公开(公告)号：US07342004B2

公开(公告)日：2008-03-11

申请号：US10367623

申请日：2003-02-14

申请人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Graham Keith Packham ,  Matthew Paul Leese

发明人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Graham Keith Packham ,  Matthew Paul Leese

IPC分类号： A61K31/56 ,  C07J31/00

CPC分类号： A61K31/37 ,  A61K31/565

摘要： There is provided use of a compound of Formula XI: wherein R3 is a sulphamate group and at least of R1 or R2 is a thioether group as disclosed by the present specification, capable of inhibiting steroid sulphatase.

摘要翻译： 提供式XI化合物的用途：其中R 3是氨基磺酸酯基团，并且至少R 1或R 2是 如本说明书所公开的能够抑制类固醇硫酸酯酶的硫醚基团。

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。

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。

公开(公告)号：US07067503B2

公开(公告)日：2006-06-27

申请号：US10367622

申请日：2003-02-14

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

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

IPC分类号： A61K31/58 ,  C07J1/00 ,  C07J43/00

CPC分类号： A61K31/565 ,  A61K31/37

摘要： There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of 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 an aromatic hydrocarbyl group.

摘要翻译： 提供了包含选自氨基磺酸盐基团，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甾体环系统和基团R 1的化合物; 其中所述甾体环体系的D环被式-LR 3 SO 2的基团R 2取代，其中L是任选的连接基团，R 3 芳香族烃基。

公开(公告)号：US08124614B2

公开(公告)日：2012-02-28

申请号：US11855603

申请日：2007-09-14

申请人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo

发明人： Barry Victor Lloyd Potter ,  Michael John Reed ,  Lok Wai Lawrence Woo

IPC分类号： A61K31/473 ,  C07D221/18

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 R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.

摘要翻译： 提供了具有式（I）的化合物，其中G是H或取代基，并且其中R 1是能够抑制类固醇硫酸酯酶的氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基或磺酰胺基中的任何一种 。

公开(公告)号：US20100105764A1

公开(公告)日：2010-04-29

申请号：US12475910

申请日：2009-06-01

申请人： Michael John Reed ,  Atul Purohit ,  Paul Alexander Foster ,  Simon Paul Newman ,  Lok Wai Lawrence Woo ,  Barry Victor Lloyd Potter ,  Gillian Reed

发明人： Michael John Reed ,  Atul Purohit ,  Paul Alexander Foster ,  Simon Paul Newman ,  Lok Wai Lawrence Woo ,  Barry Victor Lloyd Potter ,  Gillian Reed

IPC分类号： A61K31/366 ,  A61P35/00

CPC分类号： A61K31/37

摘要： There is provided a method for the manufacture of a medicament for the treatment of cancer comprising a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2), wherein the cancer is of a type, in which the cancer cells overexpress aromatase enzyme.

摘要翻译： 提供了一种制备用于治疗癌症的药物的方法，其包括能够抑制类固醇硫酸酯酶的化合物（E.C.3.1.6.2），其中所述癌症是癌细胞过度表达芳香酶的类型。

公开(公告)号：US20090111862A1

公开(公告)日：2009-04-30

申请号：US12056920

申请日：2008-03-27

申请人： Barry Victor Lloyd POTTER ,  Lok Wai Lawrence Woo ,  Atul Purohit ,  Michael John Reed ,  Oliver Brook Sutcliffe ,  Christian Bubert

发明人： Barry Victor Lloyd POTTER ,  Lok Wai Lawrence Woo ,  Atul Purohit ,  Michael John Reed ,  Oliver Brook Sutcliffe ,  Christian Bubert

IPC分类号： A61K31/4196 ,  A61P35/00

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.

摘要翻译： 提供式I的化合物，其中每个T独立地选自H，烃基，-F-R和与D，E，P或Q之一的键，或与P和Q中的一个形成环; Z是一个合适的原子，其化合价是m; D，E和F各自独立地为任选的连接基团，其中当Z为氮时，E不是CH 2和C-O; P，Q和R彼此独立地是环系; 并且至少Q包含氨基磺酸酯基团。

公开(公告)号：US20090023710A1

公开(公告)日：2009-01-22

申请号：US11968436

申请日：2008-01-02

申请人： Nigel Vicker ,  Joanna Mary Day ,  Helen Victoria Bailey ,  Wesley Heaton ,  Ana Maria Ramos Gonzalez ,  Christopher Mark Sharland ,  Michael John Reed ,  Atul Purohit ,  Barry Victor Lloyd Potter

发明人： Nigel Vicker ,  Joanna Mary Day ,  Helen Victoria Bailey ,  Wesley Heaton ,  Ana Maria Ramos Gonzalez ,  Christopher Mark Sharland ,  Michael John Reed ,  Atul Purohit ,  Barry Victor Lloyd Potter

IPC分类号： A61K31/55 ,  C07D211/58 ,  C07C233/22 ,  A61P35/00 ,  C07D223/12 ,  A61K31/167

CPC分类号： C07C237/22 ,  C07C233/36 ,  C07D209/20 ,  C07D211/56 ,  C07D211/58 ,  C07D211/62 ,  C07D211/96 ,  C07D215/38 ,  C07D215/44 ,  C07D223/12 ,  C07D223/16 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D451/04

摘要： There is provided a compound having Formula (I) wherein each of R1, R2, R3, R4, R5, R6 and R7 are independently selected from (a) H, (b) R17, —OC(R17)3, —OCH(R17)2, —OCH2R17, —C(R17)3, —CH(R17)2, or —CH2R17 wherein R17 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R11)C(O)R13; wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; each of rings A and B are selected from five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring; X is an optional group selected from O, S, S═O, S(═O)2, C═O, S(═O)2NR8, C═ONR9, NR10, wherein R8, R9 and R10 are independently selected from H and hydrocarbyl, wherein n and p are independently selected from 0 and 1; Y is (R11)1-3 wherein each R11 is independently selected from NR12, CR13R14, S(═O)2 and C═O, wherein R12, R13 and R14 are independently selected from Hand hydrocarbyl; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a —R15—NR16— group wherein R15 is an optionally substituted C1-6 alkyl chain and R16 is selected from H and hydrocarbyl; and R3 is selected from Formula (A).

公开(公告)号：US07361677B2

公开(公告)日：2008-04-22

申请号：US11209186

申请日：2005-08-22

申请人： Barry Victor Lloyd Potter ,  Lok Wai Lawrence Woo ,  Atul Purohit ,  Michael John Reed ,  Oliver Brook Sutcliffe ,  Christian Bubert

发明人： Barry Victor Lloyd Potter ,  Lok Wai Lawrence Woo ,  Atul Purohit ,  Michael John Reed ,  Oliver Brook Sutcliffe ,  Christian Bubert

IPC分类号： A61K31/4196 ,  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.

摘要翻译： 提供式I的化合物，其中每个T独立地选自H，烃基，-F-R和与D，E，P或Q之一的键，或与P和Q中的一个形成环; Z是一个合适的原子，其化合价是m; D，E和F各自独立地为任选的连接基团，其中当Z为氮时，E不是CH 2和C-O; P，Q和R彼此独立地是环系; 并且至少Q包含氨基磺酸酯基团。

公开(公告)号：US07309715B2

公开(公告)日：2007-12-18

申请号：US10690708

申请日：2003-10-23

申请人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

发明人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

IPC分类号： A61K31/428 ,  C07D277/62

CPC分类号： C07D277/64 ,  C07D209/08 ,  C07D235/08 ,  C07D263/56 ,  C07D277/14 ,  C07D417/12

摘要： A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.

摘要翻译： 具有式I的化合物，其中R 1和R 2中的一个是下式的基团其中R 4选自H和烃基， R 5是烃基，L是任选的连接基团，或者R 1和R 2一起形成被下列基团取代的环，其中， R 3是H或取代基，其中X选自S，O，NR 6和C（R 7）（R 7） 其中R 6选自H和烃基，其中R 7和R 8中的每一个是 独立地选自H和烃基。