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    11.alpha.-hydroxy-steroid-4,6-dien-3-one compounds and a process for their preparation
    1.
    发明公开
    11.alpha.-hydroxy-steroid-4,6-dien-3-one compounds and a process for their preparation 失效
    羟基类固醇-4,6-二烯-3-酮在Verbindungen和ein Verfahren zu ihrer Herstellung

    公开(公告)号：EP1167380A2

    公开(公告)日：2002-01-02

    申请号：EP01122428.4

    申请日：1996-12-11

    申请人： G.D. Searle & Co.

    发明人： NG, John S. ,  Wang, Ping T. ,  Baez, Julio A. ,  Liu, Chin ,  Anderson, Dennis K. ,  Lawson, Jon P. ,  Erb, Dernhard ,  Wieczorek, Joseph ,  Mucciariello, Gennaro ,  Vanzanella, Fortunato ,  Kunda, Sastry A. ,  Letendre, Leo J. ,  Pozzo, Mark J. ,  Sing, Yuen-Lung L. ,  Yonan, Edward E.

    IPC分类号： C07J21/00 ,  C07J31/00 ,  C07J53/00 ,  C07J71/00 ,  C12P33/00 ,  C12P33/10 ,  C12Q1/02

    CPC分类号： C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J53/002 ,  C07J71/0015

    摘要： Compounds of Formula VIII
    wherein

    -A-A- represents the group -CHR 4 -CHR 5 - or -CR 4 =CR 5 -,
    R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy,
    -B-B- represents the group -CHR 6 -CHR 7 - or an alpha- or beta- oriented group:

    where R 6 and R 7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and
    R 8 and R 9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R 8 and R 9 together comprise a carbocyclic or heterocyclic ring structure, or R 8 and R 9 together with R 6 or R 7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring,
    their intermediates and processes for preparing them.

    摘要翻译： 式VIII的化合物其中-AA表示基团-CHR 4 -CHR 5 - 或-CR 4 = CR 5 - ，R 3，R 4和R 4， 5“独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳氧基，-BB-表示基团-CHR 6 -CHR 7 - 或 α-或β-取代基团：CHEM，其中R 6和R 7独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基 ，氰基，芳氧基和R 8和R 9独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基或R R 8和R 9一起包含碳环或杂环结构，或R 8和R 9与R 6或R 7一起包含与五环D稠合的碳环或杂环结构 环，其中间体和制备它们的过程。

    Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
    4.
    发明公开
    Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 失效
    中间体9,11-Epoxysteroiden的准备和其制备方法

    公开(公告)号：EP1170299A2

    公开(公告)日：2002-01-09

    申请号：EP01122427.6

    申请日：1996-12-11

    申请人： G.D. Searle & Co.

    发明人： NG, John S. ,  Wang, Ping T. ,  Baez, Julio A. ,  Liu, Chin ,  Anderson, Dennis K. ,  Lawson, Jon P. ,  Erb, Dernhard ,  Wieczorek, Joseph ,  Mucciariello, Gennaro ,  Vanzanella, Fortunato ,  Kunda, Sastry A. ,  Letendre, Leo J. ,  Pozzo, Mark J. ,  Sing, Yuen-Lung L. ,  Yonan, Edward E.

    IPC分类号： C07J21/00 ,  C07J31/00 ,  C07J53/00 ,  C07J71/00 ,  C12P33/00 ,  C12P33/10 ,  C12Q1/02

    CPC分类号： C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J53/002 ,  C07J71/0015

    摘要： Compounds of Formula II:
    and
    compounds of Formula IV:
    wherein

    -A-A- represents the group -CHR 4 -CHR 5 - or -CR 4 =CR 5 -
    R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxy carbonyl, cyano, aryloxy,
    R 1 represents an alpha-oriented lower alkoxycarbonyl or hydroxycarbonyl radical,
    -B-B- represents the group -CHR 6 -CHR 7 - or an alpha- or beta- oriented group:

    where R 6 and R 7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and
    R 8 and R 9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryioxy, or R 8 and R 9 together comprise a carbocyclic or heterocyclic ring structure, or R 8 or R 9 together with R 6 or R 7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring,
    and R 2 is lower alkylsulfonyloxy or acyloxy or a halide
    and process for preparing them.

    摘要翻译： 式II的化合物：和化合物式IV： worin -AA- darstellt组-CHR <4> -CHR <5> - 或-CR <4> = CR <5> - R的<3 >，R <4>和R <5>是unabhängig选自氢，卤素，羟基的，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳基氧基，R <1> darstellt的α-的选择 取向低级烷氧基羰基或羟基自由基，-BB- darstellt组-CHR <6> -CHR <7> - 或α-或β-取向的基团：其中R <6>和R <7>被选择unabhängig 选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，的氰基，芳基氧基，和R <8>和R <9>是unabhängig选自氢中选择的， 卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基，或R <8>和R <9>一起构成碳环或杂环结构，或者R <8> 或R <9>，其中R一起<6>或R <7>包括融合到五环D形环碳环或杂环结构，且R <2>是低级烷基磺酰基或酰氧基或卤化物和制备它们的方法。

    Processes for preparation of 3-keto-7alpha-alkoxycarbonyl-delta-4,5- steroids and intermediates useful therein
    8.
    发明公开
    Processes for preparation of 3-keto-7alpha-alkoxycarbonyl-delta-4,5- steroids and intermediates useful therein 失效
    一种用于3-酮 - 7alpha烷氧羰Delta4,5甾体和其中间体的制备方法

    公开(公告)号：EP1223174A2

    公开(公告)日：2002-07-17

    申请号：EP02007309.4

    申请日：1997-12-11

    申请人： G.D. SEARLE & CO.

    发明人： Ng, John S. ,  Liu, Chin ,  Anderson, Dennis K. ,  Lawson, Jon P. ,  Wieczorek, Joseph ,  Kunda, Sastry A. ,  Letendre, Leo J. ,  Pozzo, Marc J. ,  Sing, Yuen-Lung L. ,  Wang, Ping T. ,  Yonan, Edward E. ,  Weier, Richard M. ,  Kowar, Thomas R. ,  Baez, Julio A. ,  Erb, Bernhard

    IPC分类号： C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J71/00 ,  C12P33/00 ,  C07D301/12 ,  C07J31/00 ,  C07J53/00 ,  C12P33/10

    CPC分类号： C07J53/002 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J71/0005 ,  C07J71/0015 ,  C12P33/005 ,  C12P33/10

    摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I
    wherein:

    -A-A- represents the group -CHR 4 -CHR 5 - or -CR 4 =CR 5 - R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, varyloxy;
    R 1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;
    -B-B- represents the group -CHR 6 -CHR 7 - or an alpha- or beta- oriented group:
    where R 6 and R 7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and
    R 8 and R 9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R 8 and R 9 together comprise a carbocyclic or heterocyclic ring structure, or R 8 or R 9 together with R 6 or R 7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

    摘要翻译： 多个新的反应方案中，新颖的工艺步骤和新的中间体提供了用于epoxymexrenone和其它式化合物的合成I worin：-AA- darstellt组-CHR <4> -CHR <5> - 或-CR < 4> = CR <5> - R的<3>，R <4>和R <5>是unabhängig选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基， varyloxy; [R <1>α-取向低级烷氧基羰或羟烷基的三个代表; -BB- darstellt组-CHR <6> -CHR <7> - 或α-或β-取向的基团：氢其中R <6>和R <7>unabhängig选自的选择 卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基; 且R <8>和R <9>是unabhängig选自氢，羟基，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基中选择的，或R <8> 且R <9>一起构成碳环或杂环结构，或者R <8>或R <9>，其中R <6>或R一起<7>包括融合到五环D形环的碳环或杂环结构。

    Process for preparation of 7 alpha-carboxyl 9,11-epoxy steroids and Intermediates useful therein
    9.
    发明公开
    Process for preparation of 7 alpha-carboxyl 9,11-epoxy steroids and Intermediates useful therein 失效
    一种用于在生产7-α-羧基9,11-环氧甾体和有用的中间体过程

    公开(公告)号：EP1167381A2

    公开(公告)日：2002-01-02

    申请号：EP01122429.2

    申请日：1996-12-11

    申请人： G.D. Searle & Co.

    发明人： NG, John S. ,  Wang, Ping T. ,  Baez, Julio A. ,  Liu, Chin ,  Anderson, Dennis K. ,  Lawson, Jon P. ,  Erb, Dernhard ,  Wieczorek, Joseph ,  Mucciariello, Gennaro ,  Vanzanella, Fortunato ,  Kunda, Sastry A. ,  Letendre, Leo J. ,  Pozzo, Mark J. ,  Sing, Yuen-Lung L. ,  Yonan, Edward E.

    IPC分类号： C07J21/00 ,  C07J31/00 ,  C07J53/00 ,  C07J71/00 ,  C12P33/00 ,  C12P33/10 ,  C12Q1/02

    CPC分类号： C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J53/002 ,  C07J71/0015

    摘要： Compounds of Formula V:
    wherein

    -A-A- represents the group -CHR 4 -CHR 5 - or -CR 4 =CR 5 -,
    R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy,
    R 1 represents an alpha-oriented lower alkoxycarbonyl or hydroxycarbonyl radical,
    -B-B- represents the group -CHR 6 -CHR 7 - or an alpha- or beta- oriented group:

    where R 6 and R 7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and
    R 8 and R 9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R 8 and R 9 together comprise a carbocyclic or heterocyclic ring structure, or R 8 or R 9 together with R 6 or R 7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring,
    their intermediates and processes for preparing them.

    摘要翻译： 多个新的反应方案中，提供了用于epoxymexrenone和式（I），worin的其它化合物的合成新方法，步骤和中间物：-AA- darstellt组-CHR <4> -CHR <5 > - 或CR <4> -CR <5> - ; [R <3>，R <4>和Runabhängig选自氢中选择的<5>，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳基氧基; [R <1> darstelltα-取向低级烷氧基羰或羟烷基的，-BB- darstellt组-CHR <6> -CHR <7> - 或（III）成α-或β-式，其中R <面向组 6>和R <7>是unabhängig选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳基氧基，和R <8>和R <9>的选择 被选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳基氧基，或R <8>和R <9>一起构成的一个碳环或杂环unabhängig选择 结构，或R <8>或R <9>，其中R一起<6>或R <7>包括融合到五环D形环的碳环或杂环结构。