3-hydroxyflavones: their preparation and therapeutic application
    12.
    发明授权
    3-hydroxyflavones: their preparation and therapeutic application 失效
    3-羟基黄酮:其制备和治疗应用

    公开(公告)号:US4591600A

    公开(公告)日:1986-05-27

    申请号:US594976

    申请日:1984-03-29

    CPC分类号: C07D311/30

    摘要: This invention relates to quercetin or fisetin derivatives substituted on the oxygen in the 3 position by groups such as lower alkyl, cycloalkyl, methanesulfonyl or paratoluenesulfonyl.The derivatives substituted by methanesulfonyl or paratoluenesulfonyl are obtained from a 3-O-glycoside whose phenol OH groups are blocked in the form of benzoate, and from which the OH in the 3 position is released by the action of concentrated HCl; this OH is esterified by mesityl chloride or paratoluenesulfonic acid chloride, and the benzoate groups are eliminated by soda treatment. The O derivatives substituted by alkyl or cycloakyl are prepared from a suitably substituted acetonitrile or metadiphenol; the resulting derivative reacts with 3,4-dibenzyloxybenzoic acid and the resulting flavone is debenzylated by hydrogenolysis.The derivatives, object of this invention, are useful in preventive or curative therapy of ocular and nervous complications from diabetes and are also useful as hypolipidemic or hypoglycemic agents.

    摘要翻译: 本发明涉及通过诸如低级烷基,环烷基,甲磺酰基或对甲苯磺酰基的基团在3位上的氧上取代的槲皮素或非丝氨酸衍生物。 由甲磺酰基或对甲苯磺酰基取代的衍生物由苯酚OH基以苯甲酸酯形式封闭的3-O-糖苷获得,3位OH通过浓HCl的作用被释放; 该OH被均三甲基氯或对甲苯磺酰氯酯化,通过苏打处理除去苯甲酸酯基。 由烷基或环烷基取代的O衍生物由适当取代的乙腈或元二苯酚制备; 所得衍生物与3,4-二苄氧基苯甲酸反应,所得黄酮通过氢解脱苄基化。 本发明的目的的衍生物可用于糖尿病眼和神经并发症的预防或治疗性治疗,并且也可用作降血脂药或降血糖药。

    Orthoarylideneaminophenethylamines and pharmaceutical compositions
    13.
    发明授权
    Orthoarylideneaminophenethylamines and pharmaceutical compositions 失效
    正芳芳基氨基苯乙胺和药物组合物

    公开(公告)号:US4333930A

    公开(公告)日:1982-06-08

    申请号:US237277

    申请日:1981-02-23

    摘要: Compounds, exhibiting central nervous system activity, of the formula ##STR1## wherein R.sub.1 is phenyl which is unsubstituted or substituted by at least one member selected from the group consisting of halogen, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and COOH, orR.sub.1 is ##STR2## or R.sub.1 is a heterocycle selected from the group consisting of ##STR3## R.sub.2 R.sub.3 R.sub.4 and R.sub.5, which may be identical or different, are H or CH.sub.3 ;R.sub.6 and R.sub.7, which may be identical or different, are C.sub.1 -C.sub.6 alkyl, which may be straight-chained or branched, orR.sub.7 can be H when R.sub.6 is a branched-chain alkyl, orR.sub.6 and R.sub.7 can form, with the nitrogen to which they are bonded, a heterocycle selected from the group consisting of ##STR4## R.sub.8 R.sub.9 R.sub.10 and R.sub.11, which may be identical or different, are H, halogen, CF.sub.3, hydroxy or C.sub.1 -C.sub.4 alkoxy, or two contiguous members of R.sub.8 R.sub.9, R.sub.10 and R.sub.11 may together form a chain --O--(CH.sub.2).sub.n --O--, where n=1 or 2, or a chain --O--CH.sub.2 --O--CH.sub.2 --;and pharmaceutically acceptable addition salts thereof are disclosed, along with a method of producing the same, and pharmaceutical compositions comprising the same.

    摘要翻译: 具有下式的化合物(Ⅰ)其中R1是未被取代或被选自卤素,CF 3,C 1 -C 4烷基,C 1 -C 4烷氧基中的至少一个取代的苯基 或COOH,或R 1是或者R 1是选自下列的杂环:可以相同或不同的是H或 CH3; R6和R7可以相同或不同,可以是直链或支链的C1-C6烷基,或当R6是支链烷基或R6和R7可以与氮形成时,R7可以是H 与它们相连的杂环可以是H,卤素,CF 3,羟基或羟基,或者可以相同或不同的选自由下列组成的组的杂环:R 8 + L,R 9 + L,R 10和R 11 C 1 -C 4烷氧基或R 8 + L,R 9,R 10和R 11的两个连续成员可以一起形成-O-(CH 2)n O-链,其中n = 1或2,或链-O-CH 2 -O- CH2-; 公开了其药学上可接受的加成盐及其制备方法,以及包含其的药物组合物。

    Triterpenic saponin having pharmacological potency
    14.
    发明授权
    Triterpenic saponin having pharmacological potency 失效
    三萜皂苷具有药理作用

    公开(公告)号:US4335113A

    公开(公告)日:1982-06-15

    申请号:US148932

    申请日:1980-05-12

    CPC分类号: C07H15/256

    摘要: The present invention concerns a new triterpenic saponin derived from caulophyllogenin, the process for extracting it from varieties of Chrysanthellum, and its therapeutic use.This saponin is characterized as being the ester of O-.beta.-D-glucosyl-3.beta.-caulophyllogenin and an oligosaccharide comprising two units of L-rhamnose and two units of D-xylose. It is extracted from vegetable matter and purified using pressurized liquid preparative chromatographic techniques.This saponin is useful in human and veterinary therapeutics in phlebology, rheumatology, and traumatology.

    摘要翻译: 本发明涉及一种来源于胡萝卜素的新型三萜皂苷,其从菊花品种中提取的方法及其治疗用途。 该皂苷的特征在于是O-β-D-葡糖基-3β-开叶绿素的酯和包含两个单位的L-鼠李糖和两个D-木糖单位的寡糖。 从植物物质中提取并使用加压液体制备色谱技术纯化。 该皂苷可用于静脉,风湿病和创伤学中的人类和兽医治疗。

    Method and composition for reducing serum lipid levels using
p-chlorophenyl p-chlorophenoxyisobutyrate
    16.
    发明授权
    Method and composition for reducing serum lipid levels using p-chlorophenyl p-chlorophenoxyisobutyrate 失效
    使用对氯苯氧基异丁酸对氯苯酯降低血清脂质水平的方法和组合物

    公开(公告)号:US4179519A

    公开(公告)日:1979-12-18

    申请号:US884497

    申请日:1978-03-08

    IPC分类号: A61K31/215 A61K31/235

    CPC分类号: A61K31/215

    摘要: A method for reducing serum lipid levels in humans and animals is provided which comprises administering a hypolipidemically effective amount of p-chlorophenyl 2-(p-chlorophenoxy)-2-methylpropionate. A hypolipidemic composition is provided which comprises p-chlorophenyl 2-(p-chlorophenoxy)-2-methylpropionate, as principal active ingredient, in combination with a pharmaceutically acceptable carrier. Total serum lipids and serum cholesterol levels are significantly reduced.

    摘要翻译: 提供降低人和动物血清脂质水平的方法,其包括施用降血脂有效量的2-(对氯苯氧基)-2-甲基丙酸对氯苯酯。 提供降血脂组合物,其包含作为主要活性成分的2-(对氯苯氧基)-2-甲基丙酸对氯苯酯与药学上可接受的载体的组合。 总血清脂质和血清胆固醇水平显着降低。