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    • 3. 发明授权
    • Anti-(retro)viral conjugates of saccharides and acetamidino or guanidino compounds
    • 糖(乙酰脒或胍基)化合物的抗(复)病毒偶联物
    • US06642365B1
    • 2003-11-04
    • US09869437
    • 2001-06-28
    • Aviva LapidotAlexander LitovchickArtem G. Evdokimov
    • Aviva LapidotAlexander LitovchickArtem G. Evdokimov
    • C07H100
    • C07H15/04C07H3/04C07H3/06C07H7/00
    • Conjugates of a saccharide and an acetamidino- or guanidino-compound, of the formula: wherein A is CH3 or NH2; X is a linear or branched C1-C8 alkyl chain optionally containing hydroxy, amino and/or oxo groups; n is an integer from 1 to 6, and Sac is the residue of a mono-or oligo-saccharide, provided that when A is NH2 and X is -(CH2)3—CH(NH2)—C(=O)-, the monosaccharide residue is not substituted at the position 1, and n is an integer from 2 to 6 when Sac is the residue of an oligosaccharide, are useful as antiviral, particularly as antiretroviral, agents, and can be used either alone or together with other compounds used in AIDS treatment such as AZT and/or protease inhibitors, for the treatment of HIV-infection, AIDS and manifestations of AIDS such as Kaposi sarcoma. Particularly preferred compounds are aminoglycoside-arginine conjugates in which the saccharide is a natural aminoglycoside antibiotic such as kanamycin, gentamycin and neomycin that is conjugated to arginine residues.
    • 糖和乙酰胺基 - 或胍基 - 化合物的共轭物,其具有下式:其中A是CH 3或NH 2; X是任选含有羟基,氨基和/或氧代基的直链或支链C 1 -C 8烷基链; n为1至6的整数,Sac为单糖或寡糖的残基,条件是当A为NH 2且X为 - (CH 2)3 -CH(NH 2)-C(= O) - 时, 单糖残基在第1位没有被取代,当Sac是寡糖的残基时,n是2-6的整数,可以作为抗病毒剂,特别是作为抗逆转录病毒剂,可以单独使用或与其他物质一起使用 用于艾滋病治疗的化合物如AZT和/或蛋白酶抑制剂用于治疗艾滋病毒感染,艾滋病和艾滋病的表现如卡波西肉瘤。 特别优选的化合物是氨基糖苷 - 精氨酸缀合物,其中糖类是天然的氨基糖苷类抗生素,例如卡那霉素,庆大霉素和新霉素,其与精氨酸残基缀合。