Conjugates of vinblastine and its derivatives, process for preparing them and pharmaceutical compositions containing these conjugates.

摘要

Vinblastine-protein conjugates of formula (I) are new: n = 1-5; R = acyl; R1 = an opt. modified protein; R2 = OMe, NH2 or an N-bonded alpha-amino acid 1-6C ester gp.; R3 = H or OH. R1 = bovine or human serum albumin, fetuin or an immunoglobulin, esp. a human monoclonal antibody R2 = OMe, NH2, ethyl tryptophanate or ethyl isoleucinate. (I) are prepd. by reacting the corresp. 4-O-deacetylvinblastine cpd. (II) with an anhydride of HOOC-CH(NHR)-(CH2)n-COOH and reacting the prod. with a protein, or reacting (II) with a cpd. capable of introducing a CO-CH(NHR)-(CH2)n-COR1 gp. -