首页> 外国专利> DESAZAPURINE-NUCLEOSIDE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THE USE THEREOF FORNUCLEIC ACID SEQUENCING AND AS ANTIVIRAL AGENTS

DESAZAPURINE-NUCLEOSIDE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THE USE THEREOF FORNUCLEIC ACID SEQUENCING AND AS ANTIVIRAL AGENTS

机译:十氮杂嘌呤核苷衍生物,其制备方法,包含它们的药物组合物以及其使用的核酸序列化和抗病毒剂的使用

摘要

ABSTRACTDesazapurine-nucleoside derivatives, processes for thepreparation thereof, pharmaceutical compositionscontaining them and the use thereof for nucleic acidsequencing and as antiviral agentsThe present invention provides desazapurine-nucleoside derivatives of the general formula:-(I)wherein X is a nitrogen atom or a methine radical, W isa nitrogen atom or a radical, R1, R2, R3 and R4,which can be the same or different 3 are hydrogen orhalogen atoms, hydroxyl or mercapto groups, lower alkyl,lower alkylthio, lower alkoxy, aralkyl, aralkoxy oraryloxy radicals or amino groups optionally substitutedonce or twice, R5 is a hydrogen atom or a hydroxyl group,R6 and R7 are each hydrogen atoms or one of them is ahalogen atom or a cyano or azido group or an amino groupoptionally substituted once or twice, whereby one ofR6 and R7 can also be a hydroxyl group when X is amethine radical and, in addition, R5 and R7 can togetheralso represent a further valency bond between C-2'and C-3' and is a hydrogen atom or a mono-, di- ortri-phosphate group, as well as the tautomers andsalts thereof and nucleic acids which contain oneor more compounds of general formula (I) asstructural components; these new compounds are use-ful for nucleic acid sequencing and as antiviralagents.
机译:抽象地沙嘌呤-核苷衍生物,用于其制剂,药物组合物含有它们及其在核酸中的用途测序和作为抗病毒药本发明提供脱氮嘌呤-通式的核苷衍生物:(一世)其中X是氮原子或次甲基,W是氮原子或基团R1,R2,R3和R4,可以相同或不同的3是氢或卤素原子,羟基或巯基,低级烷基,低级烷硫基,低级烷氧基,芳烷基,芳烷氧基或任选取代的芳氧基或氨基一次或两次,R5是氢原子或羟基,R6和R7各自为氢原子或其中一个为a卤素原子或氰基或叠氮基或氨基可选取代一次或两次,其中之一当X为a时,R6和R7也可以为羟基次甲基,另外,R5和R7可以一起也代表C-2'之间的另一个价键和C-3',并且是氢原子或单,二或三磷酸基团,以及互变异构体和其盐和含有一种的核酸或更多个通式(I)的化合物为结构组件;这些新化合物的用途是可用于核酸测序和抗病毒代理商。

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