首页> 外国专利> ANTIVRAL NONCYCLIC NUCLEOSIDE AND NONCYCLIC NUCLEOTIDE

ANTIVRAL NONCYCLIC NUCLEOSIDE AND NONCYCLIC NUCLEOTIDE

机译:抗病毒非环核苷酸和非环核苷酸

摘要

Disclosed are compounds of the formula: CHEM wherein B is related to one of the heterocyclic bases found in nucleic acid (DNA, RNA) such as a purine, a substituted purine, a pyrimidine or a substituted pyrimidine wherein the substituents on the purine or pyrimidine are selected from amino, hydroxyl, halogen, thio or alkylthiol wherein the alkyl moiety of the alkylthiol has 1 to 6 carbons; R1 is fluorine, chlorine, hydroxy, alkoxy having 1 to 6 carbons or a phosphate group having the formula: CHEM wherein R4 and R5 are pharmaceutically acceptable cations; R2 and R3 are independently hydroxy, alkoxy having 1 to 6 carbons or a phosphate group having the formula: CHEM wherein R4 and R5 hydrogen or are pharmaceutically acceptable cations; or two of R1, R2 and R3 taken together form a phosphate group having the formula: CHEM wherein R4 is hydrogen or a pharmaceutically acceptable cation. The compounds have antiviral activity. They are particularly effective against the herpes group of viruses with special utility against cytomegalovirus (CMV) and varicella-zoster virus (VZV), and against retroviruses such as HTLV-III.
机译:公开了下式的化合物:其中B与核酸(DNA,RNA)中发现的杂环碱基之一有关,例如嘌呤,取代的嘌呤,嘧啶或取代的嘧啶,其中嘌呤上的取代基嘧啶或嘧啶选自氨基,羟基,卤素,硫代或烷基硫醇,其中烷基硫醇的烷基部分具有1至6个碳; R 1为氟,氯,羟基,具有1-6个碳原子的烷氧基或具有下式的磷酸基:其中R 4和R 5为药学上可接受的阳离子; R 2和R 3独立地是羟基,具有1-6个碳的烷氧基或具有下式的磷酸基:其中R 4和R 5为氢或为药学上可接受的阳离子; R 1,R 2和R 3中的两个或两个一起形成具有下式的磷酸酯基团:其中R 4是氢或药学上可接受的阳离子。该化合物具有抗病毒活性。它们对带状疱疹病毒特别有效,对巨细胞病毒(CMV)和水痘带状疱疹病毒(VZV)以及逆转录病毒(例如HTLV-III)具有特殊用途。

著录项

  • 公开/公告号JPH02264764A

    专利类型

  • 公开/公告日1990-10-29

    原文格式PDF

  • 申请/专利权人 MERCK & CO INC;

    申请/专利号JP19900022331

  • 发明设计人 JIYON HANAA;RICHIYAADO ERU TORUMAN;

    申请日1990-02-02

  • 分类号C07D239/26;A61K31/505;A61K31/52;C07D239/30;C07D239/36;C07D239/38;C07D239/42;C07D239/47;C07D473/18;C07D473/34;C07F9/6561;

  • 国家 JP

  • 入库时间 2022-08-22 06:24:55

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