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    Oestrogen derivatives as inhibitors of steroid sulphatase
    3.
    发明授权
    Oestrogen derivatives as inhibitors of steroid sulphatase 失效
    雌激素衍生物作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US07893284B2

    公开(公告)日：2011-02-22

    申请号：US11233945

    申请日：2005-09-23

    申请人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    发明人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    IPC分类号： C07J3/00 ,  C07J1/00

    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 R1 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 R2 of the formula -L-R3, wherein L is an optional linker group and R3 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 R3 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 R4, wherein R4 is a hydrocarbyl group.

    摘要翻译： 本发明提供了包含甾族环系统和选自-OH，氨基磺酸盐基团，膦酸盐基团，硫代膦酸盐基团，磺酸盐基团或磺酰胺基团中的任何一个的任选基团R1的化合物; 其中甾族环体系的D环被式-L-R3的基团R 2取代，其中L是任选的连接基团，并且R 3选自亚硝酸根基团，醇， 酯，醚，胺和烯烃，条件是当R3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与基团R 4取代，其中R 4是烃基。

    Compound
    4.
    发明授权
    Compound 有权
    复合

    公开(公告)号：US08093279B2

    公开(公告)日：2012-01-10

    申请号：US12555342

    申请日：2009-09-08

    申请人： Lok Wai Lawrence Woo ,  Toby Jackson ,  Atul Purohit ,  Michael John Reed ,  Gillian Reed, legal representative ,  Barry Victor Lloyd Potter

    发明人： Lok Wai Lawrence Woo ,  Toby Jackson ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/44 ,  C07D249/00

    CPC分类号： C07D249/08 ,  C07D405/10

    摘要： There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and —Y—R8; wherein each R8 is independently selected from —OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2), H-bond acceptors, and halogens; wherein at least one of R3, R4, R5, R6 and R7 is —Y—R8 wherein R8 is selected from substituted and unsubstituted heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further substituted; wherein R9 is selected from H, —OH and —OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is —Y—R8; OR (b) R9 is —OSO2NR1R2 or —OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is —Y—R8.

    摘要翻译： 提供式I的化合物，其中R 3，R 4，R 5，R 6和R 7独立地选自H和-Y-R 8; 其中每个R 8独立地选自-OH，烃基，羟基烃基，氰基（-CN），硝基（-NO 2），H-键受体和卤素; 其中R 3，R 4，R 5，R 6和R 7中的至少一个是-Y-R 8，其中R 8选自取代和未取代的杂环和氨基取代的苯基，其中X是键或连接基团; 其中Y是任选的连接基团; 并且其中环A任选进一步被取代; 其中R9选自H，-OH和-OSO2NR1R2; 其中R1和R2独立地选自H和烃基; 其中（a）X是键，并且R 3，R 4，R 5，R 6和R 7中的至少一个是-Y-R 8; 或（b）R9为-OSO2NR1R2或-OH，R3，R4，R5，R6和R7中的4个为H，R3，R4，R5，R6和R7之一为-Y-R8。

    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
    8.
    发明授权
    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase 有权
    雌激素-17-磺酰胺酸盐作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US08030296B2

    公开(公告)日：2011-10-04

    申请号：US11368367

    申请日：2006-03-03

    申请人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo ,  Hatem Hejaz ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    发明人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo ,  Hatem Hejaz ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： A61K31/565 ,  A61K31/37

    摘要： There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth. There is also provided a compound of Formula VIII wherein R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

    摘要翻译： 提供式I的化合物，其中X是环系; R1是氨基磺酸酯基，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; R2是氨基磺酸酯基，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; 其中当X是甾体结构且R 1和R 2均为氨基磺酸酯基团时，甾体环体系（X）代表雌激素; 并且其中所述化合物能够抑制类固醇硫酸酯酶（STS）活性和/或能够充当细胞循环的调节剂和/或作为凋亡调节剂和/或细胞生长调节剂。 还提供了式VIII的化合物，其中R 2是氨基磺酸酯基，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; 并且其中所述化合物能够抑制类固醇硫酸酯酶（STS）活性和/或能够充当细胞循环的调节剂和/或作为凋亡调节剂和/或细胞生长调节剂。