Synthelabo

Metabio Joullie

Yves Robert Pascal

Henry Najer

Don Pierre Giudicelli

Patrick Andre Lardenois

Christian J Warolin

Gabriel Maillard

Maurice Joullie

Lucien Lakah

Bogdan Iliesco-Branceni

Jean Pierre Lefevre

Compounds of the formula I ##STR1## wherein R.sub.1 represents a hydrogen or fluorine atom, and R.sub.2 represents an alkyl group containing 2 to 6 carbon atoms, or a cycloalkyl or cycloalkyl-alkyl group containing 5 to 8 carbon atoms, each of these groups being substituted by one or two hydroxy groups or an oxo group and, if desired, also by a 4-(m-trifluoromethylphenyl)-piperazino or 4-(3-trifluoromethyl-4-fluoro-phenyl)-piperazino group with the proviso that, when R.sub.1 represents a hydrogen atom, R.sub.2 does not represent a monohydroxyalkyl group, and their pharmaceutically acceptable acid addition salts are novel and have therapeutic use, notably in the region of the central nervous system and in the cardiovascular region.

M-Trifluoro-methylphenyl-piperazine

Vincamine and/or its stereoisomers, a known drug, is made from vincaminol and/or its stereoisomers by successive conversion of the latter into apovincaldehyde, apovincamine, and 16-methoxycarbonyl-eburnane, followed by conversion of the last into vincamine either directly by introduction of a 16-hydroxyl group or by hydrolysis, introduction of a 16-hydroxyl group, and re-esterification.

Apovincaldehyde

The invention provides vincaminic acid esters of formula ##SPC1## Wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is hydrogen or R.sub.1 and R.sub.2 form an additional bond between the two carbon atoms to which they are attached, and R.sub.3, R.sub.4 and R.sub.5 are hydrogen or methyl, and their salts. The esters are useful in treatment of cardiac-circulatory, cerebal-vascular or respiratory insufficiency.

Vincaminic acid esters

Compounds of the general formula ##SPC1## Wherein R.sub.1 is H or OH and R.sub.2 is H or R.sub.1 and R.sub.2 together represent an additional double bond between the two carbon atoms to which they are attached and m and n are integers of 1 to 5 and 2 to 7 respectively; and pharmaceutically acceptable acid addition salts thereof. The compounds are useful for the treatment of vascular disorders in mammals.

Vinvamine series cycloalkyl-alkyl esters

A process is provided for the preparation of cis-vincamine by oxidising trans-vincamine with tertiary butyl hypochlorite to obtain dehydrovincamine chloride, reducing the dehydrovincamine chloride with a metal in an aqeous acidic medium and neutralising the product, and separating cis-vincamine from the resulting mixture of cis- and trans-vincamines. Cis-vincamine is useful for the treatment of circulatory disorders.

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Paris, France

Yves Robert Pascal