Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-01-16
1999-12-07
Stockton, Laura L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514258, 514259, 514262, 514265, 514269, 514274, 514312, 514338, 514363, 514364, 514367, 514375, 514376, 514381, 514387, 544256, 544265, 544266, 544284, 544310, 544315, 546157, 5462737, 5463694, 548132, 548136, 548144, 548159, 548181, 548221, 548229, 548251, 5483054, 5483061, 5482638, 5482644, A61K 3141, C07D40112
Patent
active
059984562
DESCRIPTION:
BRIEF SUMMARY
This application claims the benefit under 35 U.S.C. .sctn.371 of prior PCT International Application No. PCT/JP96/01949 which has an International filing date of Jul. 12, 1997 which designated the United States of America, the entire contents of which are hereby incorporated by references.
TECHNICAL FIELD
The present invention relates to benzimidazole compounds. More precisely, the present invention relates to novel bis-type benzimidazole compounds which are useful as an active ingredient of a medicament for therapeutic and preventive treatment of hyperlipemia, arterial sclerosis and the like, or useful as an additive of a silver halide photosensitive material, a liquid crystal material and the like.
BACKGROUND ART
In recent years, patients with so-called adult diseases such as arterial sclerosis, hypertension, and diabetes mellitus have been continuously increasing with prolongation of life expectancy. In particular, patients with hyperlipemia and arterial sclerosis derived therefrom have been remarkably increasing due to excessive intake of high calorie and high cholesterol food, which have become a serious social problem. Medicaments currently used for drug therapy of hyperlipemia and arterial sclerosis are those symptomatically lower cholesterol in blood, and therefore, they cannot be expected to have potency in retracting arterial sclerosis lesions, per se. Arterial sclerosis is characterized by lesions of intimal hyperplasia and lipid accumulation in blood vessels, and it has been elucidated from recent biochemical findings that foaming of macrophages plays a main role in the formation of arterial sclerosis lesions. Accordingly, suppression of the foaming of macrophages may possibly prevent arterial sclerosis by inhibiting formation of arterial sclerosis lesions, or achieve radicular treatment of arterial sclerosis by retraction of arterial sclerosis lesions. However, no medicament having such activity has been known.
Therefore, an object of the present invention is to provide a compound having activity of suppressing the foaming of macrophages, and is useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of arterial sclerosis. Another object of the present invention is to provide a compound having the aforementioned activity, and is useful as an active ingredient of medicament for preventive and/or therapeutic treatment of hyperlipemia.
DISCLOSURE OF THE INVENTION
The inventors of the present invention conducted various research to achieve the foregoing objects, and as a result, they found that novel benzimidazole compounds represented by the formulas set out below have activity of suppressing the foaming of macrophages, and are useful as active ingredients of preventive and therapeutic medicament of arterial sclerosis and preventive and therapeutic medicament of hyperlipemia. The present invention was achieved on the basis of this finding.
According to the first aspect of the present invention, there are provided benzimidazole compounds represented by the following formula (IA): ##STR2## wherein, Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen atom, a halogen atom, an alkyl group, a haloalkyl group, an aryl group, an alkoxy group, an aryloxy group, an alkoxycarbonyl group, a carbamoyl group, a sulfamoyl group, an acylamino group, a sulfonylamino group, cyano group, hydroxyl group, or nitro group; R.sup.3 and R.sup.4 independently represent hydrogen atom, an alkyl group, an acyl group, a sulfonyl group, an alkoxycarbonyl group, a sulfamoyl group, or a carbamoyl group; n and m each independently represent an integer of 1, 2 or 3, and where n or m represents 2 or 3, two or three R.sup.1 or R.sup.2 which may be the same or different substitute on the benzene ring, respectively; and L represents a linking group selected from a group consisting of a C.sub.2-12 alkylene group, and an alkylene group containing one or more phenylene groups or ether groups and ha
REFERENCES:
patent: 4814329 (1989-03-01), Harsanyi et al.
F. M. Whittington et al., "International Journal of Obesity", XP-002076231, vol. 11, pp. 619-629, 1987.
Aikawa Kazuhiro
Aoki Kozo
Fuji Photo Film Co. , Ltd.
Stockton Laura L.
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