University of California

G.d. Searle & Company

Martin A Apple

Joseph V Formica

Hiroaki Yanagisawa

Raphael Pappo

C Anthony Hunt

The present invention relates to bis(4-demethoxydaunorubicin)dihydrazone of the formula ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen or alkyl having from 1 to 4 carbon atoms and X represents

Bis(4-demethoxydaunorubicin)dihydrazone derivatives and

A new group of compounds having an enhanced ability to inhibit nucleic acid functions have been prepared. These drugs are bis-anthracyclines wherein two anthracycline molecules are linked through their C-13 carbon atoms by amino and/or hydroxy-dicarboxylic acids and their derivatives to form the bis-compounds. Such bis-anthracyclines may be even more effectively delivered to selected sites in a mammalian organism by incorporating the same within uniformly sized liposomes.

Bis-anthracycline nucleic acid function inhibitors and improved method

Modified actinomycin compounds that incorporate azetidine in the polypeptide component of the actinomycin molecule are disclosed. These compounds are called azetomicins and specifically incorporate an azetidine derivative in the 3' peptide position in at least one of the two polypeptides normally present in actinomycins. The azetomicins are produced by bio-synthetic means from Streptomyces antibioticus that are cultured on a medium including azetidine-2 carboxylic acid and derivatives thereof.

Process for treating neoplastic disease with azetomicins

Modified actinomycin compounds that incorporate azetidine in the polypeptide component of the actinomycin molecule are disclosed. These compounds are called Azetomicins and specifically incorporate an azetidine derivative in the 3' peptide position in at least one of the two polypeptides normally present in actinomycins. The Azetomicins are produced by bio-synthetic means from Streptomyces antibioticus that are cultured on a medium including azetidine-2 carboxylic acid and derivatives thereof.

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Daly City, CA, United States of America

Martin A Apple