Vinblastin-23-oyl amino acid derivatives

US4639456A · kind A · utility

Assignee

• Omnichem S.A. · BE

Inventors

• Andre Trouet · Winksele, BE
• Jean A. A. J. Hannart · Chaumont-Gistoux, BE
• Kandukuri S. B. Rao · Bastogne, BE

Key dates

• Filing date: Dec 3, 1982
• Grant date: Jan 27, 1987
• Expiry date: Dec 3, 2002

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/29
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.