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    1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors
    4.
    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
    7.
    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。

    Compound
    8.
    发明申请
    Compound 审中-公开
    复合

    公开(公告)号：US20100120789A1

    公开(公告)日：2010-05-13

    申请号：US12554943

    申请日：2009-09-07

    申请人： Nigel Vicker ,  Xiangdong Su ,  Fabienne Praduax ,  Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Xiangdong Su ,  Fabienne Praduax ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/497 ,  C07C233/00 ,  A61K31/165 ,  A61K31/4365 ,  C07D495/04 ,  C07D405/02 ,  C12Q1/32

    CPC分类号： C11D3/0073 ,  C11D3/2086 ,  C11D3/33 ,  C11D7/265 ,  C11D7/3245 ,  C11D11/0041

    摘要： There is provided a compound having Formula I R1—Z—R2   Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S═O, and S(═O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(═O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R3, R4, R5, R6, R8, R9, R11, R12, R13, R14, R15 and R16, are independently selected from H, hydrocarbyl and halogen, wherein each of R7 and R10 are independently selected from H and hydrocarbyl.

    摘要翻译： 提供了具有式I的化合物R1-Z-R2式Ⅰ其中R1是选自任选取代的稠合多环基团，取代的烷基，支链烷基和任选取代的环烷基的基团Z是一种或多种 羰基或羰基的等排基团选自任选取代的芳环和任选取代的杂环，其中（a）R 2是2-取代的噻吩基团，和/或（b）Z是式-C （= O）-CR 3 R 4 -X-（CR 5 R 6）n - ，其中X选自NR 7，S，O，S = O和S（= O）2，其中n为0或1和/或（c） R1是金刚烷基，Z是或包含酰胺基，和/或（d）R1是金刚烷基，Z是或包含式 - （CR8R9）对NR10-S（= O）2- （CR11R12）q-，其中p为0或1，q为0或1，和/或（e）R1为金刚烷基，Z为或包含式 - （CR13R14）vY-（CR15R16）w- 在哪里 Y是杂芳基环中的键是羰基的等离子体的杂芳基，其中v是0或1，w是0或1; 其中R 3，R 4，R 5，R 6，R 8，R 9，R 11，R 12，R 13，R 14，R 15和R 16各自独立地选自H，烃基和卤素，其中R 7和R 10各自独立地选自H和烃基 。

    1,2,4-TRIAZOL-1-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMORS
    9.
    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。