Cyclopropyl and cyclobutyl epothilone analogs

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S390000, C548S204000, C548S110000, C548S182000, C548S186000

Reexamination Certificate

active

07358266

ABSTRACT:
The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IVwherein Ar is a radical represented by the following structure:and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.

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