Synthelabo

Regis Dupont

Jonathan Reid Frost

Henry Najer

Gabor I Koletar

Claude C Morel

Patrick Andre Lardenois

Bernard Gaudilliere

Jean Rousseau

Don Pierre Giudicelli

Alexander E Wick

Jean Bertin

Philippe Michel Manoury

Daniel C Obitz

Salomon Z Langer

Johannes Schoemaker

Jean P LeFevre

Jonathan B Frost

Ifenprodil and its analogues are useful for the treatment of psychoses such as schizophrenia.

Method of treatment of psychotic disorders

A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,

6-phenyl-3-(piperazinyalalkyl)-2,4(1H,3H)-pyrimidinedione derivatives,

Compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, alkyoxy, benzyloxy, alkanoyloxy, or benzoyloxy, or when R.sub.2 is hydroxyl or methoxy in the 4-position and R.sub.3 is hydrogen, R.sub.1 may also represent hydroxymethyl carbamoyl or alkoxycarbonyl,

Therapeutically useful 1-phenyl-2-piperidinoalkanol derivatives

Pyrimido- and imidazo-pyridoindole derivatives, in the form of racemates or optically active isomers, of formula: ##STR1## in which n=0 or 1, R.sub.1 =H, Hal, alkyl or alkoxy or CF.sub.3, R.sub.2 =H, alkyl, cycloalkyl-alkyl, cycloalkyl, N,N-dialkylaminoalkyl or phenyl, R.sub.3 =H or alkyl and R.sub.4 =H, alkyl or benzyl are useful as anti-anoxia or psychotropic agents in therapy. They are prepared by cyclizing a compound of formula: ##STR2## wherein R.sub.5 is alkyl, by heating it in an acidic medium, such as ethanolic hydrogen chloride.

Pyrimido- and imidazo-pyridoindole derivatives

Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk--O--, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

Pyridoindole derivatives

Derivatives of fluorenes and fluoranthenes, in the form of racemates or of enantiomers, of the formula (I) ##STR1## in which n is 1 or 2, R.sub.1 is a hydrogen or halogen atom or an alkyl or alkoxy radical, R.sub.2 is a hydrogen atom or an alkyl, cycloalkyl, cycloalkylalkyl, benzyl, halogenobenzyl, alkylbenzyl, alkoxybenzyl, acyl, alkoxycarbonyl or alkylaminocarbonyl radical, R.sub.3 is a hydrogen atom or an alkyl radical, R.sub.4 is a hydrogen atom or an alkyl, acyl or aroyl radical, the alkyl and alkoxy radicals or parts of radicals having from 1 to 4 carbon atoms and pharmaceutically acceptable acid addition salts thereof, are therapeutically valuable as anti-anoxia and psychotropic agents.

Derivatives of fluorenes and fluoranthenes and process for their

Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk-O-, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

The present invention relates to new indolo [3,2,1-de]-[1,5]naphthyridine derivatives and their addition salts with pharmaceutically acceptable acids, the preparation of such derivatives and salts and medicaments in which they are present as active principle.

Naphthyridine derivatives

The invention provides a new piperazine derivative, 1-(4-fluoro-3-trifluoromethylthio-phenyl)-piperazine of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, which is useful as a medicament in human and veterinary therapy because of its anorexia-inducing effect.

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Paris, France

Regis Dupont