Pharmaceutical compositions containing didemnins

Details Pharmaceutical compositions containing didemnins Pharmaceutical compositions containing didemnins

1992-02-18

1994-03-15

Nutter, Nathan M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 11, C07K 512, A61K 3700

Patent

active

052946037

ABSTRACT:
This invention is directed to didemnin derivatives, including N-acyl congeners of didemnin A (DA); several DDB-type analogues of DA in which either pyruvic acid has been replaced (with phenylpyruvic acid or alphaketobutyric acid) or proline at position 8 has been replaced [with L-azetidine-2-carboxylic acid (AZT), L-pipecolic acid (Pip), 1-amino-1-carboxylic cyclopentane (acc.sup.5), D-Pro or sarcosine (sar); and other cyclic depsipeptides related to the didemnins, which were isolated from a relatively polar extract of the tunicate T. solidum; namely the didemnins--X [(R)-3-hydroxy-decanoyl-(Gln).sub.3 -Lac-Pro didemnin A]; Y [(R)-3-hydroxy-decanoyl-(Gln).sub.4 -Lac-Pro didemnin A]; M (pGlu-Gln-Lac-Pro-didemnin A); N ([Tyr.sup.5 ] didemnin B); nordidemnin N ([Tyr.sup.5 ] nordidemnin B); and epididemnin A ([2S,4R-Hip.sup.2 ] didemnin A).

REFERENCES:
patent: 4782135 (1988-11-01), Rinehart, Jr.
patent: 4950649 (1990-08-01), Rinehart
patent: 5137870 (1992-08-01), Rinehart

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