Bis-indole derivatives, pharmaceutical compositions...

Details Bis-indole derivatives, pharmaceutical compositions... Bis-indole derivatives, pharmaceutical compositions...

C - Chemistry, Metallurgy

07

D

167/209, 260/237

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

Patent

CA 1278790

ABSTRACT The invention relates to novel bis-indole derivatives of the general formula. (I) Image (I) wherein R1 stands for a hydrogen atom or an acetyl group; R2 stands for a hydrogen atom; R3 means an ethyl group of .alpha.-position; or R2 and R3 together represent an oxygen bridge; R4 represents an ethyl or hydroxyl group of .beta.-position; and R5 stands for a hydrogen atom or a hydroxyl group; A represents a straight-chain C1-10 alkyl; a branched-chain C3-10 alkyl group; a C1-4 alkyl group containing in the omega position a hydroxyl, C2-5 alkanyloxy, carbamoyl or formylamino substituent; a benzyl group, a pyridyl group or a phenyl group; and X stands for a sulphur atom, or pharmaceutically acceptable acid addition salts and pharmaceutical preparations 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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