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1. 发明授权

EP1709056B1 PHOSPHORAMIDATE DERIVATIVES 有权
标题翻译：磷酰胺衍生物
公开(公告)号：EP1709056B1
公开(公告)日：2009-06-17
申请号：EP05701927.5
申请日：2005-01-18
申请人： University College Cardiff Consultants Limited
发明人： MCGUIGAN, Christopher , CARANGIO, Antonella , CATERSON, Bruce , HUGHES, Clare, Elizabeth , CURTIS, Clare Louise
IPC分类号： C07H11/04 , A61K31/7024 , A61P29/00
CPC分类号： C07H11/04 , Y02P20/55
摘要： 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.
摘要翻译：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。

2. 发明公开

EP1709056A1 PHOSPHORAMIDATE DERIVATIVES 有权
标题翻译：磷酰胺衍生物
公开(公告)号：EP1709056A1
公开(公告)日：2006-10-11
申请号：EP05701927.5
申请日：2005-01-18
申请人： University College Cardiff Consultants Limited
发明人： MCGUIGAN, Christopher , CARANGIO, Antonella , CATERSON, Bruce , HUGHES, Clare, Elizabeth , CURTIS, Clare Louise
IPC分类号： C07H11/04 , A61K31/7024 , A61P29/00
CPC分类号： C07H11/04 , Y02P20/55
摘要： 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.
摘要翻译：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。

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