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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。

3. 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

4. 发明申请

WO2008065428A3 STEROID SULPHATASE INHIBITORS FOR TREATING HORMONE DEPENDENT CANCER 审中-公开
标题翻译：用于治疗依赖于雄激素的癌症的甾体硫酸酯酶抑制剂
公开(公告)号：WO2008065428A3
公开(公告)日：2008-07-31
申请号：PCT/GB2007004612
申请日：2007-11-30
申请人： STERIX LTD , REED MICHAEL JOHN , PUROHIT ATUL , FOSTER PAUL ALEXANDER , NEWMAN SIMON PAUL , WOO LOK WAI LAWRENCE , POTTER BARRY VICTOR LLOYD
发明人： REED MICHAEL JOHN , PUROHIT ATUL , FOSTER PAUL ALEXANDER , NEWMAN SIMON PAUL , WOO LOK WAI LAWRENCE , POTTER BARRY VICTOR LLOYD
IPC分类号： A61K31/37 , A61P35/00
CPC分类号： A61K31/37
摘要： There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for the treatment of cancer, wherein the cancer is of a type in which the cancer cells overexpress aromatase enzyme.
摘要翻译：提供能够抑制类固醇硫酸酯酶（E.C.3.1.6.2）的化合物在制备用于治疗癌症的药物中的用途，其中癌症是癌细胞过度表达芳香酶的类型。

5. 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。

6. 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）。

7. 发明申请

WO2005115996B1 SULFAMIC ACID ESTER COMPOUNDS USEFUL IN THE INHIBITION OF SEROID SULPHATASE ACTIVITY AND AROMATASE ACTIVITY 审中-公开
标题翻译：用于抑制血清型硫酸酯酶活性和芳香酶活性的硫酸酯化合物
公开(公告)号：WO2005115996B1
公开(公告)日：2006-02-02
申请号：PCT/GB2005001985
申请日：2005-05-19
申请人： STERIX LTD , POTTER BARRY VICTOR LLOYD , REED MICHAEL JOHN , WOO LOK WAI LAWRENCE , PUROHIT ATUL , BURBERT CHRISTIAN , WOOD MICHAEL PAUL , SUTCLIFFE OLIVER BROOK
发明人： POTTER BARRY VICTOR LLOYD , REED MICHAEL JOHN , WOO LOK WAI LAWRENCE , PUROHIT ATUL , BURBERT CHRISTIAN , WOOD MICHAEL PAUL , SUTCLIFFE OLIVER BROOK
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08
摘要： There is provided a compound 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 R 4 and R 5 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.
摘要翻译：提供式（III）或式（IV）的化合物，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R 4和R 5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，其中所述或每个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。

8. 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。

9. 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。

10. 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。

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