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    Nanoparticles Designed for Drug Delivery
    2.
    发明申请
    Nanoparticles Designed for Drug Delivery 审中-公开
    设计用于药物输送的纳米颗粒

    公开(公告)号：US20090297613A1

    公开(公告)日：2009-12-03

    申请号：US12223420

    申请日：2007-02-02

    申请人： Kerstin Ringe ,  Hans-Eckart Radunz ,  Julia Kubasch

    发明人： Kerstin Ringe ,  Hans-Eckart Radunz ,  Julia Kubasch

    IPC分类号： A61K9/14

    CPC分类号： A61K9/5138 ,  A61K9/5192 ,  A61K49/0043 ,  A61K49/0054 ,  A61K49/0093

    摘要： The present invention is directed to a method of producing nanoparticles by the miniemulsion method, said nanoparticles being made by adding a defined amount of stabilizer to the reaction system. The present invention is further directed to nanoparticles made by this method and their use for the treatment of diseases and conditions, requiring a pharmaceutical agent to cross one or more physiological barriers, in particular the blood-brain barrier.

    摘要翻译： 本发明涉及通过细乳液法制备纳米颗粒的方法，所述纳米颗粒通过向反应体系中加入限定量的稳定剂而制备。 本发明还涉及通过该方法制备的纳米颗粒及其用于治疗疾病和病症的用途，需要药剂穿过一个或多个生理屏障，特别是血脑屏障。

    1,4-Oxathianes
    4.
    发明授权
    1,4-Oxathianes 失效

    公开(公告)号：US4125622A

    公开(公告)日：1978-11-14

    申请号：US860355

    申请日：1977-12-14

    申请人： Hans-Eckart Radunz ,  Dieter Orth ,  Manfred Baumgarth ,  Reinhard Lissner ,  Jurgen Maisenbacher

    发明人： Hans-Eckart Radunz ,  Dieter Orth ,  Manfred Baumgarth ,  Reinhard Lissner ,  Jurgen Maisenbacher

    IPC分类号： A61K31/39 ,  A61P7/02 ,  C07D327/06

    CPC分类号： C07D327/06 ,  Y10S514/822

    摘要： 1,4-Oxathianes of the formula ##STR1## and the physiologically-acceptable salts thereof wherein R.sup.1 is H or alkyl with 1-4 C-atoms; R.sup.2 is H or alkyl with 1-4 C-atoms; R.sup.3 is H, alkyl with 1-8 C-atoms, phenyl or phenyl substituted by F, Cl, Br, OH, OCH.sub.3, CF.sub.3 or NO.sub.2 ; R.sup.4 is H or CH.sub.3 ; B is a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 O--; and a wavy line ( ) indicates that these bonds can be in the .alpha.- or .beta.- positions possess thrombocyte inhibition properties.

    摘要翻译： 具有式“IMAGE”的1,4-氧硫辛酸和其生理学上可接受的盐，其中R 1是H或具有1-4个C原子的烷基; R2是H或具有1-4个C原子的烷基; R3是H，具有1-8个C原子的烷基，被F，Cl，Br，OH，OCH3，CF3或NO2取代的苯基或苯基; R4是H或CH3; B是单键，-CH 2 - ， - CH 2 CH 2 - 或-CH 2 O- 和波浪线（）表示这些键可以在α或β位具有血细胞抑制性质。

    Sulfur-containing 6-ketoprostaglandins
    6.
    发明授权
    Sulfur-containing 6-ketoprostaglandins 失效
    含硫6孔松脂腺苷

    公开(公告)号：US4680288A

    公开(公告)日：1987-07-14

    申请号：US692490

    申请日：1985-01-18

    申请人： Klaus Irmscher ,  Hans-Eckart Radunz ,  Ernst Schulze ,  Bernhard Riefling

    发明人： Klaus Irmscher ,  Hans-Eckart Radunz ,  Ernst Schulze ,  Bernhard Riefling

    IPC分类号： C07D333/18 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/70 ,  C07D309/12 ,  C07F7/18 ,  C07C177/00

    CPC分类号： C07C405/0033

    摘要： Sulfur-containing 6-ketoprostaglandins of the formula I ##STR1## in which D is a bond, alkylene having 1-3 C atoms, cis-alkenylene having 2-5 C atoms or alkinylene having 2-5 C atoms,R.sup.1 is H, alkyl having 1-4 C atoms, aryl having 6-12 C atoms or --C.sub.6 H.sub.4 NHCOC.sub.6 H.sub.5,R.sup.2 is alkyl having 1-7 C atoms, alkyl having 1-7 C atoms which is substituted by halogen, cycloalkyl having 5-6 C atoms, cycloalkyl having 5-6 C atoms which is substituted by alkyl having 1-4 C atoms, phenyl, phenyl which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3, pyridyl, naphthyl, thienyl or, if D is alkylene having 1-3 C atoms, also is alkoxy having 1-4 C atoms, alkylthio having 1-4 C atoms, phenoxy or phenoxy which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3,R.sup.3 and R.sup.4 each are H, alkyl having 1-7 C atoms, tetrahydro-2-pyranyl, trialkylsilyl having a total of 3-12 C atoms, aryldialkylsilyl having a total of 8-18 C atoms, alkoxymethyl having 2-5 C atoms, aryloxymethyl having 7-11 C atoms or acyl having 1-10 C atoms, andR.sup.5 is H or alkyl having 1-3 C atoms, and.... indicates that this bond is .alpha., indicates that this bond is .beta.,and, where R.sub.1 is H, their salts, show effects on the circulation, in particular hypotensive effects, as well as effects on the force of myocardial contraction.

    摘要翻译： 其中D为键的式I化合物I-I，含有1-3个C原子的亚烷基，具有2-5个C原子的顺式亚烯基或具有2-5个C原子的亚炔基的含硫的6-酮基前列腺素，R1为H 具有1-4个C原子的烷基，具有6-12个碳原子的芳基或-C6H4NHCOC6H5的芳基，R2是具有1-7个C原子的烷基，具有1-7个C原子的被卤素取代的烷基，具有5-6个C原子的环烷基 由具有1-4个C原子的烷基取代的具有5-6个碳原子的环烷基，苯基，被F，Cl，Br，具有1-4个C原子的烷基取代的苯基，OH，OCH3或CF3，吡啶基，萘基 ，噻吩基或如果D是具有1-3个C原子的亚烷基，也是具有1-4个C原子的烷氧基，具有1-4个C原子的烷硫基，被F，Cl，Br取代的苯氧基或苯氧基， 4个C原子，OH，OCH 3或CF 3，R 3和R 4各自为H，具有1-7个C原子的烷基，四氢-2-吡喃基，总共3-12个C原子的三烷基甲硅烷基，共有8-18个芳基二烷基甲硅烷基 C原子，具有2-5个C原子的烷氧基甲基，芳氧基甲基 具有1-10个碳原子的7-11个C原子或酰基，R5是H或具有1-3个C原子的烷基，...表示该键为α，表示该键为β，并且其中 R1是H，它们的盐，对循环有显着影响，特别是降压作用，以及对心肌收缩力的影响。

    Thiaprostaglandins
    9.
    发明授权
    Thiaprostaglandins 失效

    公开(公告)号：US4080458A

    公开(公告)日：1978-03-21

    申请号：US576140

    申请日：1975-05-09

    申请人： Hans-Eckart Radunz ,  Josef Kramer ,  Manfred Baumgarth ,  Dieter Orth

    发明人： Hans-Eckart Radunz ,  Josef Kramer ,  Manfred Baumgarth ,  Dieter Orth

    IPC分类号： C07D333/34 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C20060101 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/32 ,  C07C177/00 ,  A61K31/19 ,  A61K31/215

    CPC分类号： C07C405/0033 ,  Y02P20/55

    摘要： 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH.sub.2 --CH.sub.2 -- or --CH=CH--, R.sup.1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH=CH--, additionally 4, 5, 6, 7, 8 or 9, R.sup.2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH.sub.3 or OF.sub.3 or phenoxy substituted by F, Cl, Br, OH, OCH.sub.3, CH.sub.3 or CF.sub.3 or, when B is --CH=CH--, additionally hydrogen, phenyl or tolyl, R.sup.3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.

    摘要翻译： 其中A是-CO-或-CHOH-，B是-CH 2 -CH 2 - 或-CH = CH-，R 1是H或1-4个碳原子的烷基，m是 0至5的整数，n为0至3的整数，或当B为-CH = CH-时，另外为4，5，6，7，8或9，R 2为1至4个碳原子的烷氧基 苯氧基，吡啶基，噻吩基，萘基，被F，Cl，Br，OH，OCH3或OF3取代的苯基或被F，Cl，Br，OH，OCH3，CH3或CF3取代的苯氧基，或当B为-CH = CH- ，另外是氢，苯基或甲苯基，R3是H，甲基或乙基，具有药理活性，包括降血压活性。