New conjugates of vinblastine and its derivatives, process for preparing them and pharmaceutical compositions containing them

US4828831A · kind A · utility

Assignee

• OMNI CHEM CO., LTD. · BE

Inventors

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

Key dates

• Filing date: Dec 12, 1986
• Grant date: May 9, 1989
• Expiry date: Dec 12, 2006

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S530/866
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A description is given of conjugates of vinca alkaloid of the indole-dihydroindole type with a protein or a protein fragment, corresponding to the general formula ##STR1## in which R.sub.1 denotes a protein or a protein fragment; PA1 R.sub.2 is COO(C.sub.1-3 alkyl) or CO--R.sub.7 where R.sub.7 is NH.sub.2 or an amino acid ester or peptide ester; PA1 R.sub.3 is H, CH.sub.3 or CHO; PA1 when R.sub.5 and R.sub.6 are taken separately, R.sub.6 is H and one of R.sub.4 and R.sub.5 is ethyl and the other is H or OH; PA1 when R.sub.5 and R.sub.6 are taken together with the carbon atoms to which they are attached, they form an oxirane ring and R.sub.4 is ethyl, and A is a residue of a bifunctional organic derivative of the maleoylamino acid or maleoyl peptide or maleoylphenoxy type.