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US 4,639,456 AGranted
Vinblastin-23-oyl amino acid derivatives
AssigneeOmnichem
InventorsAndre B. L. Trouet, Jean A. A. J. Hannart, Kandukuri S. B. Rao
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AssigneeOmnichem
InventorsAndre B. L. Trouet, Jean A. A. J. Hannart, Kandukuri S. B. Rao
Estimating the term…
Vinblastine derivatives of the formula ##STR1## wherein R.sub.1 is an ester of a .alpha.-aminoacid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, glutamic acid, aspargine, glutamine, arginine, lysine, cysteine, cystine, methionine, phenylalanine, tyrosine, tryptophan, proline, histidine, hydroxy-lysine, hydroxyproline, or of a peptide consisting of 1-6 identical or different such amino-acids, and the ester group, which may be straight or branched, being a carboalkoxy group having 2-9 carbon atoms, and R.sub.2 is hydrogen or a C.sub.2 -C.sub.9 alkanoyl group, R.sub.5 is H or OH, R.sub.6 is CH.sub.3, CHO or H and X=H or Br and their pharmaceutically acceptable mineral or organic acid addition salts. The compounds are useful as antitumor drugs.
A vinblastine group of the formula ##STR9## wherein R.sub.1 is an ester, attached through the nitrogen of a .alpha.-aminoacid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threoinine, aspartic acid, glutamic acid, aspargine, glutamine, arginine, lysine, cysteine, cystine, methionine, phenylalanine, tyrosine, tryptophan, proline, histidine, hydroxy-lysine, hydroxyproline, or of a peptide consisting of 2-6 identical or different such amino-acids, and the ester group, which may be straight or branched, being a carboalkoxy group having 2-9 carbon atoms, and R.sub.2 is hydrogen or a C.sub.2 -C.sub.9 alkanoyl group, R.sub.5 is H or OH, R.sub.6 is CH.sub.3, CHO or H and X is Br and their pharmaceutically acceptable mineral or organic acid addition salts.
A vinblastine group of the formula ##STR10## wherein R.sub.2 is a hydrogen atom or a C.sub.2 -C.sub.3 alkanoyl group, R.sub.3 is a hydrogen atom, straight or branched C.sub.1 -C.sub.8 alkyl, hydroxy - C.sub.1 -C.sub.8 -alkyl, carboxy -C.sub.1 -C.sub.8 -alkyl, amido -C.sub.1 -C.sub.8 - alkyl, amino -C.sub.1 -C.sub.8 -alkyl or hydroxyalkyl, guanadino -C.sub.1 -C.sub.8 - alkyl, sulfydryl -C.sub.1 -C.sub.8 alkyl, methylthio-ethyl, benzyl, hydroxy-benzyl, or a group:
A compound of the formula ##STR12## wherein R.sub.1 is an ester, attached through the nitrogen, of L-tryptophan and the ester group, which may be straight or branched, is a carboalkoxy group, R.sub.2 is hydrogen or a C.sub.2 -C.sub.9 alkanoyl group, R.sub.5 is H or OH, R.sub.6 is CH.sub.3, CHO or H, and X is H or Br, and its pharmaceutically acceptable mineral or organic acid addition salts.
The sulfuric acid addition salt of a compound selected from the group consisting of:
Ethyl N-(O-4-deacetyl-4'-deoxy-vinblastin-23-oyl-B)L-tryptophanate sulphate or methane sulfonate.
A derivative of vinblastine selected from the group consisting of
Dependencies are inferred from the claim text.