Rhodanine derivatives and pharmaceutical compositions
    5.
    发明授权
    Rhodanine derivatives and pharmaceutical compositions 失效
    罗丹明衍生物和药物组合物

    公开(公告)号:US5116855A

    公开(公告)日:1992-05-26

    申请号:US521902

    申请日:1990-05-11

    摘要: Disclosed is a rhodanine derivative of formula (I).A rhodanine derivative of formula (I) ##STR1## wherein R.sup.1 is hdyrogen, C.sub.1 -C.sub.8 alkyl, carboxyl(C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxycarbonyl(C.sub.1 -C.sub.4)alkyl;R.sup.2 is --CH.sub.2 --CH.sub.2 --R.sup.3, CH.dbd.CH.sub.m R.sup.3 (m is 0 or 1), ##STR2## (R is C.sub.1 -C.sub.3 alkyl) or --CH.sub.2n CONHR.sup.4 (n is 0 or 1-4); R.sup.3 is a thienyl or furyl group which may be substituted by C.sub.1 -C.sub.3 alkyl or halogen; a pyrrolyl group which may be substituted by carboxy(C.sub.1 -C.sub.3)alkyl on the nitrogen atom; or a phenyl group which may be substituted by one or more substituents selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxyl, halogen, trifluoromethyl, carboxyl, (C.sub.1 -C.sub.3)alkoxycarbonyl, cyano, carboxy(C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.3)alkoxy, benzyloxycarbonyl(C.sub.1 -C.sub.3)alkoxy, piperidinylcarbonyl(C.sub.1 -C.sub.3)alkoxy, 2H-tetrazolyl, 2H-tetrazolyl-(C.sub.1 -C.sub.4)alkoxy, carboxy(C.sub.2 -C.sub.4)alkenyl, (C.sub.1 -C.sub.3)alkoxycarbonyl(C.sub.2 -C.sub.4)alkenyl, carboxy(C.sub.1 -C.sub.3)alkyl and (C.sub.1 -C.sub.3)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl; andR.sup.4 is a phenyl group which may be substituted by one or more of the same substituents as defined above, or a pharmaceutically acceptable salt thereof.The derivatives are of an inhibitory activity against aldose reductase and useful for the prevention or treatment of complications of diabetes.

    Anti-cancer activity potentiator
    10.
    发明授权
    Anti-cancer activity potentiator 失效
    抗癌活性增强剂

    公开(公告)号:US5182267A

    公开(公告)日:1993-01-26

    申请号:US626302

    申请日:1990-12-12

    IPC分类号: A61K9/107 A61K31/135

    CPC分类号: A61K9/1075 A61K31/135

    摘要: A pharmaceutical oil-in-water type microemulsion having an action of potentiating the activities of anti-cancer agents, said micro-emulsion comprisesfine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.1 to 10% (w/v) of N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl)ethylenediamine malate of formula (I) below, ##STR1## an aqueous medium, and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.

    摘要翻译: 具有增强抗癌剂活性的作用的药用油包水型微乳液,所述微乳液包含具有8至12个碳原子的中链脂肪酸的植物油或甘油三酸酯的细颗粒,其含有 0.1至10%(w / v)下式(I)的N-茄酰基-N,N'-双(3,4-二甲氧基苄基)乙二胺苹果酸盐,水性介质,和 用于将所述细颗粒分散在所述水性介质中的生理学上可接受的磷脂的0.05至25%(w / v)。