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1. 发明专利

JP2014040488A 1,2,4-triazole derivative including sulfamate group as aromatase inhibitor 审中-公开
标题翻译： 1,2,4-三唑衍生物，其中包含磺酰胺类作为芳香酶抑制剂
公开(公告)号：JP2014040488A
公开(公告)日：2014-03-06
申请号：JP2013249821
申请日：2013-12-03
申请人： Sterix Ltd , ステリックスリミテッド
发明人： POTTER BARRY VICTOR LLOYD , WOO LOK WAI LAWRENCE , PUROHIT ATUL , READ MICHAEL J , BUBERT CHRISTIAN , SUTCLIFFE OLIVER BROOK
IPC分类号： C07D249/08 , C12Q1/02 , A61K31/4196 , A61K31/423 , A61K31/424 , A61K31/428 , A61K45/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/12 , A61P15/00 , A61P15/06 , A61P15/18 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D249/14 , C07D413/12 , C07D417/12 , C07D521/00 , C12Q1/34
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a new compound appropriate for inhibiting the steroid sulfatase activity and the aromatase activity.SOLUTION: A compound represented by formula (I) is provided, where each T represents a bond with one of H, hydrocarbyl, -F-R- and D, E, P, or Q, or forms into a ring together with one of P and Q; Z is a proper atom having a valence of m; D, E, and F are proper linker groups independent from each other, and for Z of nitrogen, E is other than CHand C=O; P, Q, and R are ring systems independent from each other; and at least Q includes a sulfamate group.
摘要翻译：要解决的问题：提供适合于抑制类固醇硫酸酯酶活性和芳香酶活性的新化合物。溶液：提供由式（I）表示的化合物，其中每个T表示与H，烃基，-FR之一的键 - 和D，E，P或Q，或与P和Q之一形成环; Z是具有m价的适当原子; D，E和F是相互独立的适当的连接基团，对于氮的Z，E不是CH且C = O; P，Q和R是彼此独立的环系; 并且至少Q包括氨基磺酸酯基团。

2. 发明专利

JP2010195819A 1,2,4-triazole derivative containing sulfamate group as aromatase inhibitor 有权
标题翻译：含有磺酰胺的1,2,4-三唑衍生物作为芳香酶抑制剂
公开(公告)号：JP2010195819A
公开(公告)日：2010-09-09
申请号：JP2010108842
申请日：2010-05-10
申请人： Sterix Ltd , ステリックスリミテッド
发明人： POTTER BARRY VICTOR LLOYD , WOO LOK WAI LAWRENCE , PUROHIT ATUL , READ MICHAEL J , BUBERT CHRISTIAN , SUTCLIFFE OLIVER BROOK
IPC分类号： C07D249/08 , C12Q1/02 , A61K31/4196 , A61K31/423 , A61K31/424 , A61K31/428 , A61K45/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/12 , A61P15/00 , A61P15/06 , A61P15/18 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D249/14 , C07D413/12 , C07D417/12 , C07D521/00 , C12Q1/34
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a new compound suitable for the inhibition of steroidsulfatase activity and aromatase activity. SOLUTION: This compound expressed by formula I [wherein, Ts are each H, hydrocarbyl, -F-R- or a bond with one of D, E, P or Q, or forms a ring together with one of P and Q; Z is a suitable atom having m-atomic valences; D, E and F are each independently a suitable linker group, and in the case that the Z is nitrogen, E is other than CH 2 and C=O; P, Q and R are each independently a ring system; and at least Q contains a sulfamate group] is provided. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供适合于抑制类固醇硫酸酯酶活性和芳香酶活性的新化合物。解决方案：由式I表示的化合物[其中，Ts各自为H，烃基，-F-R-或与D，E，P或Q之一的键，或与P和Q之一形成环; Z是具有m原子价的合适原子; D，E和F各自独立地为合适的连接基团，并且在Z为氮的情况下，E不是CH 2，且C = O; P，Q和R各自独立地是环系; 并且至少Q含有氨基磺酸酯基]。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2008001723A Non-steroidal polycyclic ring sulphamate derivatives as oestrone sulphatase inhibitors, their preparation and their use 有权
标题翻译：非甾体多环化合物磺酰胺衍生物作为骨架硫酸酯酶抑制剂，其制备及其用途
公开(公告)号：JP2008001723A
公开(公告)日：2008-01-10
申请号：JP2007240240
申请日：2007-09-14
申请人： Sterix Ltd , ステリックスリミテッド
发明人： READ MICHAEL J , POTTER BARRY V L
IPC分类号： C07D311/16 , A61K31/352 , A61K31/37 , A61P35/00 , A61P43/00
CPC分类号： C07D311/16 , A61K31/37
摘要： PROBLEM TO BE SOLVED: To provide a compound which is suitable for inhibiting E1-STS and does not have an oestrogene effect or a minimal oestrogene effect.
SOLUTION: 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 has a multicyclic ring structure having two or more rings, wherein at least two rings imitate the rings A and B of the oestrone. Preferably, the compound is of general Formula (A), wherein R
1 -R
6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R
1 -R
6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH
2 , or a substituted C.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供适合于抑制E1-STS并且不具有雌二醇作用或最小的雌二醇作用的化合物。解决方案：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。化合物具有具有两个或多个环的多环结构，其中至少两个环模仿所述雌酮的环A和B。优选地，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盐物; 但其中R SB 1 -R SB 6中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 或取代的C中的任何一个。（C）2008，JPO＆INPIT

4. 发明专利

JP2002145891A STEROID SULFATASE INHIBITOR 审中-公开
公开(公告)号：JP2002145891A
公开(公告)日：2002-05-22
申请号：JP2001277335
申请日：2001-09-12
申请人： STERIX LTD
发明人： READ MICHAEL J , POTTER BARRY V L
IPC分类号： A61K31/565 , A61K31/56 , A61K31/566 , A61K31/661 , A61K31/663 , A61P35/00 , A61P43/00 , C07F9/145 , C07J31/00 , C07J51/00 , C07J53/00 , C12N9/16
摘要： PROBLEM TO BE SOLVED: To obtain a new compound capable of inhibiting the steroid sulfatase activity in vitro and in vivo, a pharmaceutical composition effective in treatment of estrogen-dependent tumors and a pharmaceutical composition effective in treatment of mammary cancer and to provide a method for treating the estrogen-dependent tumors of mammals, especially humans and a method for treating the mammary cancers of mammals, especially females. SOLUTION: The sulfonate ester and phosphonate ester are represented by the following formula (R is selected from H, an alkyl, a cycloalkyl, an alkenyl and an aryl; X is P or S; Y is OH when X is P and Y is O when X is S; and an O-polycyclic group denotes a residue of a polycyclic alcohol; and the sulfate of the polycyclic alcohol is a substrate for an enzyme having the steroid sulfatase activity).

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