| 摘要 |
The present invention relates to water soluble, camptothecin derivatives of formula (I), <IMAGE> (I) wherein: 1) R1 and R2 represent independently, hydrogen, lower alkyl, C3-7)cycloalkyl, C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R1 represents hydrogen, lower alkyl, C3-7)cycloalkyl, C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R2 represents -COR3, wherein: R3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C3-7)cycloalkyl, C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; or iii) R1 and R2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) <IMAGE> (IA) wherein: Y represents O, S, SO, SO2, CH2 or NR4 wherein: R4 represents hydrogen, lower alkyl, perhalo lower alkyl, aryl, aryl substituted with one or more lower alkyl, lower alkoxy, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or; -COR5, wherein: R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or; the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.
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