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    • 1. 发明申请
      WO2011023989A1 AROMATASE INHIBITOR 审中-公开
    • AROMATASE INHIBITOR
    • 芳香酶抑制剂
    • WO2011023989A1
    • 2011-03-03
    • PCT/GB2010/051391
    • 2010-08-23
    • STERIX LIMITED , WOO, Lok Wai Lawrence , BUBERT, Christian , WOOD, Paul Michael , PUTEY, Aurélien , PUROHIT, Atul , POTTER, Barry Victor Lloyd
    • WOO, Lok Wai Lawrence , BUBERT, Christian , WOOD, Paul Michael , PUTEY, Aurélien , PUROHIT, Atul , POTTER, Barry Victor Lloyd
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K319/4196 , A61K31/496 , A61K31/5355 , A61K31/55 , A61P35/00
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
    • There is provided a compound of formula (I) wherein Z is selected from N and CR 22 , wherein R 22 is H or a bond with D, wherein D is selected from a bond, C=O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (=0), an ether (-0-) or thioether (-S-) link, wherein R 1 is selected from :triazolyl, imidazolyl, pyrimidinyl radical wherein each of R 2 to R 6 is independently selected from -H, NO 2 , halo, -CN, -N[(C=O) 0-1 R 12 ][(C=O) 0-1 R 13 ] and -(CH 2 ) 0-1 R 14 , or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R 2 to R 6 is -CN, wherein (i) at least one of R 2 to R 6 is -(CH 2 ) 0-1 R 14 , or (ii) at least one of R 2 to R 6 is -N[(C=O) 0-1 , R 12 ][(C=O) 0-1 R 13 ], or (iii) at least two adjacent groups of R 2 to R 6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R 2 to R 6 is -(CH 2 ) 0-1 O-R' 14 , wherein R 12 and R 13 are independently selected from H, linear or branched hydrocarbon groups having a carbon chain of from 1 to 10 carbon atoms, or together with the atoms to which they are attached, may form a mono or bicyclic ring having from 5 to14 ring members wherein R 14 is selected from: aliphatic ring systems; unsubstituted or substituted monocyclic aliphatic heterocycles; unsubstituted or substituted heteroaryl radical, and unsubstituted or substituted phenyl group; the group of formula (a) wherein t is 1 or 2, wherein R' 14 is a unsubstituted or substituted phenyl group, wherein each of R 7 to R 11 is independently selected from -H, NO 2 , halo, -O-(C 1 -C 6 )haloalkyl, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )alkyl, -CN, -OH, -OPh, -OBn, -Ph, -OSO 2 NR 15 R 16 , -SO 2 R 26 , -SO 2 NR 27 NR 28 , -O-(C 1 C 6 )alkyl, -(C=O) 0-1 NR 29 R 30 and -CO(O) 0-1 R 31 ; wherein R 15 and R 16 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 alkenyi optionally contain one or more hetero atoms or groups wherein each of R 26 to R 31 is independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyi or cycloalky! or alkenyl optionally contain one or more hetero atoms or groups, or any pharmaceutically acceptable salts thereof.
    • 提供式（I）化合物，其中Z选自N和CR 22，其中R 22是H或与D的键，其中D选自键，C = O和具有碳的直链或支链烃基 具有1至6个碳原子的链，其中所述碳链任选地含有氧基（= O），醚（-O-）或硫醚（-S-）连接，其中R 1选自：三唑基，咪唑基，嘧啶基 其中R2至R6各自独立地选自-H，NO2，卤素，-CN，-N [（C = O）0-1R12] [（C = O）0-1R13]和 - （CH2） 1R14或R 2至R 6的两个相邻基团与它们连接的碳原子一起形成环，其中R 2至R 6中的至少一个为-CN，其中（i）R 2至R 6中的至少一个为 - （CH 2）0-1R 14，或（ii）R 2至R 6中的至少一个为-N [（C = O）0-1，R 12] [（C = O）0-1R 13]，或（iii） R 2至R 6的至少两个相邻基团与它们所连接的碳原子一起形成环，或（iv）R 2至R 6中的至少一个为 - （CH 2）0-1R-14， ein R 12和R 13独立地选自H，具有1至10个碳原子的碳链的直链或支链烃基，或与它们所连接的原子一起可以形成具有5至14个环的单环或双环 其中R 14选自：脂族环系; 未取代或取代的单环脂族杂环; 未取代或取代的杂芳基，以及未取代或取代的苯基; 式（a）的基团，其中t为1或2，其中R'14为未取代或取代的苯基，其中R7至R11各自独立地选自-H，NO2，卤素，-O-（C1-C6 ）卤代烷基，（C1-C6）卤代烷基，（C1-C6）烷基，-CN，-OH，-OPh，-OBn，-Ph，-OSO2NR15R16，-SO2R26，-SO2NR27NR28，-O-（C1C6）烷基， （C = O）0-1NR29R30和-CO（O）0-1R31; 其中R 15和R 16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任选地含有一个或多个杂原子或基团， R 26至R 31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，其中每个烷基或环烷基 或烯基任选地含有一个或多个杂原子或基团，或其任何药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明公开
      EP2470512A1 AROMATASE INHIBITOR 有权
    • AROMATASE INHIBITOR
    • AROMATASEHEMMER
    • EP2470512A1
    • 2012-07-04
    • EP10750154.6
    • 2010-08-23
    • Sterix Limited
    • WOO, Lok Wai Lawrence , BUBERT, Christian , WOOD, Paul Michael , PUTEY, Aurélien , PUROHIT, Atul , POTTER, Barry Victor Lloyd
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/496 , A61K31/5355 , A61K31/55 , A61P35/00
    • C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
    • There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C═O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (═O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C═O)0-1R12][(C═O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C═O)0-1R12][(C═O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R′14, wherein R12 and R13 are independently selected from H, linear or branched hydrocarbon groups having a carbon chain of from 1 to 10 carbon atoms, or together with the atoms to which they are attached, may form a mono or bicyclic ring having from 5 to 14 ring members wherein R14 is selected from: aliphatic ring systems unsubstituted or substituted monocyclic aliphatic heterocycles; unsubstituted or substituted heteroaryl radical, and unsubstituted or substituted phenyl group; the group of formula wherein t is 1 or 2 wherein R′14 is a unsubstituted or substituted phenyl group; wherein each of R7 to R11 is independently selected from —H, NO2, halo, —O—(C1-C6)haloalkyl, (C1-C6)haloalkyl, (C1-C6)alkyl, —CN, —OH, —OPh, —OBn, -Ph, —OSO2NR15R16, —SO2R26, —SO2NR27R28, —O—(C1-C6)alkyl, —(C═O)0-1NR29R30 and —CO(O)0-1R31; wherein R15 and R16 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 optionally contain one or more hetero atoms or groups wherein each of R26 to R31 is 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 optionally contain one or more hetero atoms or groups; or any pharmaceutically acceptable salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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