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New parabanic - derivatives as aldose - reductase inhibitors

机译:作为醛糖-还原酶抑制剂的新的巴拉班衍生物。

摘要

Parabanic acid derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (I): ##STR1## wherein R is hydrogen, lower alkyl or benzyl; X is substituted phenyl, optionally substituted benzothiazolyl, optionally substituted naphthyl, optionally substituted pyridyl, anthraquinonyl, phthalimide, or thienyl; and n is an integer from 1 to 3. The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibitory aldehyde reductase.
机译:包含所述化合物作为有效成分的对羟基苯甲酸酯衍生物,其药学上可接受的盐和治疗剂是用于治疗糖尿病并发症的有效药物,所述糖尿病并发症例如糖尿病性神经病,糖尿病性白内障和视网膜病,糖尿病性肾病,糖尿病性皮肤病和其他糖尿病性微血管病。本发明的化合物由以下通式(I)表示:其中R为氢,低级烷基或苄基; X为取代的苯基,任选取代的苯并噻唑基,任选取代的萘基,任选取代的吡啶基,蒽醌基,邻苯二甲酰亚胺或噻吩基; n为1〜3的整数。本发明的化合物显示出对醛糖还原酶的优异的抑制作用,并且具有高的酶选择性。因此,它们可用作治疗和预防各种类型的糖尿病并发症而基本不抑制醛还原酶的药物。

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