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2. 发明授权

US6040326A 3-deoxyglucosone production inhibitor 失效
标题翻译： 3-脱氧葡萄糖酮生产抑制剂
公开(公告)号：US6040326A
公开(公告)日：2000-03-21
申请号：US997872
申请日：1997-12-24
申请人： Nigishi Hotta , Hiroki Fujisawa
发明人： Nigishi Hotta , Hiroki Fujisawa
IPC分类号： C07D233/96 , A61K31/415 , A61K31/4166 , A61K31/417 , A61K31/4174 , A61P3/08 , A61P9/00 , A61P9/10 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/28 , A61P27/02 , A61P35/00 , A61P43/00
CPC分类号： A61K31/4174 , A61K31/4166 , A61K31/417 , Y10S514/824
摘要： The production of 3-deoxyglucosone, which is an intermediate in the Maillard reaction and induces a crosslinking glycation of proteins participating in various diseases, is inhibited with an inhibitor containing at least one parabanic acid derivative as an effective ingredient. The at least one parabanic acid derivative is represented by the following formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein, R is hydrogen or lower alkyl; X is hydrogen, alkyl, cycloalkyl, lower alkylcycloalkyl, phenyl or phenylalkyl which is optionally substituted with lower alkyl, lower alkoxy, nitro and/or halogen; and n is an integer of from 1 to 4. Inhibiting the production of 3-DG, which is a highly active intermediate which participates in the formation of crosslinked protein in the Maillard reaction is useful for the treatment and the prevention of various diseases induced by deposition into tissues or sclerosis or denaturation of crosslinked protein, or diseases induced by aging and diabetic complications.
摘要翻译：使用含有至少一种对羟基苯甲酸衍生物作为有效成分的抑制剂抑制作为美拉德反应中的中间体并引起参与各种疾病的蛋白质的交联糖基化的3-脱氧葡萄糖酮的产生。所述至少一种对羟基苯甲酸衍生物由下式（I）表示或其药学上可接受的盐：其中，R为氢或低级烷基; X是氢，烷基，环烷基，低级烷基环烷基，苯基或任选被低级烷基，低级烷氧基，硝基和/或卤素取代的苯基烷基; n为1〜4的整数。抑制在美拉德反应中参与交联蛋白质形成的高活性中间体的3-DG的制备可用于治疗和预防由沉积到组织或硬化或交联蛋白质的变性，或由老化和糖尿病并发症引起的疾病。

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