Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1991-07-19
1992-04-21
Reamer, James H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514685, 562464, 568334, 568325, A61K 3119
Patent
active
051068710
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an anti-ulcer agent having, anti-ulcer action, which is effective for the medical treatment of diseases of digestive organs, such as a gastric ulcer and a duodenal ulcer, and a novel chalcone derivative having such an anti-ulcer action.
BACKGROUND ART
H.sub.2 receptor antagonists, anti-choline agents, gastric mucous membrane-protecting agents and antacids are now mainly used as anti-ulcer agent. Although these agents have medicinal effects, undesirable adverse side effects are also found. For example, the H.sub.2 receptor antagonists most frequently used at the present are excellent in the action of controlling a secretion of gastric juice, but are defective in that, after discontinuation of the administration, a counteraction of promoting a secretion of gastic juice appears. Anti-choline agents often show an excessive action of controlling a secretion of gastric juice because they have a parasympatholytic action, and moreover, they blunt the activity of the stomach and impair digestion. Since antacids temporarily neutralize gastric acid, they show a counteraction of promoting a secretion of gastric juice and other various adverse side effects. In short, an agent having excellent anti-ulcer action and showing no adverse side effects has not been developed.
DISCLOSURE OF THE INVENTION
It is therefore a primary object of the present invention to provide an anti-ulcer agent having excellent anti-ulcer action and reduced adverse side effects, which can be continuously administered for a long time.
The present inventors carried out research with a view to attaining this object, and as a result, found that a chalcone derivative represented by the following general formula I (hereinafter referred to as "compound of formula I") has a remedial effects for ulcers and the present invention was completed based on this finding: ##STR2## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for a hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.
More specifically, in accordance with the present invention, there is provided an anti-ulcer agent comprising a compound of formula I as the effective ingredient.
Of the compounds of formula I valuable for use as the anti-ulcer agent of the present invention, compounds represented by the following general formula I' are novel, and therefore, in accordance with the present invention, there is provided a novel chalcone derivative represented by the following general formula I': ##STR3## wherein X' and Y' independently stand for a hydrogen atom or together form a single bond, R'.sub.1 stands for a hydroxyl group or a carboxymethoxy group, R'.sub.2 stands for a hydrogen atom, an isoprenyl group, an isopentyl group or a propyl group, R'.sub.3 stands for a hydroxyl group or a methoxy group, R'.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R'.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R'.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R'.sub.7 stands for a hydrogen atom or a methoxy group, provided that (1) when R'.sub.2 is a hydrogen atom, at least one of R'.sub.3, R'.sub.4, R'.sub.5 and R'.sub.6 is not a methoxy group, (2) when R'.sub.2 is an isoprenyl group, R'.sub.1 is a carboxymethoxy group, (3) when R'.sub.2 is an isopentyl group and each of R'.sub.5 and R'.sub.7 is a hydrogen atom, R'.sub.4 is a hydrogen atom and one of R' and R'.sub.6 is a carboxymethoxy group, (4) when R'.sub.4 is not
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Hosaka Kunio
Komazawa Yukio
Mitsuhashi Hiroshi
Takeda Shigefumi
Watanabe Toshihiko
Reamer James H.
Tsumura & Co.
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