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1. 发明授权

US08470860B2 Phenyl-sulfamates as aromatase inhibitors 失效
标题翻译：苯基磺酸盐作为芳香酶抑制剂
公开(公告)号：US08470860B2
公开(公告)日：2013-06-25
申请号：US12841355
申请日：2010-07-22
申请人： Lok Wai Lawrence Woo , Toby Jackson , Christian Bubert , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
发明人： Lok Wai Lawrence Woo , Toby Jackson , Christian Bubert , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08
摘要： There is provided a compound of Formula I wherein X, Y and Z are each independently of each other an optional linker group; R1 is a ring system; R2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2) and halogens; R3 and R4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
摘要翻译：提供式I的化合物，其中X，Y和Z各自独立地为任选的连接基团; R1是环系; R2选自烃基，羟基烃基，氰基（-CN），硝基（-NO 2）和卤素; R 3和R 4独立地选自H和烃基，环A和B独立地任选被进一步取代。

2. 发明授权

US08148415B2 Sulfamic acid ester compounds useful in the inhibition of steroid sulphatase activity and aromatase activity 有权
标题翻译：用于抑制类固醇硫酸酯酶活性和芳香酶活性的氨基磺酸酯化合物
公开(公告)号：US08148415B2
公开(公告)日：2012-04-03
申请号：US11603941
申请日：2006-11-22
申请人： Barry Victor Lloyd Potter , Michael John Reed , Lok Wai Lawrence Woo , Atul Purohit , Christian Burbert , Paul Michael Wood , Oliver Brook Sutcliffe
发明人： Barry Victor Lloyd Potter , Michael John Reed , Lok Wai Lawrence Woo , Atul Purohit , Christian Burbert , Paul Michael Wood , Oliver Brook Sutcliffe
IPC分类号： A61K31/4192 , A61K31/4196 , C07D249/04 , C07D249/08
CPC分类号： C07D249/08
摘要： The present invention relates to steroid sulphatase and/or aromatase inhibitors of Formula III or Formula IV, wherein A is selected from H, OH, halogen and hydrocarbyl; D, E and F are each independently of each other an optional linker group; P, Q and R are independently of each other a ring system, wherein R4 and R5 are independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl or optionally contain one or more hetero atoms or groups, and which can be used in medicine.
摘要翻译：本发明涉及式III或式IV的类固醇硫酸酯酶和/或芳香酶抑制剂，其中A选自H，OH，卤素和烃基; D，E和F各自独立地为任选的连接基团; P，Q和R彼此独立地为环系，其中R4和R5独立地选自H，烷基，环烷基，烯基，酰基和芳基，或其组合，或一起表示亚烷基，其中烷基或环烷基或烯基或任选地含有一个或多个杂原子或基团，并且其可以用于医药中。

3. 发明授权

US08119627B2 Heterocyclic compounds as inhibitors of 17beta-HSD3 有权
标题翻译：杂环化合物作为17β-HSD3的抑制剂
公开(公告)号：US08119627B2
公开(公告)日：2012-02-21
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
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 rings A and B is 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, and —NR10, 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; 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.
摘要翻译：提供了具有式（I）的化合物，其中环A和B各自选自5或6元碳环，任选地含有一个或多个选自N，S和O的杂原子，并且任选地与另一个环稠合; X是选自O，S，-S = O，-S（= O）2，-C = O，-S（= O）2 NR 8，-CONONR 9和-NR 10的任选基团，其中n和p 独立地选自0和1; Y是（R 11）1-3，其中每个R 11独立地选自-NR 12，-CR 13 R 14，-S（= O）2和-C≡O; Z选自（i）含有六元或七元环的碳和至少一个氮，其可以是任选取代的，其中取代基可以一起形成稠合的另外的环; 和（ii）-R 15 -NR 16 - 基团。

4. 发明授权

US08022224B2 1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors 有权
标题翻译： 1,2,4-三唑-1-基双苯基衍生物，用于治疗内分泌依赖性肿瘤
公开(公告)号：US08022224B2
公开(公告)日：2011-09-20
申请号：US12139237
申请日：2008-06-13
申请人： Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , 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： 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. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.
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。这些化合物抑制类固醇硫酸酯酶和芳香酶活性，并且可用于治疗内分泌依赖性肿瘤。

5. 发明申请

US20100222299A1 COMPOUND 失效
标题翻译：复合
公开(公告)号：US20100222299A1
公开(公告)日：2010-09-02
申请号：US12593560
申请日：2008-03-27
申请人： Fabrice Jourdan , Meriel Kimberley , Matthew Leese , Barry Victor Lloyd Potter , Atul Purohit , Michael John Reed
发明人： Fabrice Jourdan , Meriel Kimberley , Matthew Leese , Barry Victor Lloyd Potter , Atul Purohit , Michael John Reed
IPC分类号： A61K31/695 , A61P35/00 , A61K31/472 , C07D217/04 , C07F7/18 , C07D401/06 , C07D217/24
CPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55
摘要： The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.
摘要翻译：本发明涉及四氢异喹啉化合物及其在抑制和/或预防肿瘤生长中的用途。

6. 发明授权

US07786152B2 Compound 失效
标题翻译：复合
公开(公告)号：US07786152B2
公开(公告)日：2010-08-31
申请号：US11979160
申请日：2007-10-31
申请人： Nigel Vicker , Su Xiangdon , Dharshini Ganeshapillai , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Su Xiangdon , Dharshini Ganeshapillai , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/428
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 2一起形成被其中R 3是H或取代基，其中X选自S，O，NR 6和C（R 7）（R 8），其中R 6选自H和烃基，其中R 7和R 8各自独立地选自H 和烃基。

7. 发明申请

US20100173963A1 COMPOUND 有权
标题翻译：复合
公开(公告)号：US20100173963A1
公开(公告)日：2010-07-08
申请号：US12555342
申请日：2009-09-08
申请人： Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter , Gillin Reed
发明人： Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter , Gillin Reed
IPC分类号： A61K31/4196 , C07D249/08 , C07D405/10
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。

8. 发明申请

US20100120789A1 Compound 审中-公开
标题翻译：复合
公开(公告)号：US20100120789A1
公开(公告)日：2010-05-13
申请号：US12554943
申请日：2009-09-07
申请人： Nigel Vicker , Xiangdong Su , Fabienne Praduax , Michael John Reed , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Xiangdong Su , Fabienne Praduax , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/497 , C07C233/00 , A61K31/165 , A61K31/4365 , C07D495/04 , C07D405/02 , C12Q1/32
CPC分类号： C11D3/0073 , C11D3/2086 , C11D3/33 , C11D7/265 , C11D7/3245 , C11D11/0041
摘要： There is provided a compound having Formula I R1—Z—R2 Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S═O, and S(═O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(═O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R3, R4, R5, R6, R8, R9, R11, R12, R13, R14, R15 and R16, are independently selected from H, hydrocarbyl and halogen, wherein each of R7 and R10 are independently selected from H and hydrocarbyl.
摘要翻译：提供了具有式I的化合物R1-Z-R2式Ⅰ其中R1是选自任选取代的稠合多环基团，取代的烷基，支链烷基和任选取代的环烷基的基团Z是一种或多种羰基或羰基的等排基团选自任选取代的芳环和任选取代的杂环，其中（a）R 2是2-取代的噻吩基团，和/或（b）Z是式-C （= O）-CR 3 R 4 -X-（CR 5 R 6）n - ，其中X选自NR 7，S，O，S = O和S（= O）2，其中n为0或1和/或（c） R1是金刚烷基，Z是或包含酰胺基，和/或（d）R1是金刚烷基，Z是或包含式 - （CR8R9）对NR10-S（= O）2- （CR11R12）q-，其中p为0或1，q为0或1，和/或（e）R1为金刚烷基，Z为或包含式 - （CR13R14）vY-（CR15R16）w- 在哪里 Y是杂芳基环中的键是羰基的等离子体的杂芳基，其中v是0或1，w是0或1; 其中R 3，R 4，R 5，R 6，R 8，R 9，R 11，R 12，R 13，R 14，R 15和R 16各自独立地选自H，烃基和卤素，其中R 7和R 10各自独立地选自H和烃基。

9. 发明申请

US20080319037A1 1,2,4-TRIAZOL-1-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMORS 有权
标题翻译： 1,2,4-三唑-1-基联苯衍生物用于治疗依靠内皮素的肿瘤
公开(公告)号：US20080319037A1
公开(公告)日：2008-12-25
申请号：US12139237
申请日：2008-06-13
申请人： Lok Wai Lawrence Woo , Toby Jackson , Atul Purohit , Michael John Reed , 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： A61K31/4196 , C07D249/08 , A61P35/00
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. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.
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中的四个为H，R3，R4，R5，R6和R7之一为-Y-R8。这些化合物抑制类固醇硫酸酯酶和芳香酶活性，并且可用于治疗内分泌依赖性肿瘤。

10. 发明授权

US07342004B2 Thioether sulphamate steroids as steroid inhibitors and anti-cancer compounds 失效
标题翻译：硫代硫代氨基甲酸酯类固醇作为类固醇抑制剂和抗癌化合物
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。

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