专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2007003934A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2007003934A2
公开(公告)日：2007-01-11
申请号：PCT/GB2006002465
申请日：2006-07-03
申请人： STERIX LTD , 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 , C07C233/36 , C07C237/22 , 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
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 R 1 , R 2 , R 4 , R 5 , R 6 and R 7 are independently selected from (a) H, (b) R 17 , -OC(R 17 ) 3 , -OCH(R 17 ) 2 , -(OCH 2 R) 17 , -C(R 17 ) 3 , -CH(R 17 ) 2 , or -CH 2 R 17 wherein R 17 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) -SO 2 -alkyl; and (n) -N(R 11 )C(O)R 13 ; wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C 1-6 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) 2 NR 8 , C=ONR 9 , NR 10 , wherein R 8 , R 9 and R 10 are independently selected from H and hydrocarbyl, wherein n and p are independently selected from O and 1 ; Y is (R 11 ) 1-3 wherein each R 11 is independently selected from NR 12 , CR 13 R 14 , S(=O) 2 and C=O, wherein R 12 , R 13 and R 14 are independently selected from H and 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 -R 15 -NR 16 - group wherein R 15 is an optionally substituted C 1-6 alkyl chain and R 16 is selected from H and hydrocarbyl; and R 3 is selected from Formula (A).
摘要翻译：提供了具有式（I）的化合物，其中R 1，R 2，R 4，R 5， R a，R 6和R 7独立地选自（a）H，（b）R 17，-OC（R a 3， - OCH（R 17）2 - ， - （OCH 2 R 2）） - （R 17）3 - ， - （R 17）2 - ， - （R 17）或者其中R 17是卤素;或者其中R 17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 11）C（O）R 13; 其中（d）（e）（f）（h）和（i）的任选取代基选自：C 1-6烷基，卤素，氰基，硝基，卤代烷基，羟基，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; 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，并且任选地与另外的环稠合; X是选自O，S，S = O，S（= O）2，C = O，S（= O）2 NR 8，C 其中R 8，R 9和R 10各自独立地为氢，独立地选自H和烃基，其中n和p独立地选自O和1; Y是（R 11-11）1-3，其中每个R 11独立地选自NR 12，CR 11， S（= O）2和C = O，其中R 12，R 12， 13和R 14独立地选自H和烃基; 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; 其中R 15是任选取代的C 1-6烷基，和（ⅱ）R 15是-NR 16 - 烷基链和R 16选自H和烃基; 和R 3选自式（A）。

2. 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。

3. 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。

4. 发明申请

WO02072084A2 GLYCYRRHETINIC ACID DERIVATIVES, PROGESTERONE AND PROGESTERONE DERIVATIVES AND THEIR USE FOR THE MANUFACTURE OF A MEDICAMENT TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE ACTIVITY 审中-公开
标题翻译：甘氨酸衍生物，前列腺素和孕酮衍生物及其用于制造药物以抑制11BETA-羟基脱氢酶脱氢酶活性的用途
公开(公告)号：WO02072084A2
公开(公告)日：2002-09-19
申请号：PCT/GB0201060
申请日：2002-03-07
申请人： STERIX LTD , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN , VICKER NIGEL
发明人： POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN , VICKER NIGEL
IPC分类号： A61K31/19 , A61K31/57 , A61P5/38 , A61P5/44 , A61P5/46 , C07D213/40 , C07D295/13 , C07D295/182 , C07J7/00 , C07J9/00 , C07J51/00 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/4402 , A61K31/5375 , A61K31/5685 , C07C62/32 , C07C62/34 , C07C62/38 , C07C69/753 , C07C235/40
CPC分类号： C07D213/40 , A61K31/19 , A61K31/57 , C07D295/13 , C07D295/182 , C07J7/00 , C07J9/00 , C07J51/00
摘要： The present invention provides use of a compound in the manufacture of a medicament to inhibit 11 beta -HSD activity, wherein the compound is selected from glycyrrhetinic acid derivatives, progesterone and progesterone derivatives.
摘要翻译：本发明提供化合物在制备抑制11β-HSD活性的药物中的用途，其中该化合物选自甘草次酸衍生物，孕酮和孕酮衍生物。

5. 发明申请

WO02072084A8 GLYCYRRHETINIC ACID DERIVATIVES, PROGESTERONE AND PROGESTERONE DERIVATIVES AND THEIR USE FOR THE MANUFACTURE OF A MEDICAMENT TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE ACTIVITY 审中-公开
标题翻译：甘氨酸衍生物，前列腺素和孕酮衍生物及其用于制造药物以抑制11BETA-羟基脱氢酶脱氢酶活性的用途
公开(公告)号：WO02072084A8
公开(公告)日：2003-01-09
申请号：PCT/GB0201060
申请日：2002-03-07
申请人： STERIX LTD , POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN , VICKER NIGEL
发明人： POTTER BARRY VICTOR LLOYD , PUROHIT ATUL , REED MICHAEL JOHN , VICKER NIGEL
IPC分类号： A61K31/19 , A61K31/57 , A61P5/38 , A61P5/44 , A61P5/46 , C07D213/40 , C07D295/13 , C07D295/182 , C07J7/00 , C07J9/00 , C07J51/00 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/4402 , A61K31/4453 , A61K31/5375 , A61K31/5685 , A61K31/575 , C07C62/32 , C07C62/34 , C07C62/38 , C07C69/753 , C07C69/757 , C07C235/40
CPC分类号： C07D213/40 , A61K31/19 , A61K31/57 , C07D295/13 , C07D295/182 , C07J7/00 , C07J9/00 , C07J51/00
摘要： The present invention provides use of a compound in the manufacture of a medicament to inhibit 11 beta -HSD activity, wherein the compound is selected from glycyrrhetinic acid derivatives, progesterone and progesterone derivatives.
摘要翻译：本发明提供化合物在制备抑制11β-HSD活性的药物中的用途，其中该化合物选自甘草次酸衍生物，孕酮和孕酮衍生物。

6. 发明申请

WO2004085457A3 17BETA-HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： 17BETA-HYDROXYSTERIDID DEHYDROGENASE抑制剂
公开(公告)号：WO2004085457A3
公开(公告)日：2005-02-03
申请号：PCT/GB2004001234
申请日：2004-03-22
申请人： STERIX LTD , VICKER NIGEL , LAWRENCE HARSHANI RITHMA RUCHI , ALLAN GILLIAN MARGARET , BUBERT CHRISTIAN , FISCHER DELPHINE SOPHIE MARION , PUROHIT ALAN , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
发明人： VICKER NIGEL , LAWRENCE HARSHANI RITHMA RUCHI , ALLAN GILLIAN MARGARET , BUBERT CHRISTIAN , FISCHER DELPHINE SOPHIE MARION , PUROHIT ALAN , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
IPC分类号： A61K31/56 , A61K31/566 , C07J20060101 , C07J41/00 , C07J71/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula (I) wherein (I) R is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R 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) alkyiheteroaryl 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 - CH2- or -CH2CH2-, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of a I kyl heterocycle group, al ke nyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO so that R, together with R3 provide the enol tautomer (a); OR R1 together with R form (xii) a pyrazole wherein (a) R is =N-0-alkyl or =N-0-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 -0-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R 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 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，并且其中R 2能够形成氢键（iii ）烷基芳基，其中芳基被除了其中芳基被取代的（C）芳基取代的（C 1 -C 6）烯基芳基以外的其它芳基取代;（ⅴ）芳基杂芳基，其中当杂芳基仅在环中仅包含C和N时，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）烷基的烷基酰胺是-CH 2 - 或-CH 2 CH 2 - ，（b）酰胺是二取代的，和/或（c）酰胺被I烷基杂环基，烯基杂环基，烷基杂芳基中的至少一个取代，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 so t 与R 3一起提供烯醇互变异构体（a）; 或R 1与R 3一起形成（xii）吡唑，其中（a）R 4是= N-O-烷基或= N-O-H基，（b）吡唑被烷基 - OH基，烷基酯基，烷氧基烷基。基团，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（b）的化合物; （II）R 2选自能够形成氢键的基团，氨基磺酸酯基团，膦酸酯基团，硫代膦酸酯基团，磺酸酯基团和磺酰胺基团; 和（III）R 3选自-OH，= O或-C（= O） - 模拟物。

7. 发明申请

WO2009106817A3 1 IBETA- HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： 1 IBETA-羟基甾体脱氢酶抑制剂
公开(公告)号：WO2009106817A3
公开(公告)日：2009-12-03
申请号：PCT/GB2009000518
申请日：2009-02-25
申请人： STERIX LTD , VICKER NIGEL , SU XIANGDONG , PRADAUX-CAGGIANO FABIENNE , POTTER BARRY VICTOR LLOYD
发明人： VICKER NIGEL , SU XIANGDONG , PRADAUX-CAGGIANO FABIENNE , POTTER BARRY VICTOR LLOYD
IPC分类号： C07D213/30 , C07D213/32 , C07D213/34 , C07D213/50 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/89 , C07D233/84 , C07D235/28 , C07D249/12
CPC分类号： C07D233/84 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/50 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/89 , C07D235/28 , C07D249/12 , C07D257/04 , C07D285/125 , C07D285/135 , C07D405/04 , C07D409/04
摘要： There is provided a compound of formula R1-CO-X-Y-Z-R2 wherein X and Z are each optional groups independently selected from saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH=CH, CH2CH2 or O; R1 is selected from the following groups (A) wherein - - - denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulphur; and wherein (i) when R1 is group (B) and -CO-X-Y-Z- is CO-CH2-SO, CO-CH2-S, or CO-CH2-SO2, R2 is other than group (C) and; (ii) when R1 is group (D) and -CO-X-Y-Z- is -CO-CH2-O-, R2 is other than group (E).
摘要翻译：提供式R1-CO-X-Y-Z-R2的化合物，其中X和Z各自是任选的独立地选自具有1至3个碳原子的饱和或不饱和碳链的基团; Y是SO，S，SO 2，CH = CH，CH 2 CH 2或O; R1选自以下组（A），其中 - - - 表示连接点; R2是包含任选取代的5或6元环的杂芳基，该环仅含有碳和至少一个氮，或仅含有碳，以及至少两个氮和至少一个硫; 并且其中（i）当R 1为基团（B）且-CO-X-Y-Z-为CO-CH 2 SO，CO-CH 2 -S或CO-CH 2 -SO 2时，R 2为（C）（ⅱ）当R 1为基团（D）且-CO-X-Y-Z-为-CO-CH 2 -O-时，R 2为（E）基团。

8. 发明专利

BRPI0907706A2 Composto, uso do dito composto e composição farmacéutica compreendendo o dito composto 未知
公开(公告)号：BRPI0907706A2
公开(公告)日：2015-07-21
申请号：BRPI0907706
申请日：2009-02-25
申请人： STERIX LTD
发明人： VICKER NIGEL , SU XIANGDONG , PRADAUX-CAGGIANO FABIENNE , POTTER BARRY VICTOR LLOYD
IPC分类号： C07D213/30 , C07D213/32 , C07D213/34 , C07D213/50 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/89 , C07D233/84 , C07D235/28 , C07D249/12

9. 发明专利

CA2613226C INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 3 未知
公开(公告)号：CA2613226C
公开(公告)日：2014-10-14
申请号：CA2613226
申请日：2006-07-03
申请人： STERIX LTD
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： C07D211/58 , A61K31/445 , A61K31/4468 , C07C233/36 , C07C237/22 , C07D209/20 , C07D211/56 , 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, R4, R5, R6 and R7 are independently selected from (a) H, (b) R17, -OC(R17)3, -OCH(R17)2, -(OCH2R)17, -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 O 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 H and 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).

10. 发明专利

BRPI0408697A 未知
公开(公告)号：BRPI0408697A
公开(公告)日：2006-03-28
申请号：BRPI0408697
申请日：2004-03-22
申请人： STERIX LTD
发明人： VICKER NIGEL , LAWRENCE HARSHANI RITHMA RUCHI , ALLAN GILLIAN MARGARET , BUBERT CHRISTIAN , FISHER DELPHINE SOPHIE MARION , PUROHIT ALAN , REED MICHAEL JOHN , POTTER BARRY VICTOR LLOYD
IPC分类号： A61K31/56 , A61K31/566 , C07J20060101 , C07J41/00 , C07J71/00
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

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式