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公开(公告)号：EP0360609A3
公开(公告)日：1991-05-29
申请号：EP89309634.7
申请日：1989-09-21
Applicant: GILEAD SCIENCES, INC.
Inventor： Froehler, Brian C. , Buhr, Chris A.
IPC: C07H19/10 , C07H19/20 , C07F9/201 , C07F9/202 , C07F9/203 , C07F9/204 , C07F9/205 , C07F9/58 , A61K31/70 , A61K31/66
Abstract: Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses. A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.
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公开(公告)号：EP0360609A2
公开(公告)日：1990-03-28
申请号：EP89309634.7
申请日：1989-09-21
Applicant: GILEAD SCIENCES, INC.
Inventor： Froehler, Brian C. , Buhr, Chris A.
IPC: C07H19/10 , C07H19/20 , C07F9/201 , C07F9/202 , C07F9/203 , C07F9/204 , C07F9/205 , C07F9/58 , A61K31/70 , A61K31/66
Abstract: Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses. A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.
Abstract translation: 提供了特别用于在寡核苷酸或寡核苷酸中形成核苷酸间和核苷间连接的新型氢 - 二硫代磷酸酯组合物。 通过使用氢化二硫代膦酸酯组合物制备的寡核苷酸及其类似物可以在治疗上用作抗病毒剂和抗癌剂并且可以具有其他治疗或诊断用途。 提供了制备膦二硫代磷酸氢盐的方法以及将其转化为活化的中间体以在磷原子上取代的方法。
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