申请人:Takeda Chemical Industries, Ltd.
公开号:EP0369453A2
公开(公告)日:1990-05-23
Thiourea compounds represented by the general formula:
[wherein A is an aromatic ring group which may be substituted; R1 is a hydrogen atom or a lower alkyl or aryl group which may be substituted, or may combine with A to form a cyclic ring; and -COB is an acyl group of a carboxylic acid or an esterified carboxyl group] or salts thereof are provided as agents for inhibiting the formation of AGE (Advanced Glycosidation End product) which are employable for treating diseases caused by AGE-formation, such as diabetic complications, senile cataract, atherosclerosis etc.
The compounds of the formula [I] are novel, provided that, when A is a phenyl group which may be substituted or A combines with R1 to form a cyclic ring, B is not a phenyl group which may be substituted; and can be produced by reacting the corresponding aminothiazole compounds with isocyanate compounds having the formula of BCONCS (wherein B is the same as above).
由通式表示的硫脲化合物:
[其中 A 是可被取代的芳环基团;R1 是氢原子或可被取代的低级烷基或芳基,或可与 A 结合形成环;和 -COB 是羧酸的酰基或酯化羧基]或其盐作为抑制 AGE(高级糖苷化终产物)形成的制剂,可用于治疗 AGE 形成引起的疾病,如糖尿病并发症、老年性白内障、动脉粥样硬化等。
式[I]化合物是新型化合物,条件是当 A 是可被取代的苯基或 A 与 R1 结合形成环状环时,B 不是可被取代的苯基;并且可通过使相应的氨基噻唑化合物与具有 BCONCS 式的异氰酸酯化合物(其中 B 与上述相同)反应而制得。