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1. 发明公开

EP1502915A1 Compounds with a sulfamate group 失效
标题翻译： Verwendung von Verbindungen mit einerSulfonsaüreamid-Gruppe
公开(公告)号：EP1502915A1
公开(公告)日：2005-02-02
申请号：EP04025526.7
申请日：1997-03-04
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： C07D311/30 , C07D311/32 , C07D311/36 , A61K31/35 , A61P35/00 , C07D405/04
CPC分类号： C07D311/30 , C07D311/32 , C07D311/36 , C07D405/04
摘要： There is provided a sulphamate compound suitable for use as an inhibitor of both oestrone sulphatase activity and aromatase activity.
摘要翻译：提供了适合用作雌二醇硫酸酯酶活性和芳香酶活性抑制剂的氨基磺酸盐化合物。

2. 发明公开

EP2202240A1 Compound 审中-公开
标题翻译：雌激素-17-氨基磺酸ur ur on类固醇硫酸酯酶
公开(公告)号：EP2202240A1
公开(公告)日：2010-06-30
申请号：EP09002167.6
申请日：2001-08-17
申请人： Sterix Limited
发明人： Potter, Barry Victor Lloyd , Reed, Michael John , Purohit, Atul , Leese, Matthew Paul , Leblond, Bertrand
IPC分类号： C07J41/00 , A61K31/565 , A61P35/00 , A61P5/30 , A61P5/32
CPC分类号： A61K31/565 , A61K31/37
摘要： There is provided a compound of Formula I

wherein X is a ring system; R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R 2 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 R 1 and R 2 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 R 2 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是甾族结构且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/或能够作为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/或能够作为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。

3. 发明公开

EP1657247A1 Steroidal compounds for inhibiting steroid sulphotase 有权
标题翻译： Steroidale Verbindungen zur Hemmung von steroid Sulfotase
公开(公告)号：EP1657247A1
公开(公告)日：2006-05-17
申请号：EP06000817.4
申请日：2002-10-17
申请人： Sterix Limited
发明人： Potter, Barry Victor Lloyd , Reed, Michael John , Woo, Lok Wai Lawrence
IPC分类号： C07J63/00 , A61K31/56 , A61P35/00
CPC分类号： C07J1/0051 , C07J63/00 , C07J63/008
摘要： There is provided a compound having Formula I

wherein G is H or a substituent, and wherein R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.
摘要翻译：提供具有式I的化合物，其中G是H或取代基，并且其中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。

4. 发明公开

EP2336146A1 17beta-hydroxysteroid dehydrogenase inhibitors 审中-公开
标题翻译： 17β-羟类固醇脱氢酶抑制剂
公开(公告)号：EP2336146A1
公开(公告)日：2011-06-22
申请号：EP10011417.2
申请日：2004-03-22
申请人： Sterix Limited
发明人： Vicker, Nigel , Lawrence, Harshani Rithma , Allan, Gillian Margaret , Bubert, Christian , Fisher, Delphine Sophie , Purohit, Atul , Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： C07J71/00 , A61K31/56 , A61K31/566 , C07J41/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula I

wherein (I) R 1 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R 2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is - CH 2 - or -CH 2 CH 2 -, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO so that R 1 together with R 3 provide the enol tautomer

OR R 1 together with R 3 form (xii) a pyrazole wherein (a) R 4 is =N-O-alkyl or =N-O-H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from -OH and -O-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula

(II) R 2 is selected from groups capable of forming a hydrogen bond , a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III)R 3 is selected from -OH, =O, or a -C(=O)- mimetic
摘要翻译：提供式I的化合物，其中（I）R 1选自（i）烷氧基烷基（ii）腈基，其中R 2能够形成氢键（iii）烷基芳基，其中芳基被其它芳基取代的（C 1〜C 10）烯基芳基（ⅴ）烷基杂芳基取代，其中当杂芳基仅在环中仅包含C和N时，芳基被除（vi）烯基杂芳基，（vii）= NO-烷基或= NOH基（viii）支链烯基（ix）烷基醇基（x）酰胺或烷基酰胺，其中（a）烷基酰胺的烷基是-CH 2 - 或-CH 2 CH 2 - ，（b）酰胺是二取代的和/或（c）酰胺被烷基杂环基，烯基杂环基，烷基杂芳基，烯基杂芳基，杂芳基，烷基胺中的至少一个所取代基团，烷氧基烷基，烷基芳基，直链或支链烷基，（xi）-CHO，使得 R 1与R 3一起提供烯醇互变异构体OR R 1和R 3形式（xii）吡唑，其中（a）R 4是= NO-烷基或= NOH基，（b）吡唑被烷基 -OH基，烷基酯基，烷氧基烷基，支链烷基和酰胺和/或（c）2位被选自-OH和-O-烃基（xiii）杂芳基环的基团取代，以提供式（II）化合物R 2选自能够形成氢键，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基和磺酰胺基的基团; 和（III）R 3选自-OH，= O或-C（= O） - 模拟物

5. 发明授权

EP0928609B1 Pharmaceutical compositions containing sulphamate derivatives as steroid sulphatase inhibitors 失效
标题翻译：含有药物组合物的化合物作为Sulphamatderivate steroidsulfatasehemmende
公开(公告)号：EP0928609B1
公开(公告)日：2003-04-16
申请号：EP98204337.4
申请日：1992-08-28
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Llyod
IPC分类号： A61K31/565 , C07J41/00
CPC分类号： A61K31/565 , C07J41/0033 , C07J41/0072

6. 发明授权

EP0982032B1 Use of a sterol compound comprising a sulphamic acid ester group for the manufacture of medicaments for the control of oestrogen production 失效
标题翻译：用于药物的制造中使用含氨基磺酸，甾醇酯的雌激素生产的控制
公开(公告)号：EP0982032B1
公开(公告)日：2003-08-06
申请号：EP99203449.6
申请日：1992-08-28
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： C07J41/00 , A61K31/565 , A61P5/32
CPC分类号： A61K31/565 , C07J41/0033 , C07J41/0072

7. 发明授权

EP0921130B1 Steroid sulphatase inhibitors 失效
标题翻译：类固醇硫酸酯酶的抑制性化合物
公开(公告)号：EP0921130B1
公开(公告)日：2003-05-07
申请号：EP98204340.8
申请日：1992-08-28
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： C07J41/00 , A61K31/565 , A61P5/32
CPC分类号： A61K31/565 , C07J41/0033 , C07J41/0072

8. 发明公开

EP0921130A3 Steroid sulphatase inhibitors 失效
标题翻译：类固醇硫酸酯酶的抑制性化合物
公开(公告)号：EP0921130A3
公开(公告)日：2001-09-05
申请号：EP98204340.8
申请日：1992-08-28
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： C07J41/00 , A61K31/565 , A61P5/32
CPC分类号： A61K31/565 , C07J41/0033 , C07J41/0072
摘要： The present invention provides a compound of the formula wherein each of R 1 and R 2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl; and wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); wherein if the sulphamate group on the compound were to be 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 K m value of less than 50 µM; and wherein at least one of R 1 and R 2 is H.

9. 发明公开

EP0982032A2 Use of a ring system compound comprising a sulphamic acid ester group for the manufacture of medicaments for the control of oestrogen production 失效
标题翻译：用于制备药物的制造中的用途氨基磺酸盐含酯的环系化合物的雌激素生产的控制
公开(公告)号：EP0982032A2
公开(公告)日：2000-03-01
申请号：EP99203449.6
申请日：1992-08-28
申请人： Sterix Limited
发明人： Reed, Michael John , Potter, Barry Victor Lloyd
IPC分类号： A61K31/565
CPC分类号： A61K31/565 , C07J41/0033 , C07J41/0072
摘要： The present invention provides use of a ring system compound for the manufacture of a medicament to control oestrogen production, and/or use of a ring system compound for the manufacture of a medicament to target the oestrogen metabolic pathway, wherein ring system compound comprises 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 K m value of less than 50µm.

10. 发明授权

EP1657247B1 Steroidal compounds for inhibiting steroid sulphotase 有权
标题翻译：甾族化合物抑制甾族Sulfotase
公开(公告)号：EP1657247B1
公开(公告)日：2008-09-17
申请号：EP06000817.4
申请日：2002-10-17
申请人： Sterix Limited
发明人： Potter, Barry Victor Lloyd , Reed, Michael John , Woo, Lok Wai Lawrence
IPC分类号： C07J63/00 , A61K31/56 , A61P35/00
CPC分类号： C07J1/0051 , C07J63/00 , C07J63/008

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