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    • 2. 发明授权
    • Cytotoxic tris(oxazole)-containing macrolides
    • 含有细菌毒性的三(恶唑)大环内酯类
    • US06391900B1
    • 2002-05-21
    • US09601146
    • 2001-01-12
    • Tatsuo HigaDolores Garcia GravalosJose Luis Fernandez Puentes
    • Tatsuo HigaDolores Garcia GravalosJose Luis Fernandez Puentes
    • A61P3500
    • C07D498/22
    • The present invention discloses new cytotoxic tris(oxazole)-containing macrolides having the formula: wherein X represents a lower alkyl; R1 and R2 represent hydrogen or lower alkyl; R3a represents hydrogen, and R3b represents or R3a and R3b together represent oxygen; R4 represents hydrogen, lower alkoxy or lower alkyl; R5 represents hydrogen, carbamoyl, or lower alkanoyl; R6a represents hydrogen, and R6b represents hydroxy, or R6a and R6b together represent oxygen; R7 represents hydrogen, lower alkyl, or hydroxymethyl; R8 represents lower alkoxy or lower alkyl; Y1 represents hydrogen or methyl, and y2 represents hydrogen, or Y1 and Y2 together represent a double bond. Also disclose are methods for treating mammals using the macrolides and pharmaceutical preparations including the macrolides.
    • 本发明公开了具有下式的新的具有细胞毒性的三(恶唑)的大环内酯类:其中X代表低级烷基; R1和R2表示氢或低级烷基; R3a表示氢,R3b表示R3a和R3b表示氧; R4代表氢,低级烷氧基或低级烷基; R5表示氢,氨基甲酰基或低级烷酰基; R6a表示氢,R6b表示羟基,R6a和R6b表示氧; R7表示氢,低级烷基或羟甲基; R8表示低级烷氧基或低级烷基; Y1表示氢或甲基,y2表示氢,Y1或Y2表示双键。 还公开了使用大环内酯类和包括大环内酯类药物制剂治疗哺乳动物的方法。