Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-21
1997-11-25
McKane, Jospeh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514333, 514334, 514344, 514356, 546257, 546258, 546322, 544360, 544365, A61K 31495, C07D40100
Patent
active
056913397
DESCRIPTION:
BRIEF SUMMARY
This application is a national stage filing under 35 U.S.C. 371 of PCT/JP94/01412, filed Aug. 25, 1994.
TECHNICAL FIELD
The present invention relates to a circulatory disorder improving agent comprising, as an active ingredient, a dihydropyridine derivative having a specific structure or an acid addition salt thereof.
BACKGROUND ART
A dihydropyridine derivative of the formula (I) ##STR2## wherein each symbol is as defined later, has a calcium channel antagonistic action and is already known to be useful as an hypotensive agent, a cerebral vasodilating agent and a therapeutic agent for coronary artery disorders (therapeutic agent for angina pectoris) (Japanese Patent Unexamined Publication No. 225356/1988, U.S. Pat. No. 4,886,819, EP-A-257616).
It has been also known that the above-mentioned derivative (I) is extremely useful as a cerebral blood flow increasing agent (Japanese Patent Unexamined Publication No. 62824/1990, EP-A-342577), a therapeutic agent for vasospasm (Japanese Patent Unexamined Publication No. 180826/1990, EP-A-379737) and a heart stimulant (Japanese Patent Unexamined Publication No. 235168/1992, EP-A-463407).
DISCLOSURE OF THE INVENTION
The present inventors have conducted intensive studies of the use of dihydropyridine derivatives (I) and found that the derivatives (I) and acid addition salts thereof have an unexpected action which is completely different from the above-mentioned actions heretofore found, namely, blood flow decrease-suppressive action and blood rheology-, erythrodeformability- and microcirculation-improving action, and that they are useful as organ circulatory disorder improving agents.
In particular, they effectively suppress blood flow decrease in various organs and are useful as organ circulatory disorder improving agents, as well as peripheral circulation improving agents.
Accordingly, the present invention aims at providing circulatory disorder improving agents containing, as an active ingredient, a dihydropyridine derivative (I) or an acid addition salt thereof.
Specifically, the present invention aims at providing an organ circulatory disorder improving agent and a peripheral circulation improving agent.
The present invention relates to a circulatory disorder improving agent comprising, as an active ingredient, a dihydropyridine derivative of the formula ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is an alkyl, a cycloalkyl or an alkoxyalkyl; an alkyl, a cycloalkyl, a halogenated alkyl, an alkylsulfonyl, an alkylsulfinyl, an alkylthio, an alkoxy, a halogensted alkoxy, an alkoxycarbonyl, a cyano, a halogen or a nitro, provided that R.sup.4 and R.sup.5 are not hydrogen atoms at the same time; ##STR4## wherein R.sup.6, R.sup.7 and R.sup.8 are the same or different and each is a hydrogen atom, an alkyl, a cycloalkyl, an aralkyl, an aryl or a pyridyl, referred to as dihydropyridine derivative (I)! or an acid addition salt thereof (generally a pharmacologically acceptable acid addition salt).
Of the above, a dihydropyridine derivative of the formula (I) wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is an alkyl, R.sup.4 is a hydrogen atom, R.sup.5 is a nitro, a halogenated alkyl or a cyano, R.sup.6 and R.sup.7 are the same or different and each is an alkyl, an aralkyl or an aryl, R.sup.8 is an aryl, Ar is an aryl and n is 1, is particularly preferable.
The dihydropyridine derivative (I) and an acid addition salt thereof to be used in the present invention are extremely low toxic, and show slow onset of effect and long duration thereof. Accordingly, they are highly effective and highly safe.
The symbols used in the formula (I) in the present specification are explained in the following.
R.sup.1, R.sup.2 and R.sup.3 may be the same or different. The alkyl represented by R.sup.1, R.sup.2 and R.sup.3 may be straight or branched and is preferably a lower alkyl having 1 to 6 carbon atoms, which is exemplified by methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl, neope
REFERENCES:
patent: 4886819 (1989-12-01), Ashimori et al.
patent: 5462951 (1995-10-01), Iwao et al.
The Japanese Journal of Pharmacology, vol. 49, Supplementum 1989, 62nd General Meeting, Mar. 25-28, 1989. (Abstract).
The Japanese Journal of Pharmacology, vol. 59, Supplementum 1992, 65th Annual Meeting, Mar. 22-25, 1992. (Abstract).
Clinical and Experimental Pharmacology and Physiology, Blackwell Scientific Publications, vol. 20, No. 2, Feb. 1993, pp. 103-111.
Kawamura Toru
Okita Minori
Shinyama Hiroshi
Uchida Takeshi
Watanabe Masahiro
McKane Jospeh
Myers, Jr. Richard S.
The Green Cross Corporation
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