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    5-amino-4-hydroxyhexanoic acid derivatives
    1.
    发明授权
    5-amino-4-hydroxyhexanoic acid derivatives 失效
    5-氨基-4-羟基己酸衍生物

    公开(公告)号：US5643878A

    公开(公告)日：1997-07-01

    申请号：US207646

    申请日：1994-03-08

    申请人： Guido Bold ,  Marc Lang ,  Alexander Fassler ,  Hans-Georg Capraro ,  Shripad Bhagwat ,  Peter Schneider ,  Peter van Hoogevest

    发明人： Guido Bold ,  Marc Lang ,  Alexander Fassler ,  Hans-Georg Capraro ,  Shripad Bhagwat ,  Peter Schneider ,  Peter van Hoogevest

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  A61K31/535 ,  C07P265/06

    CPC分类号： C07K5/0207 ,  C07K7/02 ,  A61K38/00

    摘要： Compounds of formula I ##STR1## or their hydroxy-protected derivatives, and compounds of formula I' ##STR2## wherein T is an acyl radical of formula Z ##STR3## wherein R.sup.z is unsubstituted or substituted hydrocarbyl wherein at least one carbon atom has been replaced by a hetero atom with the proviso that a hetero atom is not bonded directly to the carbonyl to which the radical R.sup.z is bonded, alkyl having two or more carbon atoms, lower alkenyl, lower alkynyl, aryl or unsubstituted or substituted amino, and wherein the radicals R.sub.1, B.sub.1, R.sub.2, R.sub.3, A.sub.1, A.sub.2 and NR.sub.4 R.sub.5 are as defined in the description, and precursors thereof, are described. The compounds have pharmaceutical activity, for example in the treatment of retroviral diseases, such as AIDS.

    摘要翻译： 式I化合物（I）或其羟基保护的衍生物和式I'化合物（I'）其中T是式Z的酰基（Z），其中R z是未取代的或 取代的烃基，其中至少一个碳原子已经被杂原子替代，条件是杂原子不直接键合到与基团Rz键合的羰基上，具有两个或更多个碳原子的烷基，低级链烯基，低级炔基 ，芳基或未取代或取代的氨基，并且其中基团R 1，B 1，R 2，R 3，A 1，A 2和NR 4 R 5如说明书中所定义，及其前体。 该化合物具有药物活性，例如用于治疗逆转录病毒疾病，例如艾滋病。

    Organic compounds
    4.
    发明授权
    Organic compounds 失效
    有机化合物

    公开(公告)号：US06683100B2

    公开(公告)日：2004-01-27

    申请号：US09233408

    申请日：1999-01-19

    申请人： Peter van Hoogevest

    发明人： Peter van Hoogevest

    IPC分类号： A61K31425

    CPC分类号： A61K9/19 ,  A61K9/0019 ,  A61K47/10 ,  A61K47/26

    摘要： Pharmaceutical formulations comprising an epothilone in the form of an infusion concentrate or a lyophilised composition, and methods of administration of an epothilone in suitable form for parenteral administration.

    摘要翻译： 包含输注浓缩物或冻干组合物形式的埃坡霉素的药物制剂，以及以适合形式用于肠胃外给药的埃坡霉素的给药方法。

    Process for the preparation of a liposome dispersion under elevated pressure contents
    10.
    发明授权
    Process for the preparation of a liposome dispersion under elevated pressure contents 失效
    在高压含量下制备脂质体分散体的方法

    公开(公告)号：US5700482A

    公开(公告)日：1997-12-23

    申请号：US483912

    申请日：1995-06-07

    申请人： Lene Frederiksen ,  Klaus Anton ,  Peter van Hoogevest

    发明人： Lene Frederiksen ,  Klaus Anton ,  Peter van Hoogevest

    IPC分类号： A61K9/127 ,  A61K47/24 ,  B01J13/02

    CPC分类号： A61K9/1277

    摘要： The invention relates to a novel, advantageous process for the preparation of liposomes for the inclusion of water-soluble or hydrophilic substances or mixtures of substances, which process provides the surprising advantage, in comparison with known processes, that the proportion of substances or mixtures of substances actually included is increased and which, when used pharmaceutically, provides the advantage of sterile working conditions. In this process, a mixture consisting of at least one phospholipid and customary lipophilic excipients is subjected to a mobile carrier phase consisting of carbon dioxide and a polar organic solvent (modifier) under supercritical pressure and temperature conditions, the compressed mixed phase is reduced to normal pressure and transferred to an aqueous phase comprising a substance having water-soluble or hydrophilic properties for encapsulation in liposomes.

    摘要翻译： 本发明涉及用于制备用于包含水溶性或亲水性物质或物质混合物的脂质体的新颖有利的方法，与已知方法相比，该方法提供了惊人的优点，即物质或混合物的比例 实际包括的物质增加，当药物使用时，提供无菌工作条件的优点。 在该方法中，将由至少一种磷脂和常规亲脂性赋形剂组成的混合物在超临界压力和温度条件下经受由二氧化碳和极性有机溶剂（改性剂）组成的流动载体相，压缩混合相降至正常 压力并转移到包含具有水溶性或亲水性的物质的水相中以包封在脂质体中。