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US 5,024,835 AGranted
Conjugates of a vinca derivative carrying a detergent chain in the C-3 position
AssigneeIre-Celltarg S.A.
InventorsKSP Siva Bhushana Rao, Jean-Paul Dejonghe, Marie-Paule Collard, Andre Trouet
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Abstract
The subject of the present invention is conjugates of vinca (indole-dihydroindole) derivatives carrying a detergent chain of at least 7 aliphatic carbon atoms in the C-3 position bonded via a covalent bond to a macromolecular carrier of polypeptide character, and also pharmaceutical compositions containing these conjugates and a process of preparation.
Claims16
A conjugate of a vinca (indole-dihydroindole) derivative having a formula ##STR14## in which R.sub.1 and R.sub.2 together represent (1 ) --Et and --OH or (2) --H and --Et;
- R.sub.3 represents --OH or ##STR15## A represents --NH-- or a divalent radical of an amino acid found in a protein, wherein said divalent radical of said amino acid is terminated by ##STR16## R' represents an aliphatic hydrocarbon radical having at least 7 aliphatic carbon atoms;
- and
- --NH--P represents a radical derived from NH.sub.2 P, wherein NH.sub.2 P represents a macromolecular carrier of polypeptide origin in which said NH.sub.2 represents a free amino group.
Dependencies are inferred from the claim text.