Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-07-26
1997-07-01
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 31535
Patent
active
056439075
DESCRIPTION:
BRIEF SUMMARY
This application is A-371 of PCT/PL94/00004 filed Jan. 24, 1994.
The present invention relates to the pharmaceutical composition, posessing psychotropic and especially anti-depressive activity, which can be used in the treatment of the central nervous system diseases and its functional disorders.
Psychotropic drugs known for their effects on the central nervous system are applicable in the therapy of psychical disorders and as assisting drugs in the treatment of other systems. According to their application the psychotropic drugs fall into five classes: neuroleptics, tranquilisers, anxiolytics, anti-depressants and nootropics. Depression affects in a varying degree ca 6% of the population. It is the result of interaction between the negative factors of the environment (stress) and the individual biochemical susceptibility, which is genetically conditioned. The biochemical basis for depression is related to the abnormal level of monoamines in the brain, particularly noradrenaline and serotonin (5-hydroxytryptamine). Hence the therapy of depression is focused on the question of increasing the level of monoamines in the brain. Very frequently applied in the therapy of depression are tri- and tetracyclic drugs. They produce an effect on wide range of neurotransmitters, including noradrenaline, serotonin, dopamine, histamine and acetylocholine. However, these drugs, due to their multidirectional action, have a number of side effects and can also cause an addiction. In the therapy of depression noncompetitive monoamine oxidase (MAO) inhibitors have been applied as well. MAO inhibitors, however, cause some metabolism disturbances of monoamines taken with food. This is why their application is reduced to the cases which do not react to other drugs.
The significant progress was the introduction of new serotonin re-uptake inhibitors. Their characteristic feature is high effectiveness and a smaller number of side effects. The chemical structure of these drugs considerably differs from the classical tri- and tetracyclic anti-depressants.
New drugs with anti-depressive effect have been searched in different chemical classes.
In the patent application number DE 4005371 the derivatives of N-aryl-2-piperidinoethyl-2-oxazolidinone and the pharmaceutical compositions containing them were disclosed. It was stated that those agents showed the effect on the central nervous system, particularly sedative, tranqulising, neuroleptic and anti-depressive effects.
The derivatives of 3-aryl-4-piperidinoalkil-2-oxazolidinone and pharmaceutical compositions containing them are known from the european patent application number EP 459256. They show central nervous system activity, particularly sedative, tranquilising, neuroleptic and anti-depressive activity.
According to the invention there is provided a pharmaceutical composition, which contains as the active substance 5-morpholinomethyl-3-(4-chlorobenzylideneamine)-2-oxazolidinone of formula I ##STR1## and/or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and optionally at least one auxilliary substance.
The pharmaceutical composition according to the invention contains an active substance in its free form or in the form of pharmaceutically acceptable salt, particularly acid addition salt. These can be salts with inorganic acids, such as hydrochloric, hydrobromic, phosphoric acid and organic acids, such as for example formic, acetic, propionic, malonic, citric, lactic, tartaric, gluconic, nicotinic, methane--or ethanesulphonic, ascorbic, naphthalenesulphonic and fumaric acid.
In the preferred embodiment the pharmaceutical composition according to the invention contains as the active substance 5-morpholinomethyl-3-(4-chlorobenzylideneamine)-2-oxazolidinone hydrochloride.
A further aspect the present invention relates to the use of 5-morpholinomethyl-3-(4-chlorobenzylideneamine)-2-oxazolidinone of formula I given above or pharmaceutically acceptable salt thereof for the preparation of a medicament having central nervous system activity.
Another aspect
REFERENCES:
patent: 5232931 (1993-08-01), Prucher
Swirska, A. `Hypotensive derivatives of . . . ` Chemical Abstracts, vol. 60, No. 4, (1964), Columbus, Ohio, US; abstract No. 4137.
Acta Polon. Pharm., vol. 19, No. 4, (1962), pp. 317-324.
Kessler, H.-J., et al., `Chemotherapeutische Nitro-heterocyclen XXI . . . ` Eur. J. Med. Chem. vol. 11, No. 1, 1976, pp. 19-23.
Alicja Swirska, "5-Morpholinomethylo-3-Amino-2-oxazolidone Derivatives with Hypotensive Activity," Acta Polon. Pharm., vol. 19, No. 4, 1962: 317-324.
Patent Abstracts of Japan, vol. 1, No. 120 (C-77) (2765) 12 Oct. 1977 & JP,A,52 078 881 (Sumitomo Kagaku Kogyo K.K.) 7 Feb. 1977.
Bogdal Maria
Grzeszkiewicz Andrzej
Kobylinska Maria
Krzywosinski Leszek
Serwin-Krajewska Marta
Henley III Raymond
Instytut Farmaceutiyczny
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