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1. 发明申请

WO2008117061A3 TETRAHYDROISOQUINOLINES AS TUMOUR GROWTH INHIBITORS 审中-公开
标题翻译：四氢叶酸作为肿瘤生长抑制剂
公开(公告)号：WO2008117061A3
公开(公告)日：2009-05-14
申请号：PCT/GB2008001072
申请日：2008-03-27
申请人： STERIX LTD , JOURDAN FABRICE , KIMBERLEY MERIEL , LEESE MATTHEW , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN
发明人： JOURDAN FABRICE , KIMBERLEY MERIEL , LEESE MATTHEW , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN
IPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55 , A61P35/00
CPC分类号： A61K31/40 , A61K31/403 , A61K31/435 , A61K31/47 , A61K31/55
摘要： The present invention provides a compound of Formula (I) or Formula (Il) wherein A is selected from CR10R11, -S(=O)2-, -NR12-,and C=O, wherein R10 and R11 independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, R12 is selected from H and hydrocarbyl; B is selected from (CR13R14)1-3, C=O, CR15R16C=O, -S(=O)2-, -NR17- and -NR18-C(=O)-, wherein each of R13, R14, R15 and R16 is independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, R17 and R18 are independently selected from H and hydrocarbyl; R1 is selected from OH, O-hydrocarbyl, O-heterohydrocarbyl, -SO2-hydrocarbyl, -CH=CH2, halogen, -OSO2NR19R20, -C(=O)-NR21R22, -NR23-C(=O)H and -NR35R36; wherein each of R19, R20, R21, R22, R23, R35 and R36 is independently is selected from H and hydrocarbyl; R2 is selected from H, -O-hydrocarbyl, -S-hydrocarbyl, hydrocarbyl, -CN, -NO2, and halogens, R3 is selected from Formula (A), Formula (B), Formula (C), Formula (D) wherein each of R4, R5, R6, R7 and R8 is independently selected from H, -OH, hydrocarbyl, -O-hydrocarbyl, -COOH or an ester thereof, halocarbyl, -O-halocarbyl, acyl, -O-acyl, -NR29-acyl, -O-SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, -NO2, and halogens, R9 is selected from H and hydrocarbyl, and each R29 to R33 is independently selected from H and hydrocarbyl; and wherein two or more of R4, R5, R6, R7, R8 and R9 may together form a ring; wherein when R1 is OH and R3 is of Formula (D), (i) at least one of R4, R5, R6, R7 and R8 is independently selected from halocarbyl, -O-halocarbyl, -O-acyl, -NR29-acyl, -O- SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, and halogens, or (ii) two or more of R4, R5, R6, R7 and R8 together form a ring, or (iii) at least three of R4, R5, R6, R7 and R8 are independently selected from -OH, hydrocarbyl, -O-hydrocarbyl, halocarbyl, -O-halocarbyl, -O-acyl, -NR29-acyl, -O-SO2NR19R20, -NR30R31, -NR32SO2R33, -CN, -NO2, and halogens; wherein h is an optional bond, wherein G is CR24R25, wherein R24 and R25 independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens, or wherein when h is present G is CR24, wherein R24 is selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens; n is 0, 1 or 2, each D is independently selected from O, NR26 and CR27R28, wherein each R26 is independently selected from H and hydrocarbyl; and each R27 and R28 is independently selected from H, -OH, hydrocarbyl, -CN, -NO2, and halogens.
摘要翻译：本发明提供式（I）或式（II）的化合物，其中A选自CR 10 R 11，-S（= O）2 - ， - NR 12 - 和C = O，其中R 10和R 11独立地选自H， -OH，烃基，-CN，-NO 2和卤素，R 12选自H和烃基; B选自（CR13R14）1-3，C = O，CR15R16C = O，-S（= O）2-，-NR17-和-NR18-C（= O） - ，其中R13，R14，R15 并且R 16独立地选自H，-OH，烃基，-CN，-NO 2和卤素，R 17和R 18独立地选自H和烃基; R 1选自OH，O-烃基，O-杂烃基，-SO 2 - 烃基，-CH = CH 2，卤素，-OSO 2 NR 19 R 20，-C（= O）-NR 21 R 22，-NR 23 -C（= O）H和-NR 35 R 36 ; 其中R19，R20，R21，R22，R23，R35和R36各自独立地选自H和烃基; R2选自H，-O-烃基，-S-烃基，烃基，-CN，-NO 2和卤素，R 3选自式（A），式（B），式（C），式（D）其中R4，R5，R6，R7和R8各自独立地选自H，-OH，烃基，-O-烃基，-COOH或其酯，卤代羰基，-O-卤代羰基，酰基，-O-酰基， NR29-酰基，-O-SO2NR19R20，-NR30R31，-NR32SO2R33，-CN，-NO2和卤素，R9选自H和烃基，每个R29至R33独立地选自H和烃基; 并且其中R4，R5，R6，R7，R8和R9中的两个或更多个可以一起形成环; 其中当R 1是OH且R 3具有式（D）时，（i）R 4，R 5，R 6，R 7和R 8中的至少一个独立地选自卤代烃基，-O-卤代羰基，-O-酰基，-NR 29 - ，-O-SO 2 NR 19 R 20，-NR 30 R 31，-NR 32 SO 2 R 33，-CN和卤素，或（ii）R4，R5，R6，R7和R8中的两个或更多个一起形成环，或（iii） R5，R6，R7和R8独立地选自-OH，烃基，-O-烃基，卤代烃基，-O-卤代烃基，-O-酰基，-NR29-酰基，-O-SO2NR19R20，-NR30R31，-NR32SO2R33， CN，-NO 2和卤素; 其中h是任选的键，其中G是CR 24 R 25，其中R 24和R 25独立地选自H，-OH，烃基，-CN，-NO 2和卤素，或其中当存在h时，G是CR 24，其中R 24选自 H，-OH，烃基，-CN，-NO 2和卤素; n是0,1或2，每个D独立地选自O，NR 26和CR 27 R 28，其中每个R 26独立地选自H和烃基; 并且每个R 27和R 28独立地选自H，-OH，烃基，-CN，-NO 2和卤素。

2. 发明申请

WO2007096647A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2007096647A2
公开(公告)日：2007-08-30
申请号：PCT/GB2007/000655
申请日：2007-02-26
申请人： STERIX LIMITED , VICKER, Nigel , ALLAN, Gillian, Margaret , LAWRENCE, Harshani, Rithma, Ruchiranani , DAY, Joanna, Mary , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
发明人： VICKER, Nigel , ALLAN, Gillian, Margaret , LAWRENCE, Harshani, Rithma, Ruchiranani , DAY, Joanna, Mary , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
IPC分类号： C07D213/75 , C07C49/757 , C07D231/54 , C07D213/40 , C07D231/12 , C07D261/08 , C07D277/40 , C07D307/52 , C07C255/40 , C07D231/14 , C07D231/38 , C07D307/60 , C07C43/205 , C07C43/275 , C07D317/54
CPC分类号： C07C323/22 , C07C37/62 , C07C45/00 , C07C45/46 , C07C45/673 , C07C45/68 , C07C45/71 , C07C49/747 , C07C49/753 , C07C49/755 , C07C49/757 , C07C49/83 , C07C49/84 , C07C49/86 , C07C59/90 , C07C69/712 , C07C69/738 , C07C235/74 , C07C235/78 , C07C235/84 , C07C255/40 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/75 , C07D231/12 , C07D231/38 , C07D241/12 , C07D261/08 , C07D277/40 , C07D317/54 , C07D401/12 , C07C39/367
摘要： There is provided a compound of Formula (I): wherein R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , and R 10 , are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO 2 ), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R 9 is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO 2 NR 1 R 2 ; wherein R 1 and R 2 are independently selected from H and hydrocarbyl or (B) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is the group -C(=0)-CR 11 R 12 -R 8 wherein R 8 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (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 or alkenyl-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, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 the enol tautomer thereof wherein R 11 and R 12 are independently selected from H and hydrocarbyl; or (C) at least one of R 3 , R 4 , R 5 , R 6 and R 7 together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a ring containing -C(=O)-; or (D) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, and heteroaryl groups or (E) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from -CN, -C(R 13 )=N-O-alkyl group, - C(R 14 )=N-O-H group, optionally substituted pyrazole, optionally substituted thiazole, optionally substituted oxazole, optionally substituted isoxazole, optionally substituted pyridine, and optionally substituted pyrimidine, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a nitrogen containing ring; wherein R 13 and R 14 are independently selected from H and hydrocarbyl.
摘要翻译：提供式（I）的化合物：其中R 3，R 4，R 5，R 6，/ R 7，R 9和R 10独立地选自-H，-OH，烃基，羟基烃基，氰基（-CN），硝基（-NO 2 N 2）和卤素; 其中环A任选进一步被取代，其中X是键或连接基团，其中（A）（i）R 9选自烷基和卤素基团; 和（ii）R 10选自-OH，羟基烃基和-OSO 2 NR 1 R 2 R 2。其中R 1和R 2独立地选自H和烃基或（B）R 3，R 4中的至少一个 R 5，R 6和R 7是基团-C（= O）-CR 11，其中R 8选自（ⅰ）烷氧基烷基（ⅱ）腈基，（ⅰ） iii）烷基芳基，其中芳基被除了其中芳基被取代的（C 1 -C 6）烯基芳基以外的其它取代基取代（v）烷基杂芳基，其中当杂芳基仅在环中仅包含C和N时，芳基被甲基除外（vi）烯基杂芳基（vii）= NO-烷基或= NOH基（viii）支链烯基（ix）烷基醇基或链烯基（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 - 取代和/或（c）酰胺被至少一个烷基取代烯基杂环基，烷基杂芳基，烯基杂芳基，杂芳基，烷基胺基，烷氧基烷基，烷基芳基，直链或支链烷基，（xi）-CHO，或与另一个R 3 R 4，R 5，R 6和R 7其烯醇互变异构体，其中R 11 R 12和R 12独立地选自H和烃基; 或（C）R 3，R 4，R 5，R 6和R 6中的至少一个，与R 3，R 4，R 5，R 6，R 6，R 5，R 5，和R 7形成含有-C（= O） - 的环; 或（D）R 3，R 4，R 5，R 6和R 6中的至少一个，选自烷基杂环基，烯基杂环基，烷基杂芳基，烯基杂芳基和杂芳基，或（E）R 3，R 4中的至少一个， R 5，R 6，R 7和R 7选自-CN，-C（R 13））= NO-烷基，-C（R 14）= NOH基，任选取代的吡唑，任选取代的噻唑，任选取代的恶唑，任选取代的异恶唑，任选取代的吡啶和任选取代的嘧啶，或与R 3，R 4，R 5，R 6和R 7中的另一个一起， / SUB>形成含氮环; 其中R 13和R 14独立地选自H和烃基。

3. 发明申请

WO2007068905A1 1,2,4-TRIAZOL-l-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMOURS 审中-公开
标题翻译：用于治疗依靠内肿瘤的肿瘤的1,2,4-三唑-1-基联苯衍生物
公开(公告)号：WO2007068905A1
公开(公告)日：2007-06-21
申请号：PCT/GB2006/004630
申请日：2006-12-12
申请人： STERIX LIMITED , WOO, Lok, Wai, Lawrence , JACKSON, Toby , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
发明人： WOO, Lok, Wai, Lawrence , JACKSON, Toby , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
IPC分类号： C07D249/08 , C07D405/10 , A61K31/4196 , A61P35/00
CPC分类号： C07D249/08 , C07D405/10
摘要： There is provided a compound of Formula I wherein R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from H and -Y-R 6 ; wherein each R 8 is independently selected from -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO 2 ), H-bond acceptors, and halogens; wherein at Jeast one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 wherein R 8 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 R 9 is selected from H, -OH and -OSO 2 NR 1 R 2 ; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 ; OR (b) R 9 is -OSO 2 NR 1 R 2 or - OH and four of R 3 , R 4 , R 5 , R 6 and R 7 are H and one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 . These compounds inhibit steroid sulphatase and aronatase activity and are useful in the treatment of endocrine-dependent tumours.
摘要翻译：提供式I的化合物，其中R 3，R 4，R 5，R 6和R 3 7个独立地选自H和-YR 6; 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 2），H键受体和卤素; 其中在R 3 R 3，R 4，R 5，R 6和R 7的每一个其中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R 8选自取代和未取代的杂环和氨基取代的苯基。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R 9选自H，-OH和-OSO 2 NR 1 R 2; 其中R1和R2独立地选自H和烃基; 其中（a）X是一个键，R 3，R 4，R 5，R 6， R 3和R 7是-YR 8; OR（b）R 9是-OSO 2 NR 1 R 2 R 2或 - OH，R 4中的四个 R 3，R 4，R 5，R 6和R 7均为H和 R 3，R 4，R 5，R 6和R 7中的一个，是-YR <8> 。这些化合物抑制类固醇硫酸酯酶和aronatase活性，并且可用于治疗内分泌依赖性肿瘤。

4. 发明申请

WO2004037251A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 AND TYPE 2 审中-公开
标题翻译： 11-羟基甾体脱氢脱氢酶1型和2型的抑制剂
公开(公告)号：WO2004037251A1
公开(公告)日：2004-05-06
申请号：PCT/GB2003/004590
申请日：2003-10-23
申请人： STERIX LIMITED , VICKER, Nigel , SU, Xiangdong , GANESHAPILLAI, Dharshini , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
发明人： VICKER, Nigel , SU, Xiangdong , GANESHAPILLAI, Dharshini , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
IPC分类号： A61K31/428
CPC分类号： C07D263/56 , C07D209/08 , C07D209/42 , C07D235/08 , C07D235/10 , C07D277/64 , C07D277/68 , C07D277/74 , C07D277/82
摘要： There is provided a compound having Formula (I): wherein one of R 1 and R 2 is a group of the Formula (a), wherein R 4 is selected from H and hydrocarbyl, R 5 is a hydrocarbyl group and L is an optional linker group, or R 1 and R 2 together form a ring substituted with the group (Formula (a)) wherein R 3 is H or a substituent, and wherein X is selected from S, O, NR 6 and C(R 7 )(R 8 ), wherein R 6 is selected from H and hydrocarbyl groups, wherein each of R 7 and R 8 are independently selected from H and hydrocarbyl groups.
摘要翻译：提供具有式（I）的化合物：其中R 1和R 2之一是式（a）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 R 1和R 2一起形成被其中R 3为H或取代基的基团（式（a））取代的环，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。

5. 发明申请

WO2009066072A3 INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGENASE 审中-公开
标题翻译： 17BA-羟基脱氢酶抑制剂的抑制剂
公开(公告)号：WO2009066072A3
公开(公告)日：2009-10-15
申请号：PCT/GB2008003889
申请日：2008-11-19
申请人： STERIX LTD , VICKER NIGEL , BAILEY HELEN VICTORIA , HEATON WESLEY , DAY JOANNA MARY , PUROHIT ATUL , POTTER BARRY VICTOR LLOYD
发明人： VICKER NIGEL , BAILEY HELEN VICTORIA , HEATON WESLEY , DAY JOANNA MARY , PUROHIT ATUL , POTTER BARRY VICTOR LLOYD
IPC分类号： C07C209/14 , A61K31/167 , A61K31/36 , A61K31/4409 , A61P5/24 , A61P35/00 , C07C211/50 , C07C233/43 , C07C237/42 , C07D207/26 , C07D211/58 , C07D211/62 , C07D317/66
CPC分类号： C07D207/26 , C07C217/90 , C07C233/43 , C07C237/42 , C07D211/58 , C07D211/62 , C07D317/66
摘要： There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 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; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted 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, and wherein the one or more substituents are selected from hydrocarbyl groups.
摘要翻译：提供具有式（I）的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自（a）H，（b）R13，-OC（R13） 3，-OCH（R 13）2，-OCH 2 R 13，-C（R 13）3，-CH（R 13）2或-CH 2 R 13，其中R 13是卤素; （c）-CN; （d）任选取代的烷基，（e）任选取代的杂烷基; （f）任选取代的芳基; （g）任选取代的杂芳基; （h）任选取代的芳基烷基; （i）任选取代的杂芳基烷基; （j）羟基; （k）烷氧基; （I）芳氧基; （m）-SO 2 - 烷基; 和（n）-N（R 14）C（O）R 15，其中R 14和R 15独立地选自H和烃基，其中选择（d）（e）（T）（h）和（i）羟基，C 1-6烷氧基，羧基，羧基烷基，羧酰胺，巯基，氨基，烷基氨基，二烷基氨基，磺酰基，亚磺酰氨基，芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O，S，S = O，S（= O）2，C = O，S（= O）2NR16，C = ONR17，NR18的任选基团，其中R 16，R 17和R 18独立地选自 R 10选自H和烃基，R 11选自CR 19 R 20和C = O，其中R 19和R 20独立地选自H和烃基，R 12选自取代的五或六元碳环，任选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，并且其中一个或多个取代基选自烃基。

6. 发明申请

WO2009066072A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2009066072A2
公开(公告)日：2009-05-28
申请号：PCT/GB2008/003889
申请日：2008-11-19
申请人： STERIX LIMITED , VICKER, Nigel , BAILEY, Helen, Victoria , HEATON, Wesley , DAY, Joanna, Mary , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
发明人： VICKER, Nigel , BAILEY, Helen, Victoria , HEATON, Wesley , DAY, Joanna, Mary , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
IPC分类号： C07C209/14 , C07C211/50 , C07C233/43 , C07C237/42 , C07D207/26 , C07D211/58 , C07D211/62 , C07D317/66 , A61K31/167 , A61K31/4409 , A61K31/36
CPC分类号： C07D207/26 , C07C217/90 , C07C233/43 , C07C237/42 , C07D211/58 , C07D211/62 , C07D317/66
摘要： There is provided a compound having Formula (I), wherein each of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are independently selected from (a) H, (b) R13, -OC(R 13 ) 3 , -OCH(R 13 ) 2 , -OCH 2 R 13 , -C(R 13 ) 3 , -CH(R 13 ) 2 , or -CH 2 R 13 wherein R 13 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; (I) aryloxy; (m) -SO 2 -alkyl; and (n) -N(R 14 )C(O)R 15 , wherein R 14 and R 15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C 1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C 1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O) 2 , C=O, S(=O) 2 NR 16 , C=ONR 17 , NR 18 , in which R 16 , R 17 , and R 18 are independently selected from H and hydrocarbyl, R 10 is selected from H and hydrocarbyl, R 11 is selected from CR 19 R 20 and C=O, in which R 19 and R 20 are independently selected from H and hydrocarbyl, R 12 is selected from a substituted 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, and wherein the one or more substituents are selected from hydrocarbyl groups.
摘要翻译：提供具有式（I）的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自（a）H，（b）R13，-OC（R13） 3，-OCH（R 13）2，-OCH 2 R 13，-C（R 13）3，-CH（R 13）2或-CH 2 R 13，其中R 13是卤素; （c）-CN; （d）任选取代的烷基，（e）任选取代的杂烷基; （f）任选取代的芳基; （g）任选取代的杂芳基; （h）任选取代的芳基烷基; （i）任选取代的杂芳基烷基; （j）羟基; （k）烷氧基; （I）芳氧基; （m）-SO 2 - 烷基; 和（n）-N（R 14）C（O）R 15，其中R 14和R 15独立地选自H和烃基，其中选择（d）（e）（T）（h）和（i）羟基，C 1-6烷氧基，羧基，羧基烷基，羧酰胺，巯基，氨基，烷基氨基，二烷基氨基，磺酰基，亚磺酰氨基，芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O，S，S = O，S（= O）2，C = O，S（= O）2NR16，C = ONR17，NR18的任选基团，其中R 16，R 17和R 18独立地选自 R 10选自H和烃基，R 11选自CR 19 R 20和C = O，其中R 19和R 20独立地选自H和烃基，R 12选自取代的五或六元碳环，任选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，并且其中一个或多个取代基选自烃基。

7. 发明申请

WO2008096155A1 COMPOSITION COMPRISING A GLYCOLYTIC INHIBITOR AND A RING SYSTEM COMPRISING A SULPHAMATE GROUP FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：包含糖尿病抑制剂和包含用于治疗癌症的磺酰胺类的环系统的组合物
公开(公告)号：WO2008096155A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000448
申请日：2008-02-07
申请人： STERIX LIMITED , TAGG, Sarah, Louise, Claire , FOSTER, Paul, Alexander , NEWMAN, Simon, Paul , REED, Michael, John , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
发明人： TAGG, Sarah, Louise, Claire , FOSTER, Paul, Alexander , NEWMAN, Simon, Paul , REED, Michael, John , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
IPC分类号： A61K31/33 , A61K31/7004 , A61K31/565 , A61P35/00
CPC分类号： A61K31/33 , A61K31/565 , A61K31/7004 , A61K45/06 , A61K2300/00
摘要： The present invention provides a composition comprising (a) a glycolytic inhibitor (b) a compound comprising a ring system substituted with at least one of a suiphamate group and an alkoxy group; wherein (a) and (b) are different.
摘要翻译：本发明提供一种组合物，其包含（a）糖酵解抑制剂（b）包含被至少一个磺酸酯基和烷氧基取代的环系的化合物; 其中（a）和（b）不同。

8. 发明申请

WO2007096647A3 DIARYL COMPOUNDS AS NON-STEROIDAL INHIBITORS OF 17-BETA HYDROXYSTEROID DEHYDROGENASE AND/OR STEROID SULPHATASE FOR THE TREATMENT OF OESTROGEN-RELATED DISEASES SUCH AS HORMONE DEPENDENT BREAST CANCER 审中-公开
标题翻译：作为用于治疗类雌激素相关疾病的17-羟基睾酮脱氢酶和/或甾体硫酸酯的非甾体抑制剂的DIARYL化合物如依赖于乳腺癌的乳腺癌
公开(公告)号：WO2007096647A3
公开(公告)日：2008-01-17
申请号：PCT/GB2007000655
申请日：2007-02-26
申请人： STERIX LTD , VICKER NIGEL , ALLAN GILLIAN MARGARET , LAWRENCE HARSHANI RITHMA RUCHI , DAY JOANNA MARY , PUROHIT ATUL , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
发明人： VICKER NIGEL , ALLAN GILLIAN MARGARET , LAWRENCE HARSHANI RITHMA RUCHI , DAY JOANNA MARY , PUROHIT ATUL , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
IPC分类号： C07D213/75 , C07C43/205 , C07C43/275 , C07C49/757 , C07C255/40 , C07D213/40 , C07D231/12 , C07D231/14 , C07D231/38 , C07D231/40 , C07D231/54 , C07D261/08 , C07D277/40 , C07D307/52 , C07D307/60 , C07D317/54
CPC分类号： C07C323/22 , C07C37/62 , C07C45/00 , C07C45/46 , C07C45/673 , C07C45/68 , C07C45/71 , C07C49/747 , C07C49/753 , C07C49/755 , C07C49/757 , C07C49/83 , C07C49/84 , C07C49/86 , C07C59/90 , C07C69/712 , C07C69/738 , C07C235/74 , C07C235/78 , C07C235/84 , C07C255/40 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/75 , C07D231/12 , C07D231/38 , C07D241/12 , C07D261/08 , C07D277/40 , C07D317/54 , C07D401/12 , C07C39/367
摘要： There is provided a compound of Formula (I): wherein R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , and R 10 , are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO 2 ), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R 9 is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO 2 NR 1 R 2 ; wherein R 1 and R 2 are independently selected from H and hydrocarbyl or (B) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is the group -C(=0)-CR 11 R 12 -R 8 wherein R 8 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (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 or alkenyl-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, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 the enol tautomer thereof wherein R 11 and R 12 are independently selected from H and hydrocarbyl; or (C) at least one of R 3 , R 4 , R 5 , R 6 and R 7 together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a ring containing -C(=O)-; or (D) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, and heteroaryl groups or (E) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from -CN, -C(R 13 )=N-O-alkyl group, - C(R 14 )=N-O-H group, optionally substituted pyrazole, optionally substituted thiazole, optionally substituted oxazole, optionally substituted isoxazole, optionally substituted pyridine, and optionally substituted pyrimidine, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a nitrogen containing ring; wherein R 13 and R 14 are independently selected from H and hydrocarbyl.
摘要翻译：提供式（I）的化合物：其中R 3，R 4，R 5，R 6，/ R 7，R 9和R 10独立地选自-H，-OH，烃基，羟基烃基，氰基（-CN），硝基（-NO 2 N 2）和卤素; 其中环A任选进一步被取代，其中X是键或连接基团，其中（A）（i）R 9选自烷基和卤素基团; 和（ii）R 10选自-OH，羟基烃基和-OSO 2 NR 1 R 2 R 2。其中R 1和R 2独立地选自H和烃基或（B）R 3，R 4中的至少一个 R 5，R 6和R 7是基团-C（= O）-CR 11，其中R 8选自（ⅰ）烷氧基烷基（ⅱ）腈基，（ⅰ） iii）烷基芳基，其中芳基被除了其中芳基被取代的（C 1 -C 6）烯基芳基以外的其它取代基取代（v）烷基杂芳基，其中当杂芳基仅在环中仅包含C和N时，芳基被甲基除外（vi）烯基杂芳基（vii）= NO-烷基或= NOH基（viii）支链烯基（ix）烷基醇基或链烯基（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 - 取代和/或（c）酰胺被至少一个烷基取代烯基杂环基，烷基杂芳基，烯基杂芳基，杂芳基，烷基胺基，烷氧基烷基，烷基芳基，直链或支链烷基，（xi）-CHO，或与另一个R 3 R 4，R 5，R 6和R 7其烯醇互变异构体，其中R 11 R 12和R 12独立地选自H和烃基; 或（C）R 3，R 4，R 5，R 6和R 6中的至少一个，与R 3，R 4，R 5，R 6，R 6，R 5，R 5，和R 7形成含有-C（= O） - 的环; 或（D）R 3，R 4，R 5，R 6和R 6中的至少一个，选自烷基杂环基，烯基杂环基，烷基杂芳基，烯基杂芳基和杂芳基，或（E）R 3，R 4中的至少一个， R 5，R 6，R 7和R 7选自-CN，-C（R 13））= NO-烷基，-C（R 14）= NOH基，任选取代的吡唑，任选取代的噻唑，任选取代的恶唑，任选取代的异恶唑，任选取代的吡啶和任选取代的嘧啶，或与R 3，R 4，R 5，R 6和R 7中的另一个一起， / SUB>形成含氮环; 其中R 13和R 14独立地选自H和烃基。

9. 发明申请

WO2007003934A3 17BETA-HYDR0XYSTER0ID DEHYDROGENASE TYPE 3 (17BETA-HSD3 ) INHIBITORS 审中-公开
公开(公告)号：WO2007003934A3
公开(公告)日：2007-01-11
申请号：PCT/GB2006/002465
申请日：2006-07-03
申请人： STERIX LIMITED , VICKER, Nigel , DAY, Joanna, Mary , BAILEY, Helen, Victoria , HEATON, Wesley , GONZALEZ, Ana, Maria, Ramos , SHARLAND, Christopher, Mark , REED, Michael, John , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
发明人： VICKER, Nigel , DAY, Joanna, Mary , BAILEY, Helen, Victoria , HEATON, Wesley , GONZALEZ, Ana, Maria, Ramos , SHARLAND, Christopher, Mark , REED, Michael, John , PUROHIT, Atul , POTTER, Barry, Victor, Lloyd
IPC分类号： C07C211/00 , C07C211/58 , C07D211/58 , C07D211/62 , C07D405/06 , C07D223/12 , C07D209/20 , C07D401/12 , C07D451/04 , C07D215/44 , C07D223/16 , C07D211/96 , C07D409/12 , C07D409/06 , C07D401/14 , C07D215/38 , C07D405/12 , C07C233/38 , C07C237/22 , A61P5/24 , A61K31/435 , A61K31/495
摘要： There is provided a compound having Formula (I). In particular the present invention provides compounds capable of inhibiting 17β-hydroxysteroid dehydrogenase Type 3 (17β-HSD3).

10. 发明申请

WO2005118560A1 PHENYL-SULFAMATES AS AROMATASE INHIBITORS 审中-公开
标题翻译：苯磺酰胺作为芳香酶抑制剂
公开(公告)号：WO2005118560A1
公开(公告)日：2005-12-15
申请号：PCT/GB2005/002194
申请日：2005-06-03
申请人： STERIX LIMITED , WOO, Lok, Wai, Lawrence , JACKSON, Toby , BUBERT, Christian , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
发明人： WOO, Lok, Wai, Lawrence , JACKSON, Toby , BUBERT, Christian , PUROHIT, Atul , REED, Michael, John , POTTER, Barry, Victor, Lloyd
IPC分类号： 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; R, is a ring system; R 2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (CN), nitro (-NO 2 ) and halogens; R 3 and R 4 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; R，是一个戒指系统; 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。

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