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    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-(2-(4-phenylpiperazinylethyl)anilino)-isobenzofuranones, their method of preparation and their use as antihypertensive and antiallergic drugs
    2.
    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。

    Orthoarylideneaminophenethylamines and pharmaceutical compositions
    3.
    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

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

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

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61K31/357 ,  A61K31/36 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C241/00 ,  C07C251/02 ,  C07D213/53 ,  C07D213/89 ,  C07D307/52 ,  C07D317/66 ,  C07D333/22 ,  C07D405/12 ,  C07D409/12 ,  A61K31/535 ,  C07D317/58 ,  C07D413/06

    CPC分类号： C07D213/53 ,  C07D213/89 ,  C07D307/52 ,  C07D317/66 ,  C07D333/22

    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。

    3-hydroxyflavones: their preparation and therapeutic application
    6.
    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。

    2-(4-Phenylpiperazinylethyl) anilines
    7.
    发明授权
    2-(4-Phenylpiperazinylethyl) anilines 失效
    2-（4-苯基哌嗪基乙基）苯胺

    公开(公告)号：US4668681A

    公开(公告)日：1987-05-26

    申请号：US843915

    申请日：1986-03-21

    申请人： Henri Pontagnier ,  Marie-H/e/ l/e/ ne Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gis/e/ le Prat

    发明人： Henri Pontagnier ,  Marie-H/e/ l/e/ ne Creuzet ,  Claude Feniou ,  Francoise Guichard ,  Gis/e/ le Prat

    IPC分类号： C07D295/12 ,  A61K31/495 ,  A61P37/08 ,  A61P43/00 ,  C07D295/135 ,  C07D317/66

    CPC分类号： C07D295/135 ,  C07D317/66

    摘要： This invention relates to 2-(4-phenylpiperazinylethyl)anilines, to methods for preparing them and to their uses in medical therapy.These compounds have the following general formula ##STR1## wherein R.sub.1 represents one or more substituents selected from the group consisting of H, CH.sub.3, CF.sub.3, F, Cl, and OCH.sub.3 ; R.sub.2 and R.sub.3, which may be the same or different, and are selected from the group consisting of H and (C.sub.1 -C.sub.4) alkoxy, or R.sub.2 and R.sub.3 taken together can form a chain selected from the group consisting of --O-- (CH.sub.2).sub.n --O--, wherein n=1 or 2 and --O--CH.sub.2 --O--CH.sub.2 with the proviso that R.sub.1 is not meta CF.sub.3 when R.sub.2 =R.sub.3 =H, and pharmaceutically non-toxic salts thereof. The compounds of this invention are useful in the treatment of allergic and anaphylatic conditions and motion sickness.

    摘要翻译： 本发明涉及2-（4-苯基哌嗪基乙基）苯胺，其制备方法及其在药物治疗中的用途。 这些化合物具有下列通式（I）其中R 1表示一个或多个选自H，CH 3，CF 3，F，Cl和OCH 3的取代基; R 2和R 3可以相同或不同，并且选自H和（C 1 -C 4）烷氧基，或者R 2和R 3一起可以形成选自-O-（CH 2 ）nO-，其中n = 1或2和-O-CH 2 -O-CH 2，条件是当R 2 = R 3 = H时R 1不为CF 3，及其药学上无毒的盐。 本发明的化合物可用于治疗过敏性和过敏性疾病和晕车病。