公开(公告)号：US08884011B2

公开(公告)日：2014-11-11

申请号：US12514285

申请日：2007-11-08

申请人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

发明人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

IPC分类号： C07F9/02 ,  C07F9/6561

CPC分类号： C07F9/65616

摘要： This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

摘要翻译： 本发明涉及式（I）的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B，X和R 1 -R 3如本文中的类别和子类所定义。 这些化合物可以用作抗病毒前体。 本发明还涉及这些化合物的治疗组合物及其用于制备用于测试和/或预防患者病毒感染的药物的用途。 本发明还提供了制备这些化合物的方法。 特别地，本发明提供了式（II）的H-次膦酸盐前体中间体，其中B是如本文所定义的嘌呤或嘧啶碱基，R 1选自氢原子和甲基，乙基，羟甲基，羟乙基和 C 1-6卤代烷基。

公开(公告)号：US20100099869A1

公开(公告)日：2010-04-22

申请号：US12514285

申请日：2007-11-08

申请人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

发明人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

IPC分类号： C07F9/02

CPC分类号： C07F9/65616

摘要： This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

摘要翻译： 本发明涉及式（I）的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B，X和R 1 -R 3如本文中的类别和子类所定义。 这些化合物可以用作抗病毒前体。 本发明还涉及这些化合物的治疗组合物及其用于制备用于测试和/或预防患者病毒感染的药物的用途。 本发明还提供了制备这些化合物的方法。 特别地，本发明提供了式（II）的H-次膦酸盐前体中间体，其中B是如本文所定义的嘌呤或嘧啶碱基，R 1选自氢原子和甲基，乙基，羟甲基，羟乙基和 C 1-6卤代烷基。