Nitro derivatives of vinblastine-type bisindoles,...

C - Chemistry – Metallurgy – 07 – D

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C07D 519/04 (2006.01) A61K 31/475 (2006.01)

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CA 1276632

NITRO DERIVATIVES OF VINBLASTINE-TYPE BISINDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARINC SAME A b s t r a c t The invention relates to novel nitro derivatives of the general formula (I) (I) Image wherein Rl stands for a methyl or a formyl group; R2 stands for a hydroxy or ethyl group of .beta.-position; R3 means an ethyl group of ?-position; R4 represents a hydrogen atom; or R3 and R4 together represent an oxygen bridge or a double bond; R5, R6 and R7 each stand for a nitro group or hydrogen atom, with with the proviso that if one of these substituents stands for nitro then the other two substituents each stand for hydrogen; and Y stands for -N= when R5 stands for a nitro group; whereas Y stands for -NH- when R5 stands for a hydrogen atom and a valence bond exists between the C2, and C7, atoms, as well as their acid addition salts and pharmaceutical prepara- tions containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations. The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine- type bis-indole alkaloid drugs which are commercially available.

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