Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-03-23
1997-08-26
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514381, 514824, A61K 3147, A61K 3141
Patent
active
056611587
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/01052, filed Jul. 27, 1993.
TECHNICAL FIELD
The present invention relates to a new use of a compound having angiotensin II antagonism.
More particularly, the present invention relates to a new use of a compound having angiotensin II antagonism (hereinafter referred to as "angiotensin II antagonist") for lowering lipids in living bodies.
DISCLOSURE OF THE INVENTION
Accordingly, one object of the present invention is to provide a lipids-lowering agent which comprises an angiotensin II antagonist as an active ingredient.
Another object of the present invention is to provide a new use of an angiotensin II antagonist as a lipids-lowering agent.
Further object of the present invention is to provide a new use of an angiotensin II antagonist for manufacturing a medicament for treating or preventing lipids-associated diseases and conditions such as hypercholesterolemia, hyperlipidemia, hyperlipemia, hyperlipoproteinemia, atherosclerosis, and the like.
Still further object of the present invention is to provide a method for treating or preventing lipids-associated diseases and conditions as mentioned above which comprises administering an effective amount of an angiotensin II antagonist to a host such as animals including human.
It is reported that angiotensin II, which is a kind of hormones existing in living bodies of animals and is mainly produced by angiotensin II converting enzyme from angiotensin I, possesses strong vasoconstrictive action and releasing action for aldosterone from the adrenal cortex. Therefore, it is known that an angiotensin II antagonist exhibits vasodilating activity, and is of use for treating hypertension and some heart failures.
The inventors of the present invention extensively investigated various effects of the angiotensin II antagonists, and during such investigations, it has been found that an angiotensin II antagonist further exhibits lipids-lowering activity in living bodies of animals, particularly in blood. This finding is really new and is not expectable at all for a person skilled in this field.
In the present invention, so-called "lipids" include various cholesterols, particularly high and low density lipoprotein cholesterols (HDL-C, LDL-C), phospholipids, neutral fats (e.g. triglycerides of fatty acids, etc.), and the like. Therefore, according to the present invention, any angiotensin II antagonist is capable of lowering the level of various lipids including the above lipids in living bodies of animals, particularly total cholesterols, LDL-C and phospholipids in blood serum of human.
The angiotensin II antagonist used in the present invention is not limitative and includes any compound which exhibits angiotensin II antagonism, particularly non-peptide angiotensin II antagonist.
The preferred embodiment of the angiotensin II antagonist of the present invention can be represented by the following general formula: ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, lower alkyl, lower alkoxy, amino or acylamino, ##STR2## in which R.sup.3 and R.sup.4 are each hydrogen or an imino-protective group, lower alkyl, lower alkenyl, lower alkylthio, mono or di or trihalo(lower)alkyl, oxo(lower)alkyl, hydroxy(lower)alkyl or optionally esterified carboxy; or ##STR3## is condensed or uncondensed imidazolyl which may be substituted by suitable substituent(s), or a pharmaceutically acceptable salt thereof.
Another embodiment of the angiotensin II antagonist used in the present invention is a compound of the formula: ##STR4## in which Z is 2-lower alkyl-4-halo-5-hydroxy(lower)alkylimidazol-1-yl; 2-lower alkylquinolin-4-yloxy; 2-lower alkoxy-7-carboxy (or esterified carboxy)-1H-benzimidazol-1-yl; or 2- or 2,7-di or 2,5,7-tri-(lower)alkyl-3H-imidazo[4,5-b]pyridin-3-yl; and ##STR5## Z is 2- or 2,7-di or 2,5,7-tri-(lower)alkyl-3H-imidazo[4,5-b]pyridin-3-yl; 2-lower alkoxy-7-carboxy (or esterified carboxy) -1H-benzimidazol-1-yl; or 2-lower alkoxy- 5,7-di(lower)alkyl-3H-imidazo[4,5-b]pyridin-3-yl; and ##STR6## wherein R.sup.5 R.sup.6 and R.sup.7 are ea
REFERENCES:
patent: 5243054 (1993-09-01), Naka et al.
CA 118:73665, Hill, 1992.
CA 117:245603, Darrow et al., 1992.
CA 117:131218, Bovy et al., 1992.
Ohtsuka Minoru
Sakai Shigeru
Fujisawa Pharmaceutical Co. Ltd.
Jordan Kimberly
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