申请人:ONO PHARMACEUTICAL CO., LTD.
公开号:EP0323590A2
公开(公告)日:1989-07-12
A carbazoyl derivative of the general formula:
(wherein, R1b represents a bond, alkylene group of from 1 to 6 carbon atom(s) or alkenylene group of from 2 to 6 carbon atoms,
R2b represents a carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three halogen atom(s), hydroxy group, nitro group, amino group, alkyl or alkoxy group of from 1 to 4 carbon atom(s), 3-aminoureido group, phenoxy group or acylamino group of from 2 to 5 carbon atoms, or R1b together with R2b, represents an alkyl group of from 1 to 12 carbon atom(s) unsubstituted or substituted by 3-aminoureido group,
R3b represents (1) a hydrogen atom,
(2) an alkyl group of from 1 to 6 carbon atom(s) or
(3) a phenyl or benzyl group unsubstituted or substituted by from one to three halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), hydroxy group or nitro group,
Xb represents a bond or imino gorup,
with the proviso that the compounds wherein the groups shown by Xb-R1b-R2b represent a phenyl group, 4-aminophenyl gorup, anilino group and 2-thienyl group and the groups shown by R3b represent a hydrogen atom, are excluded.),
or an acid addition salt thereof possesses inhibitory activity on Maillard reaction, and therfore is useful for treating and/or prevention of several diabetic complications and deseases induced by aging.
通式如下的咔唑衍生物
(其中,R1b 代表键、1 至 6 个碳原子的亚烷基或 2 至 6 个碳原子的烯基、
R2b 代表未被或被 1 至 3 个卤素原子、羟基、硝基、氨基、1 至 4 个碳原子的烷基或烷氧基、3-氨基脲基、苯氧基或 2 至 5 个碳原子的酰氨基取代的碳环或杂环,或 R1b 与 R2b 一起代表未被或被 3-氨基脲基取代的 1 至 12 个碳原子的烷基、
R3b 代表 (1) 氢原子
(2) 1 至 6 个碳原子的烷基或
(3) 未被或被 1 至 3 个卤素原子、1 至 4 个碳原子的烷基或烷氧基、羟基或硝基取代的苯基或苄基、
Xb 代表键或亚胺基、
但不包括 Xb-R1b-R2b 所示基团代表苯基、4-氨基苯基、苯胺基和 2-噻吩基以及 R3b 所示基团代表氢原子的化合物)、
或其酸加成盐具有抑制 Maillard 反应的活性,因此可用于治疗和/或预防多种糖尿病并发症和由衰老引起的疾病。