Sanofi

Marco Landi

Umberto Guzzi

Marco Baroni

Antonina Giudice

Dino Nisato

Tiziano Croci

Vivian Mazza

A compound of formula (VIII): ##STR1## in which Alk is a (C.sub.1 -C.sub.4)alkyl group, R.cndot. is hydrogen or a protecting group cleavable by hydrolysis and R is hydrogen, a protecting group cleavable by reduction or a heterocycle of structure (IX): ##STR2## in which Hal is a halogen atom and X, Y and Z are each --CH.dbd. or one of them is a nitrogen atom and the others are --CH.dbd., and its salts, R.cndot. being other than hydrogen if R is hydrogen or a group of structure (IX).

Heteroarylpiperidines

The present invention relates to novel heteroarylpiperidines of formula (I): ##STR1## in which Hal is a halogen atom, Alk is a C.sub.1-4 alkyl group and one of X, Y and Z is a nitrogen atom while the others are .dbd.CH--, and their salts. These compounds are useful as 5-HT.sub.3 agonists.

1-Halopyrazin- and 1-halopyrimidin-4-amino-4-alkylpiperidines

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

The present invention relates to novel heteroarylpiperidines of formula (I): ##STR1## in which Hal is a halogen atom, Alk is a C.sub.1 -C.sub.4 alkyl group and X, Y and Z are each --CH.dbd. and their salts, to a process for their preparation and to their use as drugs active as 5-HT.sub.3 agonists.

1-halopyridin-4-amino-4-alkylpiperidines

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.

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Bussero, Italy

Marco Landi