Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-12
2000-05-23
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514422, 514662, A61K 31445, A61K 3140, A61K 3113
Patent
active
060666528
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The invention relates to the use of adamantane derivatives of the formula ##STR2##
in which R1 and R2 branched alkyl groups having 1 to 6 carbon atoms, or or 6 ring atoms,
in which R3 and R4 are identical or different and can be hydrogen, straight-chained or branched alkyl groups having between 1 and 6 carbon atoms, cycloalkyl groups having 5 or 6 carbon atoms or a phenyl group, and in which R5 is hydrogen or a straight-chained or branched alkyl group having between 1 and 6 carbon atoms.
BACKGROUND OF THE INVENTION
The use of adamantane derivatives falling under the cited general formula I for the therapy of certain diseases is already known. Thus, for instance, the dopamine-related influence of amantadine (1-adamantanamine) is described in a series of publications. Also an antiviral effect of certain amino-adamantanes has been demonstrated. In addition, EP B1-392059 shows the use of adamantane derivatives in preventing and treating cerebral ischaemia. According to this publication adamantane derivatives having the formulua I as described above can protectively prevent destruction of brain cells following an ischaemia, the adamantane derivatives being employed as antagonists for the NDMA receptor channels of the nerve cells. In EP-B1-392059 both general and special methods of producing adamantane derivatives falling under the above-cited formula I are described.
The publication by Ehrenberger and Felix in Acta Otalarygnol (Stockholm) 1995; 115: 236-240 concerns neurotransmission between the inner hair cell of the inner ear and the afferent neuron. An attempt is made to explain certain illnesses of the inner ear in a model by a so-called glutamate neurotoxicity, it being indicated in this context to use antagonists which block the glutamate link of the postsynaptic membrane. It is in this context that it is also termed conceivable to use antagonists for the glycine link, the redoxmodulating location or for the NMDA receptor complex, for example an adamantane derivative. The quinoxaline derivate caroverine tested in the Ehrenberger and Felix publication fails to produce any satisfactory results in the treatment of tinnitus thought to be induced by a glutamate, however.
At the same time it is to be realized that diseases of the inner ear are widespread, especially as regards diseases or disturbances in which subjective noise in the ear, so-called tinnitus occurs. It is estimated that in Germany alone roughly 6 million people suffer from tinnitus. In roughly 800,000 cases the tinnitus is so pronounced that these patients need intensive treatment by a physician, due to the patient being seriously handicapped by tormenting ear noise. At this time no reliable therapy is available.
As regards the complexity of inner ear diseases, especially in the case of tinnitus which is still to be conclusively explained, a series of medicamentous therapies has been proposed hitherto. These include, in addition to the use of anaesthetica, for example the application of lidocaine-type antiarrhythmica or anticonvulsiva, e.g. carbamazepine. However, in most cases treatments of this kind fail to bring satisfactory results. In-patient infusion therapy with procaine appears to be the sole form of tinnitus therapy which is superior to a placebo, albeit only to a minor degree. Here too, the effect is only temporary, however.
SUMMARY OF THE INVENTION
The object of the invention is thus to define a possibility of treating diseases of the inner ear, more particularly in the case of tinnitus, with which a perceptible compensation of the symptoms associated with the disease is achieved. More particularly, the tormenting ear noise is made to disappear or diminished to such a degree that the patient reattains his normal quality of life.
This object is achieved by the use of formulua I adamantane derivatives as claimed. It has been surprisingly discovered that, more particularly, tinnitus can be effectively compensated by use of the compounds cited. Further fields of application may materialize in the treatment of chroni
REFERENCES:
patent: 3328251 (1967-06-01), Smith
patent: 4331686 (1982-05-01), Djurickovic
patent: 5061703 (1991-10-01), Bormann et al.
H. Spoendlin: Ohr, 1990, pp. 875-878, "Allgemeine Pathologie und Pathologische Anatomie" by Max Eder et al.
Acta Otolaryngol, Bd. 115, Nr. 2, Mar. 1995, pp. 236-240 "Receptor Pharmacological Models for Inner Ear Therapies with Emphasis on Glutamate Receptors: A Survey" by K. Ehrenberger et al.
Otorhinolaryngol, Nova Bd. 5, Nr. 3-4, Mai 1995--Aug. 1995, pp. 148-152 "Rezeptorpharmakologische Modelle fur eine siehe das ganze Dokument".
Busch Andreas
Ruppersberg J. Peter
Zenner Hans Peter
Fay Zohreh
Tinnitus Forschungs-und Entwicklungs GmbH
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