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    1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors
    23.
    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
    26.
    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。

    1,2,4-TRIAZOL-1-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMORS
    27.
    发明申请
    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-基联苯衍生物用于治疗依靠内皮素的肿瘤

    公开(公告)号：US20080319037A1

    公开(公告)日：2008-12-25

    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： A61K31/4196 ,  C07D249/08 ,  A61P35/00

    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。

    11β-hydroxysteroid dehydrogenase inhibitors
    28.
    发明授权
    11β-hydroxysteroid dehydrogenase inhibitors 失效
    11beta-羟类固醇脱氢酶抑制剂

    公开(公告)号：US07230020B2

    公开(公告)日：2007-06-12

    申请号：US10970064

    申请日：2004-10-22

    申请人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/423 ,  A61K31/426 ,  C07D263/56 ,  C07D277/64

    CPC分类号： C07D209/48 ,  C07D211/28 ,  C07D213/76 ,  C07D215/38 ,  C07D231/56 ,  C07D241/42 ,  C07D261/16 ,  C07D261/20 ,  C07D275/04 ,  C07D277/64 ,  C07D295/135 ,  C07D307/79 ,  C07D311/18 ,  C07D319/18 ,  C07D333/54 ,  C07D333/70 ,  C07D495/04

    摘要： A compound having Formula I R1—Z—R2Formula I wherein R1 is an optionally substituted phenyl ring; R2 is or comprises an optionally substituted aromatic ring; and Z is —X—Y—L— or —Y—X—L— wherein either X is selected from —S(═O)(═O)— and —C(═O)—; and Y is —NR3—; or X is selected from —S(═O)(═O)— and —S—, and Y is —C(R4)(R5)—; L is an optional linker; and R3, R4 and R5 are each independently selected from H and hydrocarbyl; and wherein when R2 comprises the following structural moiety wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1—C(═O)—NR3—L—R2; R1—S(═O)(═O)—C(R4)(R5)—L—R2; R1—S—C(R4)(R5)—L—R2; R1—NR3—S(═O)(═O)—L—R2; R1—NR3—C(═O)—L—R2; R1—C(R4)(R5)—S(═O)(═O)—L—R2; and R1—C(R4)(R5)—S—L—R2.

    摘要翻译： 具有式I的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -ZR 2式I < in-line-formula description =“In-line formula”end =“tail”？>其中R 1是任选取代的苯环; R 2是或包含任选取代的芳环; Z是-X-Y-L-或-Y-X-L-，其中X选自-S（-O）（ - O） - 和-C（-O） - ; 和Y是-NR 3 - ; 或者X选自-S（-O）（ - O） - 和-S-，Y是-C（R 4a）（R 5） - ; L是可选的接头; 和R 3，R 4和R 5各自独立地选自H和烃基; 并且其中当R 2包含以下结构部分时，其中Q是选自S，O，N和C的原子; 该化合物选自式R 1 -C（-O）-NR 3 -L-R 2的化合物; R 1 -S（-O）（ - O）-C（R 4）（R 5） - R L 2 / SUB>; R 1 -S-C（R 4）（R 5） - L-R 2; R 1 -SO 2 -S（-O）（ - O）-L-R 2; R 1 -NR 3 -C（-O）-L-R 2; R 1 -C（R 4）（R 5）-S（-O）（ - O）-LR 2， / SUB>; 和R 1 -C（R 4）（R 5）-S-L-R 2。