Macrolides
    4.
    发明授权
    Macrolides 失效
    大环内酯类

    公开(公告)号:US6124453A

    公开(公告)日:2000-09-26

    申请号:US774114

    申请日:1996-12-24

    摘要: A novel class of macrolides in whichi) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/orii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic .alpha.-amino acid residue; and/oriii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic .alpha.-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula IX ##STR1## is provided having immunosuppressant and antinflammatory properties and protected and ring-open forms thereof.

    摘要翻译: 其中i)位置2至6(包括大环)的新一类大环内酯由哌嗪基羧酸残基提供; 和/或ii)包含大环的位置7至9由芳族α-氨基酸残基提供; 和/或iii)包含大环的位置10至12由脂族α-氨基酸残基提供,优选包含两个或特别是所有三种特征结构特征i),ii)和iii),更特别地, 提供具有免疫抑制剂和抗炎特性及其保护和开环形式的式IX化合物。