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15 条记录 (耗时 0.024 秒)

    4'-flavonecarboxylic acids and pharmaceutically acceptable derivatives their preparation, and their application
    1.
    发明授权
    4'-flavonecarboxylic acids and pharmaceutically acceptable derivatives their preparation, and their application 失效
    4'-黄酮羧酸及其药学上可接受的衍生物及其应用

    公开(公告)号：US4600788A

    公开(公告)日：1986-07-15

    申请号：US592272

    申请日：1984-03-22

    申请人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Jacqueline Mosser ,  Henri Pontagnier

    发明人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Jacqueline Mosser ,  Henri Pontagnier

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P3/08 ,  A61P3/10 ,  A61P7/10 ,  C07D311/30 ,  C07D311/04

    CPC分类号： C07D311/30

    摘要： This invention relates to new products of the general formula ##STR1## where R.sub.1 =H, OH, OCOCH.sub.3, OSO.sub.2 CH.sub.3, branched or unbranched alkyl containing 1 to 5 carbon atoms. R.sub.2 =NHCOR.sub.3, NHCOCH.sub.2 X, NHSO.sub.2 CH.sub.3, N(SO.sub.2 CH.sub.3).sub.2, SO.sub.2 N(CH.sub.3).sub.2, SO.sub.2 NHCH.sub.3, SO.sub.2 NCH.sub.3 CH.sub.2 CH.sub.2 OH, SO.sub.2 NH.sub.2 wherein R.sub.3 is a lower alkyl containing 1 to 4 carbon atoms; and X is NR.sub.4 R.sub.5 or ##STR2## wherein R.sub.4 and R.sub.5 are both independently lower alkyls containing 1 to 4 carbon atoms and ##STR3## is piperidine, pyrrolidine or morpholine. These products can be in the form of pharmaceutically acceptable derivatives such as esters, amides, salts. When R.sub.2 contains an amino function, the product can be in the form of an acid salt.These products are prepared from their methyl esters either by reaction between ##STR4## and paramethoxycarbonylbenzoic acid chloride or by means of derivative I such as R.sub.2 is NH.sub.2.The products of this invention are used in therapy in the prevention and treatment of complications from diabetes or as diuretics.

    摘要翻译： 本发明涉及通式“IMAGE”的新产物，其中R1 = H，OH，OCOCH3，OSO2CH3，含有1至5个碳原子的支链或非支链烷基。 R2 = NHCOR3，NHCOCH2X，NHSO2CH3，N（SO2CH3）2，SO2N（CH3）2，SO2NHCH3，SO2NCH3CH2CH2OH，SO2NH2，其中R3是含有1至4个碳原子的低级烷基; 并且X是NR 4 R 5或者其中R 4和R 5各自独立地是含有1至4个碳原子的低级烷基，并且“IMAGE”是哌啶，吡咯烷或吗啉。 这些产物可以是药学上可接受的衍生物，例如酯，酰胺，盐。 当R2含有氨基官能团时，该产物可以是酸式盐。 这些产物由其甲酯制备，可以通过和对甲氧基羰基苯甲酰氯之间的反应或通过衍生物I如R2是NH2来制备。 本发明的产品用于预防和治疗糖尿病并发症或用作利尿剂的治疗。

    3-hydroxyflavones: their preparation and therapeutic application
    2.
    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

    申请人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Jacqueline Mosser ,  Henri Pontagnier

    发明人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Jacqueline Mosser ,  Henri Pontagnier

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P3/08 ,  A61P3/10 ,  A61P7/10 ,  C07D311/30 ,  C07D311/32

    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。

    3-(2-(4-phenylpiperazinylethyl)anilino)-isobenzofuranones, their method of preparation and their use as antihypertensive and antiallergic drugs
    3.
    发明授权
    3-(2-(4-phenylpiperazinylethyl)anilino)-isobenzofuranones, their method of preparation and their use as antihypertensive and antiallergic drugs 失效
    3-（2-（4-苯基哌嗪基乙基）苯胺基） - 异苯并呋喃酮，其制备方法及其作为抗高血压药和抗过敏药物

    公开(公告)号：US4590193A

    公开(公告)日：1986-05-20

    申请号：US517653

    申请日：1983-07-27

    申请人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Henri Pontagnier

    发明人： Marie-Helene Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gisele Prat ,  Henri Pontagnier

    IPC分类号： C07D307/91 ,  A61K31/495 ,  A61P9/12 ,  A61P37/08 ,  A61P43/00 ,  C07D307/90 ,  C07D241/04

    CPC分类号： C07D307/90

    摘要： This invention relates to 3-(2-(4-phenylpiperazinylethyl)anilino)-isobenzofuranones, their method of preparation and their use in the treatment of conditions such as hypertension, and allergies.These compounds are characterized by the formula: ##STR1## in which R.sub.1 may be one or more substituents located at the ortho, meta, or para positions selected from the group of H, CH.sub.3, CF.sub.3, F, Cl and OCH.sub.3 ; R.sub.2 and R.sub.3 are the same or different and are H or OCH.sub.3. These compounds are in the form of free bases or their pharmaceutically safe salts. They can be obtained by a reaction between a 2-(phenylpiperazinylethyl) aniline and an aromatic aldehyde having an acid function at the ortho position of the carboxaldehyde function.These derivatives are useful for the treatment of hypertension and allergic conditions.

    摘要翻译： 本发明涉及3-（2-（4-苯基哌嗪基乙基）苯胺基） - 异苯并呋喃酮，其制备方法及其用于治疗高血压和过敏等病症。 这些化合物的特征在于下式：其中R 1可以是位于选自H，CH 3，CF 3，F，Cl和OCH 3的邻位，间位或对位的一个或多个取代基; R2和R3相同或不同，为H或OCH3。 这些化合物是游离碱或其药学上安全的盐的形式。 它们可以通过2-（苯基哌嗪基乙基）苯胺与在羧甲醛官能团的邻位具有酸官能团的芳族醛的反应来获得。 这些衍生物可用于治疗高血压和过敏性疾病。

    N-(5-aminomethyl-2-oxazolin-2-yl)-N'-phenylureas, compositions and use
    9.
    发明授权
    N-(5-aminomethyl-2-oxazolin-2-yl)-N'-phenylureas, compositions and use 失效
    N-（5-氨基甲基-2-恶唑啉-2-基）-N'-苯基脲，组合物和用途

    公开(公告)号：US4499090A

    公开(公告)日：1985-02-12

    申请号：US539285

    申请日：1983-10-05

    申请人： Marie-Helene Creuzet ,  Claude Feniou ,  Christian Jarry ,  Gisele Prat ,  Henri Pontagnier

    发明人： Marie-Helene Creuzet ,  Claude Feniou ,  Christian Jarry ,  Gisele Prat ,  Henri Pontagnier

    IPC分类号： C07D263/28 ,  C07D413/06 ,  A61K31/42 ,  A61K31/535 ,  C07D295/14

    CPC分类号： C07D413/06 ,  C07D263/28

    摘要： This invention relates to new N-(5-aminomethyl-2-oxazoline-2-yl)-N'-phenylureas, the method for producing them and their application in therapy, particularly in treating convulsions, rhythm troubles, ulcerous disorders or inflammatory or edematous conditions.The products of this invention have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 independently represent an alkyl radical of C.sub.1 to C.sub.4, or a carbocyclic alkyl radical having 3 or less rings, or a carbocyclic radical having 3 or less rings; R.sub.1 and R.sub.2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms and 1 or 0 oxygen atoms, said heterocycle can be substituted by R with R being an alkyl radical of C.sub.1 to C.sub.4, allyl, benzyl, pyridyl, phenyl substituted or not by one or more substituents such as halogen, trihalomethyl, alkyl of C.sub.1 to C.sub.4, hydroxy, or alkoxy having a C.sub.1 to C.sub.4 alkyl radical.

    摘要翻译： 本发明涉及新的N-（5-氨基甲基-2-恶唑啉-2-基）-N'-苯基脲，其制备方法及其在治疗中的应用，特别是治疗惊厥，节律麻烦，溃疡性障碍或炎性或 水肿状况。 本发明的产物具有以下通式：其中R 1和R 2独立地表示C1至C4的烷基或具有3个或更少个环的碳环烷基或具有3个或更少个环的碳环基; R1和R2可以与它们所连接的氮原子一起形成含有1或2个氮原子和1或0个氧原子的4至7个成员杂环，所述杂环可以被R取代，其中R是C1的烷基 C4，烯丙基，苄基，吡啶基，被一个或多个取代基取代或未取代的苯基，如卤素，三卤代甲基，C1至C4烷基，羟基或具有C1至C4烷基的烷氧基。