申请人:Wakamoto Pharmaceutical Co., Ltd.
公开号:US05055481A1
公开(公告)日:1991-10-08
The present invention relates to an aldose reductase inhibitor having the following formula: ##STR1## R.sub.1 is a hydrogen atom or --A--COOR.sub.5 (A is an alkylene group having 1 to 4 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl group), and R.sub.2, R.sub.3 and R.sub.4 are the same as or different from each other and selected from the group consisting of a hydrogen atom, a hydroxy group, a halogen atom, a carboxyl group, an alkyl group, an amide group, an amino group, an alkoxy group, an aryl group, an aryloxy group, an alkylthio group, an alkylsulfinyl group, an alkylsulfonyl group, a nitro group, --NHCOCOOR.sub.6 (R.sub.6 is a hydrogen atom or a lower alkyl group), a mono- or dialkylaminosulfonyl group, and a residual group having the following formula: ##STR2## (A and R.sub.5 are the same as in the above). The compounds defined in the above are excellent in aldose reductase inhibitory activity and low in toxicity. Therefore, those compounds are useful as a preventive agent and/or a remedy for diabetic complications such as neuropathy, retinopathy, nephropathy, cataracts and keratopathy.
本发明涉及一种醛还原酶抑制剂,其具有以下式子:##STR1##其中,R.sub.1是氢原子或--A--COOR.sub.5(A是具有1至4个碳原子的烷基基团,R.sub.5是氢原子或较低的烷基基团),而R.sub.2、R.sub.3和R.sub.4相同或不同,选自以下组中的一种:氢原子、羟基、卤原子、羧基、烷基、酰胺基、氨基、烷氧基、芳基、芳氧基、烷硫基、烷基亚硫酰基、烷基磺酰基、硝基、--NHCOCOOR.sub.6(R.sub.6是氢原子或较低的烷基基团)、单烷基或双烷基氨基磺酰基,以及以下式子的残基:##STR2##(其中,A和R.sub.5与上述相同)。上述定义的化合物具有出色的醛还原酶抑制活性,并且毒性低。因此,这些化合物可用作糖尿病并发症(如神经病变、视网膜病变、肾病、白内障和角膜病变)的预防剂和/或治疗剂。