R11 may be taken together to form a ring);
R4 and R5are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R4 and R2 may be taken together to form a ring, provided that, when ring A is an optionally substituted indole, Y is not an oxygen atom or a sulfur atom; when Y is an oxygen atom, a sulfur atom, -SO-, -SO2- or -NR8- (R8 is as defined above), ring A is not a benzene ring optionally having substituents; and when Y is an oxygen atom and ring A is an optionally substituted . 4-pyrone, an optionally substituted 4-pyridone or an optionally substituted pyridine-N-oxide, R2 is not a thiazole substituted by an optionally protected amino group or a thiadiazole substituted by an optionally protected amino group,
and a salt thereof are useful as an agent for the prophylaxis or treatment of diabetes and the like.
一种由式表示的化合物
式中
R1 是任选取代的烃基或任选取代的杂环基;
X是键、氧原子、硫原子或由-CO-、-CS-、-CR6(OR7)-或-NR8-代表的基团(R6和R8各自是氢原子或任选取代的烃基,R7是氢原子或羟基保护基团);
n 是 0 至 3 的整数;
Y是氧原子、硫原子或由-SO-、-SO2-、-NR8-、-CONR8-或-NR8CO-代表的基团(R8是氢原子或任选取代的烃基);
环 A 是可选具有 1 至 3 个额外取代基的杂环或可选具有 1 至 3 个额外取代基的烃环;
p 是 1 至 8 的整数;
R2 是氢原子、任选取代的烃基或任选取代的杂环基;
q 是 0 至 6 的整数;
mis 0 或 1;
R3是由-OR9(R9是氢原子或任选取代的烃基)或-NR10R11(R10和R11相同或不同,各自是氢原子、任选取代的烃基、任选取代的杂环基团或任选取代的酰基,R10和R11可结合在一起形成一个环)代表的基团;
R4 和 R5 相同或不同,且各自为氢原子或任选取代的烃基,R4 和 R2 可结合在一起形成一个环,条件是当环 A 是任选取代的吲哚时,Y 不是氧原子或硫原子;当 Y 是氧原子、硫原子、-SO-、-SO2- 或 -NR8- (R8 如上定义)时,环 A 不是任选具有取代基的苯环;当 Y 是氧原子且环 A 是任选取代的.4-吡啶酮、任选取代的 4-吡啶酮或任选取代的吡啶-N-氧化物时,R2 不是被任选保护的氨基取代的噻唑或被任选保护的氨基取代的噻二唑、
及其盐可作为预防或治疗糖尿病等疾病的药物。