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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.
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。 -
2.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.
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。 -
3.发明公开11.alpha.-hydroxy-steroid-4,6-dien-3-one compounds and a process for their preparation 失效11.alpha.羟基类固醇孕甾-4,6-二烯-3-酮化合物和它们的制备方法
公开(公告)号：EP1167380A3
公开(公告)日：2004-12-08
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.
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 -CHR4-CHR5- or -CR4=CR5-, R3, R4 and R5 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 -CHR6-CHR7- or an alpha- or beta- oriented group: where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 and R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring, their intermediates and processes for preparing them.
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4.发明公开Intermediates useful in the preparation of 9,11-epoxy steroids and methods for their production 失效中间体9,11-Epoxysteroiden的准备和其制备方法
公开(公告)号：EP1170299A3
公开(公告)日：2004-11-10
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.
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 -CHR4-CHR5- or -CR4=CR5- R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxy carbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxycarbonyl radical, -B-B- represents the group -CHR6-CHR7- or an alpha- or beta- oriented group: where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryioxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring, and R2 is lower alkylsulfonyloxy or acyloxy or a halide and process for preparing them.
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5.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：EP1167381A3
公开(公告)日：2004-09-29
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.
CPC分类号： C07J21/00 , C07J21/003 , C07J31/006 , C07J53/002 , C07J71/0015
摘要： Multiple novel reaction schemes, novel process steps and 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, aryloxy; 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 of formula (III), 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.
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6.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.
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。
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