Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-12-21
1998-05-05
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31495
Patent
active
057474931
DESCRIPTION:
BRIEF SUMMARY
The present application is a 371 of PCT/JP94/00728, filed Apr. 28, 1994.
1. Technical Field
The present invention relates to a dopamine re-uptake inhibitor, which is safe and high in efficacy, and a therapeutic agent for Parkinson's syndrome.
2. Background Art
Dopamine (hereinafter referred to as DA) is one of principal neurotransmitters having various physiological functions in central and peripheral nervous systems. The central dopaminergic has been known to play many roles in the motor function in an extrapyramidal system, the emotional control in a limbic system and the secretion of hormones in a pituitary system. Therefore, DA deficiency and decrease in the dopaminergic nerve activity form the cause of critical diseases.
For example, Parkinson's syndrome is a disease mainly showing a symptom that involuntary labile movement is often manifested. This disease is said to be caused by the disorder of a dopaminergic transmission system caused by the deficiency of catecholamines, in particular, DA.
For example, the DA deficiency has also been known to be one of causes of a psychosis accompanied by the reduction in spontaneous movement.
For such diseases caused by the DA deficiency, agents such as amantadine for accelerating the release of DA toward a nerve ending, agents such as biperiden for recovering the collapsed balance between a DA system and an acetylcholine system, which may be caused by antagonizing acetylcholine, and agents such as bromocriptine for binding to a DA receptor to manifest DA-like action so as to supply the deficiency of DA have been already marketed for use. However, while these agents are able to relieve the condition of a patient to some extent, neither of them are able completely cure the condition. In addition, they have side effects such as vertigo and headache to a considerable extent and hence have been not fully satisfactory.
It is accordingly an object of the present invention to provide a neurergic agent which does not produce any side effect, is safe and has potent activities of inhibiting DA re-uptake.
With the foregoing circumstances in view, the present inventors have carried out an extensive investigation. As a result, it has been found that a compound represented by the general formula (1), which will be described subsequently, is safe and has an excellent effect of inhibiting DA re-uptake, thus leading to completion of the present invention.
DISCLOSURE OF THE INVENTION
The present invention is related to a DA re-uptake inhibitor comprising a compound represented by the following general formula (1) or a physiologically acceptable salt thereof as an active ingredient: ##STR2## wherein R.sup.1 and R.sup.2 may be identical with or different from each other and mean individually a hydrogen or halogen atom, R.sup.3 denotes a hydrogen atom, or an alkyl or acyl group, R.sup.4 represents a hydrogen atom, or an alkyl, acyl, alkylsulfonyl or optionally esterified carboxyl group, Ar means a phenyl or nitrogen-containing monocyclic heteroaromatic group which may have 1 to 3 substituents selected from halogen atoms, and alkyl, alkoxy, nitro, amino, alkylamino and hydroxyl groups, m stands for a number of 1 to 5, and n stands for a number of 0 to 5.
The present invention is also related to a therapeutic agent for Parkinson's syndrome comprising the compound represented by the general formula (1) or the physiologically acceptable salt thereof as an active ingredient.
BEST MODE FOR CARRYING OUT THE INVENTION
In the compound useful in the practice of the present invention, which is represented by the general formula (1), with respect to the groups indicated by R.sup.3, R.sup.4 or Ar in the formula, the alkyl group is preferably that having 1-4 carbon atoms, the acyl group is preferably an alkylcarbonyl group having 1-4 carbon atoms, the alkylsulfonyl group is preferably that having a C.sub.1-4 alkyl group, the alkoxy group is preferably that having 1-4 carbon atoms, the alkylamino group is preferably that having a C.sub.1-4 alkyl group and the nitrogen-containing monocyclic het
Harada Kazunori
Inazu Masato
Kawakatsu Nobuyuki
Kimura Makoto
Kishii Kenichi
Pola Chemical Industries Inc.
Spivack Phyllis G.
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