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    Compound
    2.
    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。

    Oestrogen derivatives as inhibitors of steroid sulphatase
    4.
    发明授权
    Oestrogen derivatives as inhibitors of steroid sulphatase 失效
    雌激素衍生物作为类固醇硫酸酯酶的抑制剂

    公开(公告)号：US07893284B2

    公开(公告)日：2011-02-22

    申请号：US11233945

    申请日：2005-09-23

    申请人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    发明人： Matthew Leese ,  Atul Purohit ,  Michael John Reed ,  Simon Paul Newman ,  Surinder Kuman Chander ,  Fabrice Jourdan ,  Barry Victor Lloyd Potter

    IPC分类号： C07J3/00 ,  C07J1/00

    CPC分类号： C07J43/00 ,  C07J41/00

    摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.

    摘要翻译： 本发明提供了包含甾族环系统和选自-OH，氨基磺酸盐基团，膦酸盐基团，硫代膦酸盐基团，磺酸盐基团或磺酰胺基团中的任何一个的任选基团R1的化合物; 其中甾族环体系的D环被式-L-R3的基团R 2取代，其中L是任选的连接基团，并且R 3选自亚硝酸根基团，醇， 酯，醚，胺和烯烃，条件是当R3是或包含醇时，存在L; 并且其中所述甾族环系统的A环在位置2或4与基团R 4取代，其中R 4是烃基。

    Steroid sulphatase inhibitors
    8.
    发明授权
    Steroid sulphatase inhibitors 失效
    类固醇硫酸酶抑制剂

    公开(公告)号：US06677325B2

    公开(公告)日：2004-01-13

    申请号：US10082007

    申请日：2002-02-21

    申请人： Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K3135

    CPC分类号： A61K31/37 ,  C07D311/16 ,  C07D311/30 ,  C07D311/32 ,  C07D311/36 ,  C07J41/0072

    摘要： A method for controlling estrone or estrodiol production comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M. A method to target the estrogen metabolic pathway comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M.

    摘要翻译： 用于控制雌酮或雌二醇生产的方法，包括施用包含氨基磺酸酯基团的环系化合物; 其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（EC 3.1.6.2）; 并且其中如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC 3.1.6.2）温育，则其提供Km值 小于50亩。 靶向雌激素代谢途径的方法，包括施用包含氨基磺酸酯基团的环系化合物; 其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（EC 3.1.6.2）; 并且其中如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC 3.1.6.2）温育，则其提供Km值 小于50亩。

    Oxime-group containing oestrone sulphatase inhibitors
    9.
    发明授权
    Oxime-group containing oestrone sulphatase inhibitors 失效
    含肟基的磺胺类化合物抑制剂

    公开(公告)号：US06670353B2

    公开(公告)日：2003-12-30

    申请号：US09572237

    申请日：2000-05-17

    申请人： Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K3156

    CPC分类号： A61K31/565

    摘要： A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one oxime group is attached to or is part of at least one of the ring components.

    摘要翻译： 描述了适合用作奥斯汀硫酸酯酶抑制剂（E.C.3.1.6.2）的氨基磺酸盐化合物。 化合物是包含至少两个环组分的多环化合物，其中多环化合物包含至少一个连接至至少一个环组分的氨基磺酸酯基团，并且其中至少一个肟基团连接至至少一个 的环组件。

    Methods for introducing an estrogenic compound
    10.
    发明授权
    Methods for introducing an estrogenic compound 失效
    引入雌激素化合物的方法

    公开(公告)号：US06476011B1

    公开(公告)日：2002-11-05

    申请号：US09193970

    申请日：1998-11-18

    申请人： Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K3156

    CPC分类号： A61K31/37 ,  C07D311/16 ,  C07D311/30 ,  C07D311/32 ,  C07D311/36 ,  C07J41/0072

    摘要： The invention pertains to methods for introducing an estrogenic compound into a subject in need thereof involving administering an effective amount of a ring system compound having the formula (II) wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, and at least one of R1 and R2 is H, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and the ring system ABCD represents a substituted or unsubstituted, saturated or unsaturated steroid nucleus selected from the group consisting of oestrones, dehydroepiandrosterones, substituted oestrones, oestradiols, substituted oestradiols, oestriols, substituted dehydroepiandrosterones, or substituted oestriols; wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3,1,6,2), or a pharmceutically acceptable salt thereof.

    摘要翻译： 本发明涉及向有需要的受试者中引入雌激素化合物的方法，包括给予有效量的具有式（II）的环系化合物，其中R 1和R 2各自独立地选自H，烷基，烯基，环烷基和 芳基，并且R 1和R 2中的至少一个为H，或一起表示亚烷基链中任选含有一个或多个杂原子或基团的亚烷基; 环系ABCD代表选自以下组中的取代或未取代的饱和或不饱和类固醇核：地塞米松，脱氢表雄酮，取代的雌二醇，雌二醇，取代的雌二醇，雌三醇，取代的脱氢表雄甾酮或取代的雌三醇; 其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（EC 3,1,6,2）或其药学上可接受的盐。