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1. 发明申请

WO2006032885A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2006032885A2
公开(公告)日：2006-03-30
申请号：PCT/GB2005/003641
申请日：2005-09-21
申请人： STERIX LIMITED , LEESE, Mathew , PUROHIT, Alan , REED, Michael, John , JOURDAN, Fabrice , POTTER, Barry, Victor, Lloyd , BURBERT, Christian
发明人： LEESE, Mathew , PUROHIT, Alan , REED, Michael, John , JOURDAN, Fabrice , POTTER, Barry, Victor, Lloyd , BURBERT, Christian
IPC分类号： C07J41/00 , C07J43/00 , C07J31/00 , C07J3/00 , C07J7/00 , A61K31/565 , A61K31/566 , A61K31/57 , A61K31/58 , A61P5/32
CPC分类号： C07J43/003 , C07J3/00 , C07J7/0005 , C07J31/006 , C07J41/0005 , C07J41/0072
摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R 1 selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R 4 which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R 2 of the formula -L-R 3 , wherein L is an optional linker group and R 3 is selected from groups which are or which comprise one of (i) -S0 2 R 5 , wherein R 5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO 2 ; (iii) -SOR 6 , wherein R 6 is H or a hydrocarbyl group; (iv) -R 7 , wherein R 7 is a halogen; (v) - alkyl; (vi) -C(=O)R 8 , wherein R 8 is H or hydrocarbyl; (vii) -C≡CR 9 , wherein R 9 is H or hydrocarbyl; (viii) -OC(=O)NR 10 R 11 wherein R 10 and R 11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R 3 is -alkyl, R 4 is present as a hydrocarbon group, when R 3 is -NO 2 R 4 is present and/or R 1 is present as a sulphamate group, and when R 3 is -C(=O)R 8 R 4 is present and R 1 is present as a sulphamate group.
摘要翻译：本发明提供了包含选自-OH，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺中的任何一种的甾体环系和任选的基团R 1的化合物组; 其中所述甾族环系统的A环任选在位置2或4处被基团R 4取代，所述基团R 4可以是合适的取代基，其中所述甾族环系统的D环被基团R 其中L是任选的连接基团，R 3选自以下基团：其中R 1，R 2，R 3，（i）-S 0 2 R 5，其中R 5是H，连接到D环的烃基或键或基团; （ii）-NO 2 2; （iii）-SOR 6，其中R 6是H或烃基; （iv）-R 7，其中R 7为卤素; （ⅴ） - 烷基; （vi）-C（= O）R 8，其中R 8为H或烃基; （vii）-C = CR 9，其中R 9是H或烃基; （viii）-OC（= O）NR 10 R 11，其中R 10和R 11独立地选自由H和烃基组成; （ix），（x），（xi），（xii）和（xiii）是其中当R 3为 - 烷基时，R 4为烃，当R 3为-NO 2 R 4存在时，和/或R 1存在作为并且当R 3为-C（= O）时，存在R 8 R 4和R 4，并且R 1〜 >以氨基磺酸盐基团存在。

2. 发明申请

WO2006032885A3 2-SUBSTITUTED ESTROGEN SULPHAMATES FOR INHIBITION OF STEROID SULPHATASE 审中-公开
标题翻译： 2-取代的雌激素用于抑制甾体硫酸酯酶
公开(公告)号：WO2006032885A3
公开(公告)日：2006-08-24
申请号：PCT/GB2005003641
申请日：2005-09-21
申请人： STERIX LTD , LEESE MATHEW , PUROHIT ALAN , REED MICHAEL JOHN , JOURDAN FABRICE , POTTER BARRY VICTOR LLOYD , BURBERT CHRISTIAN
发明人： LEESE MATHEW , PUROHIT ALAN , REED MICHAEL JOHN , JOURDAN FABRICE , POTTER BARRY VICTOR LLOYD , BURBERT CHRISTIAN
IPC分类号： C07J41/00 , A61K31/565 , A61K31/566 , A61K31/57 , A61K31/58 , A61P5/32 , C07J3/00 , C07J7/00 , C07J31/00 , C07J43/00
CPC分类号： C07J43/003 , C07J3/00 , C07J7/0005 , C07J31/006 , C07J41/0005 , C07J41/0072
摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R 1 selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R 4 which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R 2 of the formula -L-R 3 , wherein L is an optional linker group and R 3 is selected from groups which are or which comprise one of (i) -S0 2 R 5 , wherein R 5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO 2 ; (iii) -SOR 6 , wherein R 6 is H or a hydrocarbyl group; (iv) -R 7 , wherein R 7 is a halogen; (v) - alkyl; (vi) -C(=O)R 8 , wherein R 8 is H or hydrocarbyl; (vii) -C=CR 9 , wherein R 9 is H or hydrocarbyl; (viii) -OC(=O)NR 10 R 11 wherein R 10 and R 11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R 3 is -alkyl, R 4 is present as a hydrocarbon group, when R 3 is -NO 2 R 4 is present and/or R 1 is present as a sulphamate group, and when R 3 is -C(=O)R 8 R 4 is present and R 1 is present as a sulphamate group.
摘要翻译：本发明提供了包含选自-OH，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺中的任何一种的甾体环系和任选的基团R 1的化合物组; 其中所述甾族环系统的A环任选在位置2或4处被基团R 4取代，所述基团R 4可以是合适的取代基，其中所述甾族环系统的D环被基团R 其中L是任选的连接基团，R 3选自以下基团：其中R 1，R 2，R 3，（i）-S 0 2 R 5，其中R 5是H，连接到D环的烃基或键或基团; （ii）-NO 2 2; （iii）-SOR 6，其中R 6是H或烃基; （iv）-R 7，其中R 7为卤素; （ⅴ） - 烷基; （vi）-C（= O）R 8，其中R 8为H或烃基; （vii）-C = CR 9，其中R 9是H或烃基; （viii）-OC（= O）NR 10 R 11，其中R 10和R 11独立地选自由H和烃基组成; （ix），（x），（xi），（xii）和（xiii）是其中当R 3为 - 烷基时，R 4为烃，当R 3为-NO 2 R 4存在时，和/或R 1存在作为并且当R 3为-C（= O）时，存在R 8 R 4和R 4，并且R 1〜 >作为氨基磺酸盐基团存在。

3. 发明申请

WO2004085459A1 OESTROGEN DERIVATIVES AS INHIBITORS OF STEROID SULPHATASE 审中-公开
标题翻译：雌激素衍生物作为甾体硫酸酯的抑制剂
公开(公告)号：WO2004085459A1
公开(公告)日：2004-10-07
申请号：PCT/GB2004/000705
申请日：2004-02-20
申请人： STERIX LIMITED , LEESE, Mathew , PUROHIT, Alan , REED, Michael, John , NEWMAN, Simon, Paul , CHANDER, Surinder, Kumar , JOURDAN, Fabrice , POTTER, Barry, Victor, Lloyd
发明人： LEESE, Mathew , PUROHIT, Alan , REED, Michael, John , NEWMAN, Simon, Paul , CHANDER, Surinder, Kumar , JOURDAN, Fabrice , POTTER, Barry, Victor, Lloyd
IPC分类号： C07J41/00
CPC分类号： C07J43/00 , C07J41/00
摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R 1 selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R 2 of the formula -L-R 3 , wherein L is an optional linker group and R 3 is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R 3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R 4 , wherein R 4 is a hydrocarbyl group.
摘要翻译：本发明提供了包含甾族环系和选自-OH，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺基中的任何一个的任选基团R 1的化合物; 其中甾族环体系的D环被式-LR 3的基团R 2取代，其中L是任选的连接基团，R 3选自以下基团：亚硝酸酯基，醇，酯，醚，胺和烯烃，条件是当R 3是或包含醇时，存在L; 并且其中所述甾族环系统的A环在位置2或4被基团R 4取代，其中R 4是烃基。

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