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    • 1. 发明申请
    • 2-SUBSTITUTED ESTROGEN SULPHAMATES FOR INHIBITION OF STEROID SULPHATASE
    • 2-取代的雌激素用于抑制甾体硫酸酯酶
    • WO2006032885A3
    • 2006-08-24
    • PCT/GB2005003641
    • 2005-09-21
    • STERIX LTDLEESE MATHEWPUROHIT ALANREED MICHAEL JOHNJOURDAN FABRICEPOTTER BARRY VICTOR LLOYDBURBERT CHRISTIAN
    • LEESE MATHEWPUROHIT ALANREED MICHAEL JOHNJOURDAN FABRICEPOTTER BARRY VICTOR LLOYDBURBERT CHRISTIAN
    • C07J41/00A61K31/565A61K31/566A61K31/57A61K31/58A61P5/32C07J3/00C07J7/00C07J31/00C07J43/00
    • C07J43/003C07J3/00C07J7/0005C07J31/006C07J41/0005C07J41/0072
    • 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.
    • 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。