The present invention is directed to novel taxanes having utility as antitumor agents.
The taxane family of terpenes, of which baccatin III and taxol, also commonly referred to as paclitaxel, are members, has been the subject of considerable interest in both the biological and chemical arts. Taxol itself is employed as a cancer chemotherapeutic agent and possesses a broad range of tumor-inhibiting activity. Taxol has a 2'R, 3'S configuration and the following structural formula:
wherein Ac is acetyl and Bz is benzoyl.
Colin et al. reported in U.S. Pat. No. 4,814,470 that certain paclitaxel analogs have an activity significantly greater than that of taxol. One of these analogs, commonly referred to as docetaxel (Taxotere®), has the following structural formula:

Although taxol and docetaxel are useful chemotherapeutic agents, there are limitations to their effectiveness, including limited efficacy against certain types of cancers and toxicity to subjects when administered at various doses. Accordingly, a need remains for additional chemotherapeutic agents with improved efficacy and less toxicity.
USPTO Backgrounds
USPTO Backgrounds