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    Compound
    8.
    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。

    1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors
    9.
    发明授权
    1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors 有权
    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

    公开(公告)号：US08022224B2

    公开(公告)日：2011-09-20

    申请号：US12139237

    申请日：2008-06-13

    申请人： Lok Wai Lawrence Woo ,  Toby Jackson ,  Atul Purohit ,  Michael John Reed ,  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： 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. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.

    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。 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。

    COMPOUND
    10.
    发明申请
    COMPOUND 有权
    复合

    公开(公告)号：US20100173963A1

    公开(公告)日：2010-07-08

    申请号：US12555342

    申请日：2009-09-08

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

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

    IPC分类号： A61K31/4196 ,  C07D249/08 ,  C07D405/10

    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。