Paclitaxel analogs, preparation and use as antitumor agents

Details Paclitaxel analogs, preparation and use as antitumor agents Paclitaxel analogs, preparation and use as antitumor agents

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/335 (2006.01)

Patent

CA 2210924

The present invention provides novel paclitaxel analogs, specifically 2", 3" side-chain halogenated cephalomannine of the formula Image wherein, I. (2"R,3"S)-dihalocephalomannine Image II. (2"S,3"R)-dihalocephalomannine Image III. (2"R,3"S)-dihalo-7-epi-cephalomannine Image IV. (2"S,3"R)-dihalo-7-epi-cephalomannine Image (2"y 3"S)-dihalocephalomannine Image R1=H R2=OH (2" R~3"R)-dihalocepha~omannine R ' Image Rt=OH Ri=H (2"'S~3"S)-dihalo-7-epi-cephalomannine Rl-H RZnOH Image (2"R,3"R)-dihalo-7-epi-cephalomannine R _ R~=H Ri=OH Image and X = halogen, which show strong in vitro and in vivo paclitaxel-like efficacy in a variety of tumors.

La présente invention concerne des nouveaux analogues du paclitaxel, notamment des céphalomannines halogénées à chaîne latérale 2", 3", lesquelles présentent in vitro et in vivo une grande efficacité, du type de celle du paclitaxel, à l'égard de diverses tumeurs.

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