利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

65 条记录 (耗时 0.06 秒)

    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
    12.
    发明授权
    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase 有权
    雌激素-17-磺酰胺酸盐作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US08030296B2

    公开(公告)日：2011-10-04

    申请号：US11368367

    申请日：2006-03-03

    申请人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo ,  Hatem Hejaz ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    发明人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo ,  Hatem Hejaz ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： A61K31/565 ,  A61K31/37

    摘要： 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.

    摘要翻译： 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。

    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
    15.
    发明授权
    Oestrogen-17-sulphamates as inhibitors of steroid sulphatase 有权
    雌激素-17-磺酰胺酸盐作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US07119081B2

    公开(公告)日：2006-10-10

    申请号：US10367114

    申请日：2003-02-14

    申请人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    发明人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Bertrand Leblond ,  Matthew Paul Leese ,  Atul Purohit

    IPC分类号： A01N1/00 ,  A61K31/56 ,  C07J1/00

    CPC分类号： A61K31/565 ,  A61K31/37

    摘要： 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.

    摘要翻译： 提供式I的化合物，其中X是环系; R 1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; 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; 其中当X是甾体结构且R 1和R 2两者都是氨基磺酸酯基团时，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。

    Compound
    18.
    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 。

    Compound
    19.
    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。