Substituted acetamide derivatives, process for their preparation

Details Substituted acetamide derivatives, process for their preparation Substituted acetamide derivatives, process for their preparation

1990-05-07

1993-03-09

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514326, 514331, 514385, 514422, 514428, 546192, 546210, 546230, 546233, 548517, 5483147, A01N 4340, C07D21132, C07D21160

Patent

active

051927748

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION



Technical Field

This invention relates to novel substituted acetamide derivatives, their cyclodextrin inclusion compounds, a process for their preparation and antiulcer drugs containing the same.


Background Art

The developmental mechanism of a peptic ulcer is complicated because it is influenced by a variety of factors. Peptic ulcers are considered to be caused when the balance between aggressive factors (inhibition of gastric acid secretion) and protective factors (cytoprotective action) for the tunica mucosa of the stomach is lost. It is therefore effective preventive or curative means to inhibit the secretion of the gastric acid serving as an aggressive factor.
Hitherto, in the clinical field, anticholinergic agents and histamine H.sub.2 receptor blockers such as cimetidine have widely been used as effective agents for suppressing the gastric acid secretion.
However, the anticholinergic agents are accompanied by side-effects such as the suppression of the discharge movement of the stomach, thirst, mydriasis and inhibition of perspiration. What is worse, they cannot effectively prevent the aggravation of the ulcer nor prevent the relapse of it even when they are used in such amounts that would substantially inhibit the gastic acid secretion. Meanwhile, cimetidine causes undesirable side effects such as central actions and an antiandrogen effect. Furthermore, a problem arises in that the protective factors in the tunica mucosa function less if cimetidine is administered for a long term. As a result, it causes the relapse of the ulcer when the administration of cimetidine has been stopped.
Therefore, a desire has been arisen for an improved antiulcer drug capable of effectively controlling the secretion of gastric acid which serves as an aggressive factor, and having a protective factor potentiation action (cytoprotective action).
The inventors have studied for the purpose of finding an improved antiulcer compound capable of effectively controlling the secretion of gastric acid which serves as an aggressive factor, and having a protective factor potentiation action (cytoprotective action). As a result, the present invention was achieved, in which a substituted acetamide derivative of formula (I), its salts, and inclusion compounds thereof in cyclodextrin were found to meet the above objects.


DISCLOSURE OF INVENTION

According to the present invention, there is provided substituted acetamide derivatives, salts thereof, inclusion compounds obtained by causing said substituted acetamide derivatives or the salts thereof included in cyclodextrin and antiulcer drugs comprising them as active ingredient, the substituted acetamide derivative being represented by the following general formula (I): ##STR3## [in which Y represents a piperidino group, 1-pyrrolidinyl group, or 3-hydroxy-1-pyrrolidinyl group, and Z represents a group selected from the group consisting of (a) to (e): ##STR4## (in which l represents an integer from 0 to 2, n represents an integer from 1 to 3, R.sup.1 represents a hydroxy group, 1,2-dihydroxyethyl group, 1-hydroxyethyl group, 2-phenyl-1-hydroxyethyl group, 2-hydroxyethoxy group, lower alkoxycarbonyl group, 2,2-dimethyl-1,3-dioxolan-4-yl group, or a lower acyloxymethyl group); ##STR5## (in which R.sup.2 represents an amino group, lower alkylamino group, di(2-hydroxyethyl)amino group, lower alkyl group, or a lower alkoxy group); ##STR6## (in which R.sup.3 and R.sup.4 respectively represent a hydrogen atom, or a lower alkyl group); ##STR7## (in which l represents an integer from 0 to 2, and R.sup.5 and R.sup.6 respectively represent a hydrogen atom or a lower alkyl group).


BEST MODE OF THE INVENTION

The lower alkyl group of compound (I) according to the present invention is exemplified by a straight or a branched chain alkyl group having 1 to 6 carbon atoms, preferably methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl and tert-butyl groups. The lower alkozy group is exemplified by a straight or a branched chain alkoxy group having 1 to 6 carbon atoms, preferably me

REFERENCES:
patent: 4837316 (1989-06-01), Sekine et al.

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