首页> 外国专利> NUCLEOSIDE AND NUCLEOTIDE ANALOGUES BEARING A QUATERNARY ALL-CARBON STEREOGENIC CENTER AT THE 2' POSITION AND METHODS OF USE AS A CARDIOPROTECTIVE AGENT

NUCLEOSIDE AND NUCLEOTIDE ANALOGUES BEARING A QUATERNARY ALL-CARBON STEREOGENIC CENTER AT THE 2' POSITION AND METHODS OF USE AS A CARDIOPROTECTIVE AGENT

机译:处于2'位置的全碳立体异构中心的核苷和核苷类似物以及用作心脏保护剂的方法

摘要

Nucleoside analogues that can be used as anticancer or antiviral agents are presented. These compounds are nucleoside and/or nucleotide prodrugs. In particular, the subject matter relates to nucleoside analogues comprising a tetrahydrofuranyl, or tetrahydrothienyl moiety which: have a quaternary stereogenic all-carbon center at the 3′ position and bear a phosphoryl group at either one of, or both of positions C5′ and/or C3′; have a quaternary stereogenic all-carbon center at one of the 3′ position, 2′ position, or no quaternary stereogenic center at all, and bear a β-blocked lipoate derivative attached through an amide bond to the primary amine of the nucleobase; or have a quaternary stereogenic all-carbon center at the 2′ position and bear a phosphorylated prodrug at the C5′-position and a β-blocked lipoate derivative attached through an amide bond to the primary amine of the nucleobase.
机译:提出了可用作抗癌剂或抗病毒剂的核苷类似物。这些化合物是核苷和/或核苷酸前药。特别地,该主题涉及包含四氢呋喃基或四氢噻吩基部分的核苷类似物,所述四氢呋喃基或四氢噻吩基部分:在3'位置具有季立体立体全碳中心,并且在C5'和/或位置C5'中的一个或两个均带有磷酸基团。或C3';在3'位置,2'位置之一上具有一个立体立体异构全碳中心,或根本没有一个第四立体立体异构中心,并且带有一个通过酰胺键连接到核碱基的伯胺上的β嵌段硫辛酸酯衍生物;或在2'位具有一个立体立体异构全碳中心,并在C5'位带有一个磷酸化的前药,以及一个通过酰胺键连接到核碱基的伯胺上的β嵌段硫辛酸酯衍生物。

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