1-heteroarylazetidines and -pyrrolidines process for their prepa

Details 1-heteroarylazetidines and -pyrrolidines process for their prepa 1-heteroarylazetidines and -pyrrolidines process for their prepa

1995-01-05

1996-10-15

Gupta, Yogendra N.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514255, 514256, 514343, 514210, 544298, 544322, 544334, 544336, 544408, 544409, 546193, 5462681, 5462764, A61K 3144, C07D40104

Patent

active

055654746

ABSTRACT:
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.

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patent: 5138062 (1992-08-01), Osdene et al.
patent: 5304555 (1994-04-01), Awaya et al.
patent: 5410057 (1995-04-01), Baroni et al.
Evans et al., Pharmacology Biochemistry & Behavior, 40, 4, 1991, 1033-1040.

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