Derivatives of taxol, pharmaceutical compositions thereof...

Details Derivatives of taxol, pharmaceutical compositions thereof... Derivatives of taxol, pharmaceutical compositions thereof...

C - Chemistry, Metallurgy

07

D

167/233, 167/243

C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/40 (2006.01) C07D 405/00 (2006.01)

Patent

CA 2028096

2028096 9010443 PCTABScor01 Derivatives of taxol represented by formula, (II) wherein R and R' are each H or the residue of an amino acid selected from the group consisting of alanine, leucine, isoleucine, saline, phenylalanine, proline, lysine and arginine or a group of formula (III), wherein n is an integer of 1 to 3 and R2 and R3 are each hydrogen on an alkyl radical having from one to three carbon atoms or wherein R2 and R3 together with the nitrogen atom to which they are attached form a saturated heterocyclic ring having four to five carbon atoms, with the proviso that at least one of R and R1 is not hydrogen, are provided together with pharmaceutical compositions of such derivatives. The taxol derivatives have increased water solubility as compared to taxol, and have excellent antitumor activity.

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