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    • 6. 发明授权
    • Compound
    • 复合
    • US08093279B2
    • 2012-01-10
    • US12555342
    • 2009-09-08
    • Lok Wai Lawrence WooToby JacksonAtul PurohitMichael John ReedGillian Reed, legal representativeBarry Victor Lloyd Potter
    • Lok Wai Lawrence WooToby JacksonAtul PurohitMichael John ReedBarry Victor Lloyd Potter
    • A61K31/44C07D249/00
    • C07D249/08C07D405/10
    • 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.
    • 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。
    • 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
    • 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。