N-(vinblastinoyl-23) derivatives of amino acids, their...

Details N-(vinblastinoyl-23) derivatives of amino acids, their... N-(vinblastinoyl-23) derivatives of amino acids, their...

C - Chemistry, Metallurgy

07

D

260/237.3

C07D 519/04 (2006.01)

Patent

CA 1198422

ABSTRACT OF THE DISCLOSURE Vinblastine derivatives of the general formula: (II) Image wherein R is an ester of an amino-acid which may be protected, attached to the vinblastin-23-oyl moiety by an amide bond, the ester group, which may be straight or branched, contain- ing 2-9 carbon atoms and R1 is a hydrogen atom or a hydroxy group, R2 is a hydrogen atom, a formyl group of a C2-C9 acyl group, R5 is a hydrogen atom or a methyl group or a formyl group, with the provision that compounds where R5 is methyl and R1 is a .beta.-hydroxy group are excluded; or their phar- maceutically acceptable addition salts with mineral or organic acids which compounds are useful in treating leukemia and malignant tumors in humans.

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