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1. 发明申请

US20060142360A1 Compound 失效
公开(公告)号：US20060142360A1
公开(公告)日：2006-06-29
申请号：US11209186
申请日：2005-08-22
申请人： Barry Lloyd Potter , Lok Wai Woo , Atul Purohit , Michael Reed , Oliver Sutcliffe , Christian Bubert
发明人： Barry Lloyd Potter , Lok Wai Woo , Atul Purohit , Michael Reed , Oliver Sutcliffe , Christian Bubert
IPC分类号： A61K31/4196 , C07D249/14 , C07D249/08
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D413/12 , C07D417/12
摘要： There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C═O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

2. 发明申请

US20060281719A1 Oestrogen-17-sulphamates as inhibitors of steroid sulphatase 有权
公开(公告)号：US20060281719A1
公开(公告)日：2006-12-14
申请号：US11368367
申请日：2006-03-03
申请人： Barry Lloyd Potter , Michael Reed , Lok Woo , Hatem Hejaz , Bertrand Leblond , Matthew Leese , Atul Purohit
发明人： Barry Lloyd Potter , Michael Reed , Lok Woo , Hatem Hejaz , Bertrand Leblond , Matthew 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.

3. 发明申请

US20070021624A1 Steroid sulphatase inhibitors 审中-公开
标题翻译：类固醇硫酸酶抑制剂
公开(公告)号：US20070021624A1
公开(公告)日：2007-01-25
申请号：US11406079
申请日：2006-04-18
申请人： Michael Reed , Barry Lloyd Potter
发明人： Michael Reed , Barry Lloyd Potter
IPC分类号： C07J1/00
CPC分类号： C07J1/00 , A61K31/56
摘要： A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 μM.
摘要翻译：描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 该环系化合物包含连接下式的氨基磺酸酯基团的环，其中R 1和R 2各自独立地选自H，烷基，烯基，环烷基或芳基，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; 并且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（E.C.3.1.6.2）; 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团取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（EC3.1.6.2）一起孵育，则其将提供K 值小于50μM。

4. 发明申请

US20070173531A1 Compound 失效
标题翻译：复合
公开(公告)号：US20070173531A1
公开(公告)日：2007-07-26
申请号：US11710846
申请日：2007-02-26
申请人： Michael Reed , Barry Lloyd Potter
发明人： Michael Reed , Barry Lloyd Potter
IPC分类号： A61K31/4704 , A61K31/382 , A61K31/366 , C07D311/02
CPC分类号： C07D311/78 , A61K31/37 , C07D311/16
摘要： A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.
摘要翻译：描述化合物。特别地，描述了非甾体氨基磺酸盐化合物。该化合物适合用作奥斯汀硫酸酯酶的抑制剂。该化合物为通式（A），其中R 1至R 6独立地选自H，卤素，羟基，氨基磺酸酯，烷基和取代的变体或其盐; 但其中R 1 -R 6中的至少一个为氨基磺酸酯基; 并且其中X是S，NH，取代的N，CH 2或任何一个取代的C

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