Sanofi

Elf Sanofi

Sonofi

Antonina Giudice

Umberto Guzzi

Marco Baroni

Marco Landi

Vivian Mazza

Paolo Carminati

Tiziano Croci

Daniel Frehel

Alberto Bianchetti

Alain Badorc

Claudine Serradeil-Legal

Luciano Manara

Philippe Soubrie

Claude Moulineau

Daniel Ducros

Jean Courregelongue

G Erard Le Fur

The present invention concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl, trifluoromethylthio, (C.sub.1 -C.sub.3)alkoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, or phenoxy group optionally substituted with a halogen atom, a trifluoromethyl, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkylthio, or cyano group, or of a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment or prophylaxis of those conditions deriving from disorders of the serotoninergic systems wherein a serotoninergic action selectively mediated by the 5-HT.sub.3 receptors is required, e.g. affective disorders, anxiety, psychotic troubles, constipation.

Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a

The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (I): ##STR1## in which A is --CH.dbd.N-- or --N.dbd.CH--; R is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, cyano, carboxamido, trifluoromethyl, a vinyl group, a formyl group, a carboxyl group in free, salt or esterified form, hydroxyl, hydroxymethyl, mercapto, amine, mono- or di-(C.sub.1-4 alkyl)amino, aminomethyl, mono- or di(C.sub.1-4 alkyl)aminomethyl, 1-piperido, 1-pyrrolidino, 1-piperazino or 4-(C.sub.1-4 alkyl)-1-piperazino, where R may replace any one of the hydrogen atoms of the heteroaryl nucleus;

1-heteruarylazetidines and -pyrrolidines, process for their preparation

The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (I): ##STR1## in which A is --CH=CH--; R is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, cyano, carboxamido, trifluoromethyl, a vinyl group, a formyl group, a carboxyl group in free, salt or esterified form, hydroxyl, hydroxymethyl, mercapto, amino, mono- or di-(C.sub.1-4 alkyl)amino, aminomethyl, mono- or di(C.sub.1-4 alkyl)aminomethyl, 1-piperido, 1-pyrrolidino, 1-piperazino or 4-(C.sub.1-4 alkyl)-1-piperazino, where R may replace any one of the hydrogen atoms of the heteroaryl nucleus; R.sub.1 is hydrogen or a methyl group; R.sub.2 and R.sub.3, which are identical or different, are hydrogen or C.sub.1-4 alkyl; n is 1 or 2; m is 0 or 1; and m+n.gtoreq.2; and addition salts with inorganic or organic acids of the compounds of formula (I). The invention also relates to pharmaceutical compositions containing these compounds, as well as to methods of treatment or prophylaxis of disorders which involve the peripheral or central serotoninergic systems.

1-heteroarylazetidines and -pyrrolidines process for their preparation

New therapeutic use of some heterocyclylpiperazines of formula (I) ##STR1## wherein R represents hydrogen or (C.sub.1 -C.sub.4)alkyl, R.sub.1 represents hydrogen or a methyl group, R.sub.2 represents hydrogen or a halogen atom; X et Y represent each --CH.dbd., or one is --CH.dbd. and the other is --N.dbd., as well as their pharmaceutically acceptable salts for the preparation of a medicament for the treatment or prophylaxis of the pathological conditions which can be improved by 5-HT.sub.3 mediated selective agonism and new compounds deriving from this chemical class.

New therapeutic use of heterocyclylpiperazines as 5-HT.sub.3 agonists

The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (IV): ##STR1## The substituents A, R', R.sub.1 and P, and the variables n and m, are as herein described.

1-heteroarylazetidines and -pyrrolidines

The compounds of the invention having the formula: ##STR1## in which: A, which is a ring condensed with cyclopentane, represents a substituted or unsubstituted thiophene ring, Q represents an alkylene chain, R.sub.1 and R.sub.2 each represent H or an alkyl, or they form, with the nitrogen atom to which they are linked, a saturated nitrogenous heterocyclic ring containing 5 to 7 atoms, R.sub.3 and R.sub.4 each represent H, alkyl, cycloalkyl, trifluoromethyl or an optionally substituted phenyl, thienyl or furyl group or R.sub.3 and R.sub.4 together form a (C.sub.5 -C.sub.8) cycloalkyl, as well as their addition salts with an acid and their quaternary ammonium derivatives. They can be used as medicines.

Ethers of thienocyclopentanone oximes, their preparation and

The present invention relates to a pharmaceutical composition having a peripheral antagonistic action with respect to opiates containing, as active ingredient, a haloallylate of levallorphan of formula: ##STR1## where X is chlorine, bromine or iodine, mixed with a pharmaceutical excipient.

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Milan, Italy

Antonina Giudice