Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
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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Evans et al., Pharmacology Biochemistry & Behavior, 40, 4, 1991, 1033-1040.
Baroni Marco
Giudice Antonina
Guzzi Umberto
Landi Marco
Mazza Vivian
Gupta Yogendra N.
Sanofi
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