Nitroapovincaminic acid derivatives, pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 461/00 (2006.01) A61K 31/475 (2006.01)

Patent

CA 1266659

ABSTRACT The invention relates to a new process for preparing novel racemic and optically active 9- or 11- -nitroapovincaminic acid derivatives of the general formula (I) (I) Image wherein R stands for a -CO-X group, wherein X means a halogen atom; or for a -CO-OR1 group, wherein R1 means an optionally mono- or polysubstituted C1-10 aliphatic group, a C3-8 ali- cyclic group or an aromatic C6-14 hydrocarbyl group;or for a -CO-NR2R3 group, wherein R2 and R3 are the same or different and stand for a hydrogen atom or a C1-8 alkyl group optionally forming a saturated - 2 - heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R3 may also represent an amino group when R2 stands for a hydrogen atom; or for a cyano group, as well as their salts and pharmaceutical preparations eontaining these compounds. Furthermore the invention relates to a proeess for preparing these eompounds and preparations. The racemia and optically active substances of the general formula (I) as well as their pharma- ceutically acceptable acid addition and quaternary salts have valuable therapeutie properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.

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