Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-03-02
1994-04-19
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514252, 544360, 544361, 544363, A61K 31495, C07D21152, C07D21704, C07D40100
Patent
active
053045580
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to novel diphenylmethyl piperazine derivatives, in particular novel diphenylmethyl piperazine derivatives having an effect of inhibiting overcontraction and overextension of the myocardium and protecting against myocardial necrosis without being accompanied by a cardiodepressant effect.
In addition, this invention relates to drugs containing the aforementioned novel diphenylmethyl piperazine derivatives as an effective ingredient which work on the circulatory system, in particular, drugs containing the novel diphenylmethyl piperazine derivatives as an effective ingredient which inhibit myocardial necrosis and which inhibit overcontraction and overextension of myocardium and protect against myocardial necrosis without being accompanied by a cardiodepressant effect, and drugs containing the same for treatment and prevention of acute myocardial infarction.
BACKGROUND ART
The recent increase in the average age of the population has been accompanied by an increase in circulatory diseases, such as hypertension, angina and myocardial infarction. In particular, there have been many sudden occurrences of acute myocardial infarction with a high mortality rate. Hitherto, the cause of this acute myocardial infarction has been attributed to obstruction, by thrombus or coronary spasm, of the coronary antery which supplies nutrition to the heart. Recently, however, Kaneko et al. have proposed a new mechanism for acute myocardial infarction, according to which the myocardia of myocardial infarction patients exhibit two forms of necrosis, Static cell death (SD) and Kinetic cell death (KD), with KD being the main cause of acute myocardial infarction. (Journal of Tokyo Women's Medical College, 52, 1443, 1982). In addition, Kaneko et al. have reported using a rabbit to create a model of an acute myocardial infarction caused by KD, and using calcium antagonists to inhibit the symptoms thereof (refer to Japanese Patent Application No. Sho 61-40651). Moreover, they have recently succeeded in creating a model of an acute myocardial infarction caused by KD in a Langendorff in vitro system using an isolated rat heart, and using this model they have found that some Ca antagonists have a KD-inhibiting effect similar to that found in the in vivo system. However, some of these Ca antagonists have a strong cardiodepressant effect, and it was thought desirable to develop compounds having a weak cardiodepressant effect, and a strong KD-inhibiting effect.
DISCLOSURE OF THE INVENTION
It is an object of this invention to provide compounds having the above-mentioned KD-inhibiting effect without being accompanied by a cardiodepressant effect, and to provide drugs containing the compounds as an effective ingredient for inhibition of myocardial necrosis and treatment and prevention of acute myocardial infarction.
In addition, it is an object of this invention to provide not only novel diphenylmethyl piperazine derivatives having a KD-inhibiting effect without any accompanying cardiodepressant effect, particularly novel diphenylmethyl piperazine derivatives having specific substituent groups and pharmaceutically acceptable salts thereof, but also to provide drugs for the inhibition of myocardial necrosis and for the treatment and prevention of acute myocardial infarction in which the above novel diphenylmethyl piperazine derivatives having specific substituent groups and pharmaceutically acceptable salts thereof are contained as effective ingredient.
Namely, the compounds of this invention are diphenylmethyl piperazine derivatives having a chemical structure represented by the following Formula [I]: ##STR3## wherein R represents ##STR4## or pharmaceutically acceptable salts thereof.
Moreover, the drugs of this invention for the inhibition of myocardial necrosis and for the treatment and prevention of acute myocardial infarction contain as an effective ingredient one or more of the diphenylmethyl piperazine derivatives having a chemical structure represented by Formula [I] above or pharmaceutically acc
REFERENCES:
patent: 4832934 (1983-05-01), Teraji et al.
Akimoto Kouji
Kaneko Noboru
Nakajima Tatsuo
Oosawa Tatsushi
Oota Hideo
Kirin Brewery Co. Ltd.
Tsang Cecilia
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