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    • 5. 发明授权
      US08093279B2 Compound 有权
    • Compound
    • 复合
    • US08093279B2
    • 2012-01-10
    • US12555342
    • 2009-09-08
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Gillian Reed, legal representative , Barry Victor Lloyd Potter
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
    • A61K31/44 , C07D249/00
    • C07D249/08 , C07D405/10
    • 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。
    • 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
    • 6. 发明授权
      US08022224B2 1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors 有权
    • 1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors
    • 1,2,4-三唑-1-基双苯基衍生物，用于治疗内分泌依赖性肿瘤
    • US08022224B2
    • 2011-09-20
    • US12139237
    • 2008-06-13
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
    • C07D249/00
    • C07D249/08 , C07D405/10
    • 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. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.
    • 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。 这些化合物抑制类固醇硫酸酯酶和芳香酶活性，并且可用于治疗内分泌依赖性肿瘤。
    • 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
    • 7. 发明申请
      US20100173963A1 COMPOUND 有权
    • COMPOUND
    • 复合
    • US20100173963A1
    • 2010-07-08
    • US12555342
    • 2009-09-08
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter , Gillin Reed
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter , Gillin Reed
    • A61K31/4196 , C07D249/08 , C07D405/10
    • C07D249/08 , C07D405/10
    • 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。
    • 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
    • 8. 发明申请
      US20080319037A1 1,2,4-TRIAZOL-1-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMORS 有权
    • 1,2,4-TRIAZOL-1-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMORS
    • 1,2,4-三唑-1-基联苯衍生物用于治疗依靠内皮素的肿瘤
    • US20080319037A1
    • 2008-12-25
    • US12139237
    • 2008-06-13
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
    • Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
    • A61K31/4196 , C07D249/08 , A61P35/00
    • C07D249/08 , C07D405/10
    • 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. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.
    • 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中的四个为H，R3，R4，R5，R6和R7之一为-Y-R8。 这些化合物抑制类固醇硫酸酯酶和芳香酶活性，并且可用于治疗内分泌依赖性肿瘤。
    • 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
    • 9. 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
    • 10. 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
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