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    SOFT STEROIDS HAVING ANTI-INFLAMMATORY ACTIVITY
    2.
    发明授权
    SOFT STEROIDS HAVING ANTI-INFLAMMATORY ACTIVITY 失效
    具有抗炎活性的软性甾体化合物

    公开(公告)号：EP0334853B1

    公开(公告)日：1993-06-09

    申请号：EP87907186.8

    申请日：1987-10-13

    申请人： BODOR, Nicholas S.

    发明人： BODOR, Nicholas S.

    IPC分类号： C07J1/00 ,  A61K31/56 ,  A61K31/58 ,  C07J21/00

    CPC分类号： C07J31/006 ,  C07J3/005 ,  C07J21/006

    摘要： Novel soft steroid anti-inflammatory agents, said agents being esters or thioesters of 17alpha-alkoxy-11beta-hydroxyandrost-4-en-3-one-17beta-carboxylic acids, pharmaceutical compositions containing said agents, novel chemical intermediates useful in the preparation of said agents and methods of administering same to mammals in the treatment of inflammation. Preferred compounds are the haloalkyl esters of 17alpha-alkoxy-11beta-hydroxyandrost-4-en-3-one-17beta-carboxylic acids.

    COMBINATION OF STEROIDS HAVING TRANSPORTER-ENHANCED CORTICOSTEROID ACTIVITY
    4.
    发明授权
    COMBINATION OF STEROIDS HAVING TRANSPORTER-ENHANCED CORTICOSTEROID ACTIVITY 有权
    类固醇具有先进的运输类固醇活动组合

    公开(公告)号：EP2026818B1

    公开(公告)日：2010-12-22

    申请号：EP07795241.4

    申请日：2007-05-24

    申请人： Bodor, Nicholas S.

    发明人： Bodor, Nicholas S.

    IPC分类号： A61K31/568 ,  A61P29/00

    CPC分类号： C07J5/0053 ,  A61K31/568 ,  C07J3/005 ,  A61K2300/00

    摘要： Combinations and compositions for use in enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17α-alkoxycarbonyloxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4-compounds are described. The enhancing agents have the formula:(II) wherein Z1 is carbonyl, β-hydroxymethylene or methylene; R2 is H, -OH or -OCOR3 wherein R3 is C1-C5 alkyl; Y is -OH, -SH or -OCOR4 wherein R4 is C1-C5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Also use of the combinations and compositions in treating topical or other localized inflammation.

    ORALLY ACTIVE HEPARIN MULTIPLETS
    5.
    发明授权
    ORALLY ACTIVE HEPARIN MULTIPLETS 失效

    公开(公告)号：EP0189427B1

    公开(公告)日：1989-02-08

    申请号：EP85902404.4

    申请日：1985-05-08

    申请人： BODOR, Nicholas S.

    发明人： BODOR, Nicholas S.

    IPC分类号： C08B37/10 ,  C07H13/04 ,  C07C101/28 ,  C07D213/79 ,  C07D213/55 ,  C08B37/16 ,  A61K31/725

    CPC分类号： C07D213/80 ,  C07D213/55 ,  C07D213/82 ,  C07D295/15 ,  C07H3/04 ,  C07H3/06 ,  C07H13/04 ,  C07H13/10 ,  C08B37/0075

    摘要： Novel orally active ion multiplets of formula (I) in which $(1,5)$ is the skeleton of a polyol, n is the number of OH's in the polyol (3 to 24); p is >= 3 and = 3 and

    摘要翻译： 其中$（1,5）$是多元醇骨架的新的式（I）口服活性离子多重峰，n是多元醇中OH的数目（3-24）; p是> = 3且<= n; r是肝素单位的可用化合价并且≥3且≤7; sr等于pv; 并且R +是（a），（b），（c），（d）或（e），其中Riv是C 1 -C 3烷基; R'和R“为C1-C7烷基，相同或不同或组合使得-NR'R”代表饱和单环仲胺的残基; R“'与天然氨基酸的相应部分相同; 亚烷基含有1至3个碳原子; 和Rv是H，-CONH 2或-COO（C 1 -C 7烷基）。 多重态是稳定的脂质“离子对”或复合物，可通过胃肠壁吸收并缓慢释放肝素酸以达到持久的抗凝血活性。 也公开了作为本发明多重态中间体的新型季盐。