Processes for the preparation of new conjugates of...

Details Processes for the preparation of new conjugates of... Processes for the preparation of new conjugates of...

C - Chemistry, Metallurgy

07

D

167/139, 195/1.1

C07D 519/04 (2006.01) A61K 47/48 (2006.01)

Patent

CA 1234800

ABSTRACT NEW CONJUGATES OF VINBLASTINE, A PROCESS FOR THEIR PREPARATION AND THEIR USE IN THERAPY The invention relates to new conjugates of vin- blastine and some of its known derivatives with proteins, aminoacids or simple amines and their use as an anti- tumour agent. The invention also relates to some inter- mediates which are active in chemotherapy, and amino derivatives thereof. These compounds correspond to the following gen- eral formula Image in which A represents an "arm", such as -COCH2-, -COCH2- CH2CO- or COCH2-CH2-CH2-CO-, R1 represents an optionally modified protein radical, an amino group NR3R4, a chlor- ine atom or an aminoacid ester group bonded via the amine function, R2 represents a methoxy group, an amino group or an alpha-aminoacid ester radical which is bonded via a bond of the amide type and in which the ester group contains 1 to 6 carbon atoms, and R3 and R4 represent alkyl groups containing 1 to 3 carbon atoms or, together, an alkanediyl group containing 3 to 5 carbon atoms.

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