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    • 4. 发明授权
    • Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
    • 雌激素-17-磺酰胺酸盐作为类固醇硫酸酯酶的抑制剂
    • US08030296B2
    • 2011-10-04
    • US11368367
    • 2006-03-03
    • Barry Victor Lloyd PotterMichael John ReedLok Wai Lawrence WooHatem HejazBertrand LeblondMatthew Paul LeeseAtul Purohit
    • Barry Victor Lloyd PotterMichael John ReedLok Wai Lawrence WooHatem HejazBertrand LeblondMatthew Paul LeeseAtul Purohit
    • A61K31/56C07J1/00
    • A61K31/565A61K31/37
    • 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.
    • 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。
    • 8. 发明授权
    • Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
    • 雌激素-17-磺酰胺酸盐作为类固醇硫酸酯酶的抑制剂
    • US07119081B2
    • 2006-10-10
    • US10367114
    • 2003-02-14
    • Barry Victor Lloyd PotterMichael John ReedBertrand LeblondMatthew Paul LeeseAtul Purohit
    • Barry Victor Lloyd PotterMichael John ReedBertrand LeblondMatthew Paul LeeseAtul Purohit
    • A01N1/00A61K31/56C07J1/00
    • A61K31/565A61K31/37
    • 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.
    • 提供式I的化合物,其中X是环系; R 1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; 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; 其中当X是甾体结构且R 1和R 2两者都是氨基磺酸酯基团时,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。