Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-05-10
1995-02-21
Bernhardt, Emily
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544374, 544396, 549552, 549555, 549559, A61K 31495, C07D295088
Patent
active
053915526
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel diphenylpiperazine derivative or its salts having a strong antagonism against calcium, and to a drug for circulatory organs containing the diphenylpiperazine derivative or its salts for use in the cure and prevention of a variety of circulatory organ diseases.
BACKGROUND ART
Conventionally, a variety of drugs have been developed and clinically used for the cure and prevention of circulatory organ diseases. Among them, an antagonism against calcium particularly inhibits inflow of calcium ions into cells, which is caused by excitation of a cell membrane of cardiac muscle or vascular smooth muscle, controls contraction of such muscle and promotes vasodilation. A calcium antagonist, therefore, is useful for the cure and prevention of hypertension, angina pectoris, cerebral circulatory disturbances and the like.
As typical examples of such a calcium antagonism, furnarizine clinically applied as a cerebral circulation accelerator, cinnarizine clinically applied as an angiotelectasis agent, and the like are known. However, development of a new medicament, which has an antagonism against calcium with less side effect, has still been desired.
Accordingly, an object of the present invention is to provide a novel compound which possesses an excellent antagonism against calcium and is useful as a drug, and a drug containing this compound for circulatory organs.
Under such circumstances, the present inventors have carried out extensive studies and have found that a novel diphenylpiperazine derivative represented by general formula (1) as described hereinafter and its salts possess a strong antagonism against calcium compared with furnarizine or cinnarizine conventionally used, a less toxicity and a high safety and is widely applicable as a drug for circulatory organs.
DISCLOSURE OF INVENTION
An object of the present invention is to provide a diphenylpiperazine derivative represented by the following general formula (1) or its salts and a drug for circulatory organs, containing this compound as an active ingredient: ##STR2## [wherein, R.sup.1 and R.sup.2 are the same or different and independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a nitro group, an amino group, a hydroxy group, an optionally esterified carboxyl group or a trifluoromethyl group; R.sup.3 represents a hydrogen atom, an alkyl group, an aralkyl group, an acyl group, a nitro group or an optionally esterified carboxymethyl group; Ar represents a phenyl or naphthyl group which may have 1 to 3 substituents such as halogen, alkyl, alkoxy, aryloxy, aralkyloxy, nitro, amino, cyano, acyl, hydroxy, optionally esterified carboxyl, substituted sulfonyl, aryl or trifluoromethyl; Z represents a sulfur atom or a group of -NR.sup.4 - (R.sup.4 represents a hydrogen atom, an alkyl group, an aralkyl group, an acyl group, an aryl group, a substituted sulfonyl group or an optionally esterified carboxyl group); m represents a number of 1 to 5; and n represents a number of 0 to 5.
BEST MODE FOR CARRYING OUT THE INVENTION
In the general formula (1), examples of the halogen atom include a fluorine atom, chlorine atom, iodine atom, bromine atom. Examples of the alkyl group include groups having 1 to 10 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, octyl, nonyl, decyl, cyclopentyl, and cyclohexyl. Examples of the alkoxyl group include groups having 1 to 8 carbon atoms such as methoxyl, ethoxyl, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy, cyclopentyloxy and cyclohexyloxy. Examples of the optionally esterified carboxyl group include alkoxycarbonyl groups such as methoxycarbonyl, ethoxycarbonyl, propyloxycarbonyl, and butyloxycarboxyl. Examples of the optionally esterified carboxymethyl group include methoxycarbonylmethyl, ethoxycarbonylmethyl and carboxylmethyl. Examples of the aralkyl group include benzyl, phenylethyl, methylbenzyl and naphthylmethyl. Examples of the acyl group include a
REFERENCES:
Godfraind et al., Pharmacological Reviews, vol. 38, No. 4, 1986, pp. 321-381.
Holmes et al., Drugs, vol. 27, 1984, pp. 6-44.
Toyoda et al., Journal of the Neurological Sciences, vol. 25, 1975, pp. 371-375.
Godfraind et al., Drugs of Today, vol. 18, No. 1, 1982, pp. 27-42.
Harada Kazunori
Inazu Masato
Katoh Tetsuo
Kawakatsu Nobuyuki
Kimura Makoto
Bernhardt Emily
Pola Chemical Industries Inc.
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