Water soluble camptothecin derivatives

Details Water soluble camptothecin derivatives Water soluble camptothecin derivatives

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 317/66 (2006.01) C07D 319/18 (2006.01) C07D 405/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2081580

GLX-76/AC155 -56- ABSTRACT WATER SOLUBLE CAMPTOTHECIN DERIVATIVES The invention relates to water soluble, camptothecin derivatives of formula (1), Image (I) wherein: n represents the integer 1 or 2; and i) 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, 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 wherein: Y represents O, S, CH2, NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, 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; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

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