Water soluble derivatives of camptothecin and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/22 (2006.01) A61K 31/435 (2006.01) C07D 317/66 (2006.01) C07D 319/18 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01)

Patent

CA 2161681

The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R1 represents: hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower allcyl, lower alkylamino lower alkyl, amino lower alkyl, lower alkoxy lower alkyl or (CH2)tAr wherein: t is 0 to 5 and Ar represents phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazol, with one or more substituents independently selected from hydroxy, methoxy, halogen, and amino; and R2 represents: diphenylmethyl or (CH2)tAr; or ii) R1 and R2 taken together with the linking nitrogen represent N-tetrahydroquinolyl or N-tetrahydroisoquinolyl; and the pharmaceutically acceptable salts and solvates thereof, their use in the treatment of tumors and methods of their preparation.

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