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    Process for the production of 2,3,5-trimethylhydroquinone diesters
    51.
    发明授权
    Process for the production of 2,3,5-trimethylhydroquinone diesters 失效
    制备2,3,5-三甲基氢醌二酯的方法

    公开(公告)号：US06316661B1

    公开(公告)日：2001-11-13

    申请号：US09493065

    申请日：2000-01-28

    申请人： Steffen Krill ,  Horst Weigel ,  Klaus Huthmacher ,  Nongyuan Shi ,  Georg Markowz ,  Volker Hafner

    发明人： Steffen Krill ,  Horst Weigel ,  Klaus Huthmacher ,  Nongyuan Shi ,  Georg Markowz ,  Volker Hafner

    IPC分类号： C07C6900

    CPC分类号： C07C67/00 ,  Y02P20/582 ,  C07C69/017 ,  C07C69/16 ,  C07C69/28

    摘要： A process for the production of 2,3,5-trimethylhydroquinone diesters by aromatization of 2,6,6-trimethyl-2-cyclohexene-1,4-dione (4-oxoisophorone, ketoisophorone, KIP) with an acylating agent and an acidic soluble or insoluble catalyst, which process may be operated alternatively continuously or discontinuously. The process includes the following steps: a) a carboxylic anhydride having a C1 to C4 alkyl residue is used as the acylating agent, b) after the reaction, a proportion of the resultant carboxylic acid is optionally removed by distillation, c) the reaction solution is cooled, d) the product which has crystallized out is separated and washed, and e) the filtrate is returned to step a).

    摘要翻译： 通过2,6,6-三甲基-2-环己烯-1,4-二酮（4-氧异佛尔酮，酮异佛尔酮，KIP）与酰化剂和酸性化合物的芳构化生产2,3,5-三甲基氢醌二酯的方法 可溶或不溶的催化剂，该方法可以交替连续或不连续地操作。 该方法包括以下步骤：a）具有C1至C4烷基残基的羧酸酐用作酰化剂，b）反应后，任选地通过蒸馏除去所得羧酸的一部分，c）反应溶液 被冷却，d）结晶出来的产物被分离和洗涤，e）将滤液返回到步骤a）。

    Fatty-acid monoesters of estrogens for the treatment of obesity and/or overweight
    54.
    发明授权
    Fatty-acid monoesters of estrogens for the treatment of obesity and/or overweight 失效
    用于治疗肥胖和/或超重的雌激素的脂肪酸单酯

    公开(公告)号：US5798348A

    公开(公告)日：1998-08-25

    申请号：US739165

    申请日：1996-10-30

    申请人： Maria Alemany

    发明人： Maria Alemany

    IPC分类号： C07C69/017 ,  C07C69/28 ,  C07C69/533 ,  C07C69/58 ,  C07C69/587 ,  C07J1/00 ,  A61K31/56 ,  C07C69/00

    CPC分类号： C07C69/533 ,  C07C69/017 ,  C07C69/28 ,  C07C69/58 ,  C07C69/587 ,  C07J1/007

    摘要： The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of an estrogen and a fatty acid wherein the estrogen is estrone, diethylstilbestrol, estriol, estradiol or ethinyl estradiol and the fatty acid is oleic, linoleic, linolenic, stearic, palmitic, palmitoleic or arachidonic acids. The fatty-acid monoesters mimic the function of estrone monooleate, as a signal that informs the brain of the size of fat tissue mass. In preferred pharmaceutical and/or cosmetic compositions for intravenous injection the monoester is incorporated in a lipidic suspension, prepared from lipoproteins or from liposome components, such as soy oil and egg phospholipids. When administered to rats with a 15% of total adipose tissue, they produce weight reduction of about 10%, by a new and unexpected mechanism. They are useful for the treatment of obesity and/or overweight in mammals, with the advantages of high efficacy and low toxicity. New substantially pure fatty-acid monoesters including estrone monooleate and diethylstilbestrol monooleate are also described.

    摘要翻译： 用于治疗肥胖和/或超重的药物和/或化妆品组合物含有有效量的雌激素和脂肪酸的脂肪酸单酯，其中雌激素是雌酮，己烯雌酚，雌三醇，雌二醇或乙炔雌二醇和脂肪酸 是油酸，亚油酸，亚麻酸，硬脂酸，棕榈酸，棕榈油酸或花生四烯酸。 脂肪酸单酯模仿雌酮单油酸酯的功能，作为通知大脑脂肪组织质量大小的信号。 在用于静脉内注射的优选药物和/或化妆品组合物中，将单酯掺入由脂蛋白或脂质体组分如大豆油和蛋磷脂制备的脂质悬浮液中。 当给予15％的总脂肪组织的大鼠时，它们通过新的和意想不到的机制产生约10％的体重减轻。 它们可用于治疗哺乳动物肥胖和/或超重，具有疗效高，毒性低的优点。 还描述了包括单酯酸酯和己烯雌酚单油酸酯的新的基本上纯的脂肪酸单酯。

    Vicinal glycol ester preparation process
    56.
    发明授权
    Vicinal glycol ester preparation process 失效
    乙二醇酯制备方法

    公开(公告)号：US3907874A

    公开(公告)日：1975-09-23

    申请号：US27890372

    申请日：1972-08-09

    申请人： HALCON INTERNATIONAL INC

    发明人： HARVEY ROBERT JOSEPH ,  KOLLAR JOHN ,  SCHMIDT JOHN PHILIP

    IPC分类号： C07C67/05 ,  B01J27/00 ,  B01J27/08 ,  B01J31/00 ,  C07B61/00 ,  C07C69/02 ,  C07C67/08 ,  C07C69/16

    CPC分类号： B01J27/08 ,  C07C67/05 ,  Y02P20/582 ,  C07C69/16 ,  C07C69/28

    摘要： When vicinal glycol esters are prepared by the liquid phase reaction of (a) ethylene or propylene, (b) molecular oxygen and (c) a carboxylic acid in the presence of a catalyst system which is tellurium cation plus bromide anion or selenium cation plus chloride anion or selenium cation plus bromide anion, significant improvements in selectivity and operability are obtained by employing, in conjunction with these catalyst systems, a basicity control cation of specified characteristics. This cation is employed in an amount at least sufficient to provide at least 0.05 equivalent of cation per gram-atom of halogen present.

    摘要翻译： 当连环乙二醇酯通过（a）乙烯或丙烯的液相反应，（b）分子氧和（c）羧酸在催化剂体系的存在下制备，所述催化剂体系是碲阳离子加溴化物阴离子或硒阳离子加氯化物 阴离子或硒阳离子加溴化物阴离子，通过与这些催化剂体系结合使用具有特定特征的碱性控制阳离子，可以获得显着的选择性和可操作性的改善。 该阳离子的使用量至少足以提供每克原子卤素存在至少0.05当量的阳离子。