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    • 8. 发明授权
      US08846737B2 Compound 有权
    • Compound
    • US08846737B2
    • 2014-09-30
    • US13392206
    • 2010-08-23
    • Lok Wai Lawrence Woo , Christian Bubert , Paul Michael Wood , Aurélien Putey , Atul Purohit , Barry Victor Lloyd Potter
    • Lok Wai Lawrence Woo , Christian Bubert , Paul Michael Wood , Aurélien Putey , Atul Purohit , Barry Victor Lloyd Potter
    • C07D249/08
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
    • There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C═O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (═O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C═O)0-1R12][(C═O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C═O)0-1R12][(C═O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R′14, wherein R12 and R13 are independently selected from H, linear or branched hydrocarbon groups having a carbon chain of from 1 to 10 carbon atoms, or together with the atoms to which they are attached, may form a mono or bicyclic ring having from 5 to 14 ring members wherein R14 is selected from: aliphatic ring systems unsubstituted or substituted monocyclic aliphatic heterocycles; unsubstituted or substituted heteroaryl radical, and unsubstituted or substituted phenyl group; the group of formula wherein t is 1 or 2 wherein R′14 is a unsubstituted or substituted phenyl group; wherein each of R7 to R11 is independently selected from —H, NO2, halo, —O—(C1-C6)haloalkyl, (C1-C6)haloalkyl, (C1-C6)alkyl, —CN, —OH, —OPh, —OBn, -Ph, —OSO2NR15R16, —SO2R26, —SO2NR27R28, —O—(C1-C6)alkyl, —(C═O)0-1NR29R30 and —CO(O)0-1R31; wherein R15 and R16 are independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl optionally contain one or more hetero atoms or groups wherein each of R26 to R31 is independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl optionally contain one or more hetero atoms or groups; or any pharmaceutically acceptable salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20120238550A1 COMPOUND 有权
    • COMPOUND
    • US20120238550A1
    • 2012-09-20
    • US13392206
    • 2010-08-23
    • Lok Wai Lawrence Woo , Christian Bubert , Paul Michael Wood , Aurélien Putey , Atul Purohit , Barry Victor Lloyd Potter
    • Lok Wai Lawrence Woo , Christian Bubert , Paul Michael Wood , Aurélien Putey , Atul Purohit , Barry Victor Lloyd Potter
    • A61K31/4196 , C07D409/12 , C07D403/12 , A61K31/55 , C07D401/12 , A61P35/00 , C07D413/12 , A61K31/5377 , A61K31/496 , A61K31/4439 , C07D405/12 , C07D249/08 , A61K31/454
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
    • There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C═O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (═O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C═O)0-1R12][(C═O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C═O)0-1R12][(C═O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R′14, wherein R12 and R13 are independently selected from H, linear or branched hydrocarbon groups having a carbon chain of from 1 to 10 carbon atoms, or together with the atoms to which they are attached, may form a mono or bicyclic ring having from 5 to 14 ring members wherein R14 is selected from: aliphatic ring systems unsubstituted or substituted monocyclic aliphatic heterocycles; unsubstituted or substituted heteroaryl radical, and unsubstituted or substituted phenyl group; the group of formula wherein t is 1 or 2 wherein R′14 is a unsubstituted or substituted phenyl group; wherein each of R7 to R11 is independently selected from —H, NO2, halo, —O—(C1-C6)haloalkyl, (C1-C6)haloalkyl, (C1-C6)alkyl, —CN, —OH, —OPh, —OBn, -Ph, —OSO2NR15R16, —SO2R26, —SO2NR27R28, —O—(C1-C6)alkyl, —(C═O)0-1NR29R30 and —CO(O)0-1R31; wherein R15 and R16 are independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl optionally contain one or more hetero atoms or groups wherein each of R26 to R31 is independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl optionally contain one or more hetero atoms or groups; or any pharmaceutically acceptable salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US08030296B2 Oestrogen-17-sulphamates as inhibitors of steroid sulphatase 有权
    • 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 Potter , Michael John Reed , Lok Wai Lawrence Woo , Hatem Hejaz , Bertrand Leblond , Matthew Paul Leese , Atul Purohit
    • Barry Victor Lloyd Potter , Michael John Reed , Lok Wai Lawrence Woo , Hatem Hejaz , Bertrand Leblond , Matthew Paul Leese , Atul Purohit
    • A61K31/56 , C07J1/00
    • A61K31/565 , A61K31/37
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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