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    • 1. 发明授权
      EP1709056B1 PHOSPHORAMIDATE DERIVATIVES 有权
    • PHOSPHORAMIDATE DERIVATIVES
    • 磷酰胺衍生物
    • EP1709056B1
    • 2009-06-17
    • EP05701927.5
    • 2005-01-18
    • University College Cardiff Consultants Limited
    • MCGUIGAN, Christopher , CARANGIO, Antonella , CATERSON, Bruce , HUGHES, Clare, Elizabeth , CURTIS, Clare Louise
    • C07H11/04 , A61K31/7024 , A61P29/00
    • C07H11/04 , Y02P20/55
    • The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I)wherein: X comprises a monosaccharide group comprising the structure (II) or (III),8Formula (II) , (III) B and B are independently selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R is selected from the group consisting of -H, protecting groups and monovalent hydrocarbon radicals; R and R are independently selected from the group consisting of -H and monovalent hydrocarbon radicals, or R2 and R3 together form an alkylene or heteroalkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system; R is selected from the group consisting of -H and monovalent hydrocarbon radicals; R -R are independently selected from the group consisting of -H, -OH, N3, halogen, -SH,-OR , -SR , -NHR , -NR 2 and group Formula (1) wherein B" is selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R -R are independently selected and are as defined above, wherein R and R are independently selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , and wherein R is selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , wherein R is selected from the group consisting of -H and monovalent hydrocarbon radicals; or a pharmaceutically acceptable derivative or metabolite of a compound of formula (I). The present invention also provides processes for the production of (I) and uses thereof.
    • 本发明提供了包含结构（I）式（I）的氨基磷酸酯化合物，其中：X包含包含结构（II）或（III）的单糖基团，式（II），（III）B和B独立地选自 由-O - ， - CH 2 - 和键组成的基团，优选-O-; R 1选自-H，保护基和单价烃基; R 2和R 3独立地选自-H和一价烃基，或者R 2和R 3一起形成亚烷基或亚杂烷基链，从而与它们所连接的C原子一起提供 ，一个循环系统; R 4选自-H和一价烃基; R 5 -R 12独立地选自-H，-OH，N 3，卤素，-SH，-OR 13，-SR 13'，-NHR 14， - NR 14 2和式（1）的基团，其中B“选自-O - ， - CH 2 - 和键，优选-O-; R 1 -R 4独立地选自 如上所定义，其中R 13和R 13'独立地选自-H，一价烃基，保护基和-C（O）R 15，并且其中R 14和R 14独立地选自-H， 选自-H，一价烃基，保护基和-C（O）R 15，其中R 15选自-H和一价烃基;或药学上可接受的基团 （I）化合物的衍生物或代谢物，本发明还提供了用于生产（I）的方法及其用途。
    • 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
    • 4. 发明授权
      EP0980377B1 ANTI-VIRAL PYRIMIDINE NUCLEOSIDE ANALOGUES 失效
    • ANTI-VIRAL PYRIMIDINE NUCLEOSIDE ANALOGUES
    • 抗病毒嘧啶核苷类似物
    • EP0980377B1
    • 2002-07-31
    • EP98919313.1
    • 1998-04-27
    • University College Cardiff Consultants Limited , REGA FOUNDATION
    • MCGUIGAN, Christopher , YARNOLD, Christopher , JONES, Garry , BALZARINI, Jan , DE CLERCQ, Erik
    • C07H19/04 , C07H19/06 , A61K31/70 , C07D307/14 , C07D307/04
    • C07H19/06 , C07H19/04
    • A compound having formula (I), wherein R is selected from the group comprising C5 to C20 alkyl, C5 to C20 cycloalkyl, halogens, aryl and alkylaryl; R' is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, alkyl; R'' is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, alkyloxy, aryloxy and aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N- alkyl, (CH2)n where n is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N alkyl; U'' is H and U' is selected from H and CH2T, or U' and U'' are joined so as to form a ring moiety including Q wherein U'-U'' together is respectively selected from the group comprising -CTH-CT'T''- and -CT=CT- and -CT'=CT'-, so as to provide ring moieties selected from the group comprising formula (II) and (III) wherein T is selected from the group comprising OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2 and N3; T' is selected from the group comprising H and halogens and where more than one T' is present they may be the same or different; T'' is selected from the group comprising H and halogens, and W is selected from the group comprising H, a phosphate group and a pharmacologically acceptable salt, derivative or prodrug thereof shows potent anti-viral activity against, for example, varicella zoster virus and cytomegalovirus.
    • 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
    • 5. 发明公开
      EP1709056A1 PHOSPHORAMIDATE DERIVATIVES 有权
    • PHOSPHORAMIDATE DERIVATIVES
    • 磷酰胺衍生物
    • EP1709056A1
    • 2006-10-11
    • EP05701927.5
    • 2005-01-18
    • University College Cardiff Consultants Limited
    • MCGUIGAN, Christopher , CARANGIO, Antonella , CATERSON, Bruce , HUGHES, Clare, Elizabeth , CURTIS, Clare Louise
    • C07H11/04 , A61K31/7024 , A61P29/00
    • C07H11/04 , Y02P20/55
    • The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I)wherein: X comprises a monosaccharide group comprising the structure (II) or (III),8Formula (II) , (III) B and B are independently selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R1 is selected from the group consisting of -H, protecting groups and monovalent hydrocarbon radicals; R2 and R3 are independently selected from the group consisting of -H and monovalent hydrocarbon radicals, or R2 and R3 together form an alkylene or heteroalkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system; R4 is selected from the group consisting of -H and monovalent hydrocarbon radicals; R5-R12 are independently selected from the group consisting of -H, -OH, N3, halogen, -SH,-OR13, -SR13', -NHR14, -NR142 and group Formula (1) wherein B' is selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R1-R4 are independently selected and are as defined above, wherein R13 and R13’ are independently selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R15, and wherein R14 is selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R15, wherein R15 is selected from the group consisting of -H and monovalent hydrocarbon radicals; or a pharmaceutically acceptable derivative or metabolite of a compound of formula (I). The present invention also provides processes for the production of (I) and uses thereof.
    • 本发明提供了包含结构（I）式（I）的氨基磷酸酯化合物，其中：X包含包含结构（II）或（III）的单糖基团，式（II），（III）B和B独立地选自 由-O - ， - CH 2 - 和键组成的基团，优选-O-; R 1选自-H，保护基和单价烃基; R2和R3独立地选自-H和一价烃基，或者R2和R3一起形成亚烷基或亚杂烷基链，从而与它们所连接的C原子一起提供环状系统; R4选自-H和一价烃基; R5-R12独立地选自-H，-OH，N3，卤素，-SH，-OR13，-SR13'，-NHR14，-NR142和基团式（1），其中B'选自基团 由-O - ， - CH 2 - 和一个键组成，优选-O-; R 1 -R 4独立地选自并且如上所定义，其中R 13和R 13'独立地选自-H，一价烃基，保护基和-C（O）R 15，并且其中R 14选自基团 由-H，一价烃基，保护基和-C（O）R 15组成，其中R 15选自-H和一价烃基; 或式（I）化合物的药学上可接受的衍生物或代谢物。 本发明还提供了用于生产（I）的方法及其用途。
    • 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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