Maytansinoids, their production and pharmaceutical compositions containing them.

摘要

Novel maytansionoids of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="41" wi="67" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R is an alicyclic hydrocarbon group of 3 to 10 carbon atoms, phenyl or heterocyclic group, which may optionally be substituted, and</ListItem><ListItem>A is an alkylene group of 1 to 4 carbon atoms or a bond, provided that A means said alkylene group when attached to a N atom in said heterocyclic group R, e.g. maytansinol 3-cyclohexanecarboxylate, have antimitotic and antitumor activities, and are of value as medicines. Pharmaceutical compositions are described.</ListItem></UnorderedLists>

A method for producting a compound of the above formula comprises acylating maytansinol with a carboxylic acid of the formula:
<Chemistry id="chema02" num="0002"><Image id="ia02" he="7" wi="29" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R and A are as defined above, or a reactive derivate of said carboxylic acid with respect to the carboxyl function thereof.