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    Nouveaux stéroîdes 9(11) saturés substitués en position 10 par un radical comportant une triple liaison, leur procédé de préparation, leur application comme médicaments, les compositions pharmaceutiques les renfermant
    56.
    发明授权
    Nouveaux stéroîdes 9(11) saturés substitués en position 10 par un radical comportant une triple liaison, leur procédé de préparation, leur application comme médicaments, les compositions pharmaceutiques les renfermant 失效
    9（11）中饱和的STEROIDS和通过含有三重键的放射性位置10替代它们的制备方法，它们作为含有它们的药物和药物组合物使用

    公开(公告)号：EP0237397B1

    公开(公告)日：1990-02-07

    申请号：EP87400406.2

    申请日：1987-02-24

    申请人： ROUSSEL-UCLAF

    发明人： Nedelec, Lucien ,  Nique, Francois ,  Moura, Anne-Marie

    IPC分类号： C07J1/00 ,  C07J21/00 ,  A61K31/565 ,  A61K31/585 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J53/00

    CPC分类号： C07J21/006 ,  C07J1/007 ,  C07J21/003 ,  C07J33/005 ,  C07J43/006

    摘要： 1. The products of general formula I : see diagramm : EP0237397,P31,F2 in which R represents : - either a hydrogen atom, - or an alkyl, alkenyl or alkynyl radical having at most 8 carbon atoms possibly substituted by a radical chosen from the following radicals : hydroxyl, carboxy, methoxycarbonyl, ethoxycarbonyl, amino, tritylamino, chloroacetylamino, trifluoroacetylamino, trichloroethoxycarbonylamino, methylamino, dimethylamino or halogen, - or an aryl or aralkyl radical optionally substituted by a radical chosen from the following radicals : hydroxyl carboxy, methoxycarbonyl, ethoxycarbonyl, amino, methylamino, dimethylamino, methyl methoxy or methylthio, - or an alkoxy, carboxy, methoxycarbonyl, ethoxycarbonyl or dialkylamino radical, - or a hydrogen atom, - or a trialkylsilyl radical, R6 and R7 are such that, either R6 and R7 form with the carbons that carry them a cyclopropyl radical, or R6 represents a hydrogen atom and R7 represents the R1 radical, R1 representing : - either a hydrogen atom, - or an alkyl, alkenyl or alkynyl radical having at most 6 carbon atoms, optionally substituted by a radical chosen from the following radicals : hydroxyl, carboxy, methoxycarbonyl, ethoxycarbonyl, amino, tritylamino, chloroacetylamino, trifluoroacetylamino, trichloroethoxy-carbonylamino, methylamino, dimethylamino or halogen, - or an acetylthio radical, R2 represents a methyl or ethyl radical, X and Y are such that : - either X represents a hydroxyl, acetyloxy, propionyloxy, methoxy or ethoxy radical and Y represents either a -CH2 CH2 CO2 M in which M represents a hydrogen atom, an alkali metal atom or an ammonium radical, - or a -CH2 CH2 -CH2 OH radical - or X and Y together represent a radical : see diagramm : EP0237397,P32,F1 or see diagramm : EP0237397,P32,F2 - or X and Y together represent a radical see diagramm : EP0237397,P32,F3 in which alk represents an alkyl radical containing at most 8 carbon atoms, - or X and Y together represent a radical see diagramm : EP0237397,P32,F4 or X represents a hydroxyl radical and Y a see diagramm : EP0237397,P32,F5 M being defined as above, - or X represents a hydroxyl, acetyloxy, propionyloxy, methoxy or ethoxy radical and Y represents, either a hydrogen atom or Y represents R4 , R4 representing an alkyl, alkenyl or alkynyl radical having at most 6 carbon atoms, the dotted lines at position 1 (2) and 6 (7) indicate the possible presence of a second bond between the carbons that carry them, it being understood that there cannot be a second bond at position 6 (7) when R6 and R7 form a cyclopropyl radical with the carbons which carry them, the wavy lines at position 6 and 7 indicate that the substituents R6 and R7 can be found at one of the possible positions alpha or beta, it being understood that R cannot represent a hydrogen atom when R6 and R7 each represent a hydrogen atom, R2 represents a methyl radical, X represents a hydroxy, acetyloxy, propionyloxy, methoxy or ethoxy radical and Y represents a hydrogen atom or R4 and the dotted lines at position 1 (2) and 6 (7) together do not represent a second bond between the carbons which carry them.

    摘要翻译： 1.通式I的产物：参见图示：EP0237397，P31，F2，其中R表示： - 氢原子，或至多8个碳原子的烷基，烯基或炔基可能被选自以下的基团取代： 以下基团：羟基，羧基，甲氧基羰基，乙氧基羰基，氨基，三苯甲基氨基，氯乙酰氨基，三氟乙酰氨基，三氯乙氧基羰基氨基，甲基氨基，二甲基氨基或卤素，或任选被选自以下基团的基团取代的芳基或芳烷基：羟基羧基， ，乙氧基羰基，氨基，甲基氨基，二甲基氨基，甲基甲氧基或甲硫基， - 或烷氧基，羧基，甲氧基羰基，乙氧基羰基或二烷基氨基， - 或氢原子 - 或三烷基甲硅烷基，R6和R7， R7与带有环丙基的碳形成，或R6表示氢原子，R7表示R1基团，R1表示： - 氢原子，或具有至多6个碳原子的烷基，烯基或炔基，任选被选自以下基团的基团取代：羟基，羧基，甲氧基羰基，乙氧基羰基，氨基，三苯甲基氨基，氯乙酰氨基，三氟乙酰氨基，三氯乙氧基 - 羰基氨基， 甲基氨基，二甲基氨基或卤素， - 或乙酰基硫基，R 2表示甲基或乙基，X和Y为： - X表示羟基，乙酰氧基，丙酰氧基，甲氧基或乙氧基，Y表示-CH2 CH2 其中M表示氢原子，碱金属原子或铵基，或-CH 2 CH 2 -CH 2 OH基团的CO 2 M或X和Y一起表示基团：参见图示：EP0237397，P32，F1或参见图 ：EP0237397，P32，F2-或X和Y一起代表基团参见图：EP0237397，P32，F3，其中alk代表含有至多8个碳原子的烷基，或X和Y一起代表基团：EP0 237397，P32，F4或X表示羟基，Y a见图：EP0237397，P32，F5M如上所定义， - 或X表示羟基，乙酰氧基，丙酰氧基，甲氧基或乙氧基，Y表示氢 原子或Y表示R4，R4表示具有至多6个碳原子的烷基，烯基或炔基，位置1（2）和6（7）处的虚线表示在携带它们的碳之间可能存在第二键 ，当R6和R7与携带它们的碳形成环丙基时，在6（7）处不能有第二个键，第6和7位的波浪线表示可以发现取代基R6和R7 在可能的位置α或β中，应理解当R 6和R 7各自表示氢原子时，R不能表示氢原子，R 2表示甲基，X表示羟基，乙酰氧基，丙酰氧基，甲氧基或乙氧基， Y表示氢 原子或R 4和位置1（2）和6（7）处的虚线一起不表示携带它们的碳之间的第二键。

    Aromatic heterocyclic esters of steroids, their preparation and pharmaceutical compositions containing them
    60.
    发明公开
    Aromatic heterocyclic esters of steroids, their preparation and pharmaceutical compositions containing them 失效
    芳香族杂环类固醇酯，其制备方法和含有它们的药物组合物。

    公开(公告)号：EP0057401A1

    公开(公告)日：1982-08-11

    申请号：EP82100490.0

    申请日：1982-01-25

    申请人： SCHERING CORPORATION

    发明人： Shapiro, Elliot L.

    IPC分类号： C07J17/00 ,  C07J33/00 ,  C07J43/00 ,  A61K31/58

    CPC分类号： C07J33/002 ,  C07J17/00 ,  C07J43/003

    摘要： Disclosed herein are novel 3,20-dioxo-1,4-pregnadiene-17-01-17-aromatic heterocyclic carboxylates (and the 6-dehydro and 1,2-dihydro derivatives thereof) of general formula I:
    wherein:

    A is hydrogen or, provided that Y is (H,βOH), A may also be chloro, fluoro or methyl;
    X is hydrogen or a halogen atom having an atomic weight less than 100;
    Y is oxygen, (H,βOH) or, provided that X is hydrogen, Y may also be (H,H) or, provided X is chloro or bromo, Y may also be (H,β-halogen), the β-halogen having an atomic weight less than 100 and being at least as electronegative as X;
    Z is hydrogen, methyl, chloro or fluoro;
    Z' is hydrogen or, provided that Z is hydrogen, may also be halogen having an atomic weight of less than 100;
    V is an acyl radical of a thiophenecarboxylic acid, pyrrolecarboxylic acid or furancarboxylic acid or the methyl- or halogen-substituted derivatives thereof;
    W is (H,H), (H, lower alkyl) or (H, aOV,) where V, is hydrogen or specified acyl radicals, or W is a methylene or substituted methylene group; and
    G is hydrogen, a halogen atom having an atomic weight of less than 100 or is -QV 2 where Q is oxygen or sulfur and V 2 is specified acyl radicals.

    The novel compounds exhibit anti-inflammatory activity and their use for this purpose is disclosed. Also disclosed are methods for the preparation of the novel compounds.