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    Pharmaceutical compositions and dietary soybean food products for the prevention of osteoporosis
    13.
    发明授权
    Pharmaceutical compositions and dietary soybean food products for the prevention of osteoporosis 失效
    药物组合物和膳食大豆食品预防骨质疏松症

    公开(公告)号：US5424331A

    公开(公告)日：1995-06-13

    申请号：US258460

    申请日：1994-06-10

    申请人： Mark Shlyankevich

    发明人： Mark Shlyankevich

    IPC分类号： A61K31/35 ,  A61K36/236

    CPC分类号： A61K36/236 ,  Y10S514/874

    摘要： A composition for the treatment or prevention of osteoporosis, is disclosed, which comprises:(a) 75 to 200 parts of one or more phytoestrogen compounds;(b) 0 to 100 parts of dried licorice root extract;(c) 300 to 600 parts of calcium contained in a biologically acceptable calcium salt;(d) 70 to 280 parts of magnesium contained in a biologically acceptable magnesium salt;(e) 4 to 25 parts of zinc contained in a biologically acceptable zinc salt;(f) 5 to 20 parts of beta-carotene;(g) 0.005 to 0.010 parts of Vitamin D as cholecalciferol; and(h) 6 to 12 parts of Vitamin E,in admixture with a biologically acceptable inert carrier. The new compositions are administered to a mammalian subject as either a pharmaceutical or as a dietary supplement.

    摘要翻译： 一种用于治疗或预防骨质疏松症的组合物，其包括：（a）75至200份一种或多种植物雌激素化合物; （b）0〜100份干甘草根提取物; （c）在生物学上可接受的钙盐中含有300-600份钙; （d）70〜280份生物可接受的镁盐中所含的镁; （e）4〜25份生物可接受的锌盐中所含的锌; （f）5〜20份β-胡萝卜素; （g）0.005至0.010份维生素D作为胆钙化甾醇; 和（h）6至12份维生素E，与生物可接受的惰性载体混合。 将新组合物作为药物或膳食补充剂施用于哺乳动物受试者。

    High affinity halogenated-tamoxifen derivatives and uses thereof
    14.
    发明授权
    High affinity halogenated-tamoxifen derivatives and uses thereof 失效
    高亲和性卤代三苯氧胺衍生物及其用途

    公开(公告)号：US5219548A

    公开(公告)日：1993-06-15

    申请号：US589928

    申请日：1990-10-01

    申请人： David J. Yang ,  Sidney Wallace

    发明人： David J. Yang ,  Sidney Wallace

    IPC分类号： A61K31/135 ,  A61K31/138 ,  A61K51/00 ,  A61P35/00 ,  C07B59/00 ,  C07C217/18

    CPC分类号： C07B59/001 ,  C07C217/18 ,  Y10S514/874

    摘要： Applicants describe the synthesis of fluorotamoxifen and iodotamoxifen analogs with the halogen atom positioned on the aliphatic chain of the tamoxifen molecule. The halogenated-tamoxifen derivatives possess superior binding affinities to estrogen receptors of pig uteri compared with tamoxifen. The fluorinated tamoxifens have potential use in imaging estrogen receptors by PET whereas the iodinated tamoxifens have potential use in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing fluorotamoxifen and iodotamoxifen derivatives with high specific activity are also disclosed. Fluorotamoxifen and iodotamoxifen derivatives may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors.

    摘要翻译： 申请人描述氟托生素和碘莫昔芬类似物与位于三苯氧胺分子的脂肪链上的卤素原子的合成。 与他莫昔芬相比，卤代 - 他莫昔芬衍生物对猪子宫雌激素受体具有优越的结合亲和力。 氟化三苯氧胺在PET成像雌激素受体成像中具有潜在的用途，而碘化的三苯氧胺可以通过SPECT成像雌激素受体的潜在用途。 还公开了制备具有高比活性的氟莫西芬和碘莫昔芬衍生物的快速有效的方法。 氟他莫昔芬和碘莫昔芬衍生物可有利地用作抗癌治疗剂来阻止雌激素受体阳性肿瘤。

    High affinity tamoxifen derivatives and uses thereof
    15.
    发明授权
    High affinity tamoxifen derivatives and uses thereof 失效
    高亲和力酪氨酸衍生物及其用途

    公开(公告)号：US5192525A

    公开(公告)日：1993-03-09

    申请号：US722322

    申请日：1991-06-28

    申请人： David J. Yang ,  Sidney Wallace

    发明人： David J. Yang ,  Sidney Wallace

    IPC分类号： A61K31/135 ,  A61K31/138 ,  A61K51/00 ,  A61P35/00 ,  C07B59/00 ,  C07C217/18

    CPC分类号： C07B59/001 ,  C07C217/18 ,  Y10S514/874

    摘要： The synthesis of tamoxifen derivatives, most particularly halo, haloalkyl and hydroxy tamoxifen derivatives, wherein the native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule, is provided. Methods for imaging estrogen receptors using the tamoxifen derivatives of the invention are also described. The aliphatic chain substituted tamoxifen derivatives of the invention possess greater estrogen receptor binding affinities and more potent tumor cell inhibiting activity than native tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen, phenolic-ring substituted tamoxifen). Examples of the halogenated tamoxifen derivatives of the invention include chloro-, bromo-, iodo- and fluoro-tamoxifen derivatives, and their corresponding lower alkyl halogenated forms.

    摘要翻译： 提供了他莫昔芬衍生物，特别是卤代烷基和羟基他莫昔芬衍生物的合成，其中天然的三苯氧胺分子包括位于三苯氧胺分子脂族链上的取代的化学基团。 还描述了使用本发明的他莫昔芬衍生物成像雌激素受体的方法。 本发明的脂肪链取代的他莫昔芬衍生物与分子上其他位置上取代的天然的他莫昔芬或他莫昔芬衍生物（即非脂肪链取代的他莫昔芬，酚环取代的三苯氧胺）具有更大的雌激素受体结合亲和力和更有效的肿瘤细胞抑制活性 ）。 本发明的卤代三苯氧胺衍生物的实例包括氯代，溴代，碘代和氟代三苯氧胺衍生物及其相应的低级烷基卤化形式。

    Device for controlled release drug delivery
    16.
    发明授权
    Device for controlled release drug delivery 失效
    控释药物输送装置

    公开(公告)号：US4792450A

    公开(公告)日：1988-12-20

    申请号：US875824

    申请日：1986-06-18

    申请人： Agis F. Kydonieus ,  Bret Berner

    发明人： Agis F. Kydonieus ,  Bret Berner

    IPC分类号： A61K9/70 ,  A61K47/32 ,  A61K9/00 ,  A61L15/03

    CPC分类号： A61K9/7084 ,  A61K47/32 ,  Y10S514/874 ,  Y10S514/944 ,  Y10S514/947

    摘要： A device for the controlled release and delivery of a pharmacologically active agent, comprising a vinyl gel layer and a pharmacologically active agent uniformly dispersed in the layer in a pharmacologically effective amount, the vinyl layer comprising a polyvinyl chloride resin, a primary plasticizer for the polyvinyl chloride resin, and an organic, nonvolatile gel forming additive in an amount sufficient to form a gel.

    摘要翻译： 用于控制释放和递送药理活性剂的装置，其包含以药理学有效量均匀分散在该层中的乙烯基凝胶层和药理活性剂，所述乙烯基层包含聚氯乙烯树脂，用于聚乙烯醇的主要增塑剂 氯化物树脂和有效的非挥发性凝胶形成添加剂，其量足以形成凝胶。

    .DELTA..sup.1,3,5(10) -Estratrienes
    17.
    发明授权
    .DELTA..sup.1,3,5(10) -Estratrienes 失效
    DELTA 1,3,5（10）-Estratrienes

    公开(公告)号：US4272530A

    公开(公告)日：1981-06-09

    申请号：US867486

    申请日：1978-01-06

    申请人： Jean G. Teutsch ,  Daniel Philibert

    发明人： Jean G. Teutsch ,  Daniel Philibert

    IPC分类号： A61K31/565 ,  A61K31/58 ,  C07J1/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J51/00 ,  C07J71/00 ,  A61K31/56 ,  C07J3/00

    CPC分类号： C07J51/00 ,  C07J1/0096 ,  C07J21/006 ,  C07J33/002 ,  C07J7/0045 ,  C07J71/001 ,  Y10S514/874

    摘要： Novel 11.beta. -substituted-.DELTA. .sup.1,3,5(10) -estratrienes of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of optionally substituted unsaturated alkyl of 2 to 8 carbon atoms, optionally substituted aryl of 6 to 12 carbon atoms, optionally substituted aralkyl of 7 to 13 carbon atoms and heterocycle with at least one sulfur or oxygen heteroatom, R.sub.2 is alkyl of 1 to 4 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 9 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, hydroxy, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 8 carbon atoms, acyloxy of an organic carboxylic acid of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, with the proviso that R.sub.1 is not allyl when Z is hydrogen, R.sub.2 is methyl, R.sub.3 is hydroxy and R.sub.4 is hydrogen having estrogenic activity and their preparation.

    摘要翻译： 新颖的11β-取代的-TATA 1,3,5（10） - 结构式Ⅰ'的三亚甲基，其中R 1选自任选取代的2至8个碳原子的不饱和烷基，任选取代的6至 12个碳原子，任选取代的7至13个碳原子的芳烷基和与至少一个硫或氧杂原子杂环，R 2是1至4个碳原子的烷基，Z选自氢，1至12个碳的烷基 原子和7至9个碳原子的芳烷基，R3选自氢，羟基，1至18个碳原子的有机羧酸的酰基和1至18个碳原子的有机羧酸的酰氧基，R4是 选自氢，羟基，具有1至8个碳原子的烷基和烷氧基，具有1至8个碳原子的有机羧酸的酰氧基和2至8个碳原子的链烯基和炔基，条件是R1不是 Z为氢时为烯丙基，R2为甲基 R3是羟基，R4是具有雌激素活性的氢及其制备。