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    • 9. 发明公开
    • Macrolide compounds
    • 大环内酯化合物
    • EP0242052A2
    • 1987-10-21
    • EP87302097.8
    • 1987-03-11
    • AMERICAN CYANAMID COMPANY
    • Rudd, Brian A. M.Fletton, Richard A.Ward, John B.Noble, DavidPorter, NeilLawrence, Gordon C.Noble, Hazel M.
    • C07D493/22C07D493/20A61K31/365C12P17/08A01N43/90
    • C07H19/01A01N43/90C12P17/08C12P19/445C12R1/465
    • Compounds of the formula
      [wherein

      R 1 represents a methyl group;
      R 2 represents a methyl group
      R 3 represents a methyl, ethyl or isopropyl group; and
      -A- represents a ring which is either

      (where R 4 is a hydroxy or methoxy group and R 5 is a hydrogen atom or R 4 and R 5 together with the carbon atom to which they are attached represent a group C=0); or when -A-represents ring (ii) wherein R 4 and R 5 together with the carbon atom to which they are attached represent a group C=0 then R 2 may also represent an aldehydo group;
      or R 2 represents a hydroxymethyl group and -A- represents
      (where R 6 represents a hydrogen atom or a hydroxy group);

      (where R 7 is a hydroxy or methoxy group and Z represents either a group CHOH or a group C=0);
      or R 1 represents a hydrogen atom and

      (where R 8 is a hydroxy or methoxy group); with the provisos that when R 2 represents a methyl group and R 4 represents a methoxy group then R 3 cannot represents a methyl or isopropyl group and when R 2 represents a hydroxymethyl group and R 6 represents a hydroxy group then R 3 cannot represent a methyl group.

      Compounds of the invention have antiparasitic activity.
    • 式[其中R1代表甲基; R2代表甲基,R3代表甲基,乙基或异丙基; (其中R 4为羟基或甲氧基且R 5为氢原子或者R 4和R 5与它们所连接的碳原子一起表示C = O的基团)。 或者当-A-代表环(ii),其中R 4和R 5与它们所连接的碳原子一起代表基团C = O时,则R 2也可代表醛基; 或者R 2表示羟甲基,-A-表示(其中R 6表示氢原子或羟基)。 (其中R7是羟基或甲氧基,Z表示基团CHOH或C = O); 或者R1代表氢原子和(其中R8是羟基或甲氧基)。 条件是当R 2代表甲基且R 4代表甲氧基时,则R 3不能代表甲基或异丙基,并且当R 2代表羟甲基并且R 6代表羟基时,则R 3不能代表甲基。 本发明的化合物具有抗寄生虫活性。