Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-07-01
1998-09-08
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544105, A61K 31535, C07D26536
Patent
active
058045805
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR94/01557, filed Dec. 29, 1995.
The subject of the present invention is benzoxazine derivatives, as well as methods for obtaining them. The invention also relates to the pharmaceutical compositions containing these derivatives, and their uses in particular in the treatment of pathologies associated with the presence of free radicals, and more particularly of Alzheimer's disease. 2,3,4,3',4',5'-hexahydroxy benzophenone, also called Exifone, was described in the French Patent published under the number 2,257,272 and filed under the number 74 01228 on 15th Jan. 1974, as a medicament which can be used in the treatment of diseases of the capillary circulatory system.
Exifone is described in the above-mentioned French Patent amongst a group of compounds having a protective action for the catecholamines which is put to good use in the treatment of diseases of the capillary circulatory system (arteries, veins), and of diseases resulting from a hemostasis disorder and/or platelet aggregation, in particular varicose and haemorrhoid diseases. In addition, some of the compounds described in this Patent, including Exifone, are presented as possessing anti-inflammatory properties and improve capillary resistance.
Exifone has subsequently been more particularly described in the Patent published under the number 2,377,202 and filed under the number 77 00706 on 12th Jan. 1977 as a certificate of addition to the above-mentioned French Patent No. 74 01228.
Exifone is described in this certificate of addition as being able to be used in the treatment of functional deficits and metabolic disturbances which result from a cerebral and/or peripheral circulatory insufficiency. The functional deficits and metabolic disorders which may be treated by Exifone and are mentioned in particular in this certificate of addition, are the following: insufficiency, either by vasoregulation of micro-circulation, or by improvement of cerebral oxygenation, and more particularly: after-effects of surgical operations (in particular cerebral oedema). hypacousia and tympanolabyrinthopexy, sclerosis,
More recently still, Exifone was described as being active in the treatment of Alzheimer's disease, notably due to its effects on the memory disorders, behaviour and dependency of patients suffering from Alzheimer-type senile dementia (Piette et al., La Revue de Geriatrie, Volume 11, No. 8, 1986).
However, the use of Exifone as a medicament encounters difficulties associated in particular with the poor solubility of Exifone in aqueous solvents, as well as its poor bioavailability, and due to strong links which form between the latter and the proteins in the body.
Furthermore, Exifone might be poorly tolerated, due in particular to a certain hepatotoxicity which might be observed in some patients.
The aim of the present invention is to provide new medicaments which can be used in the treatment of the group of pathologies mentioned above, and having an improved solubility, as well as a bioavailability superior to that of Exifone, whilst being better tolerated than the latter.
Another aim of the present invention is also to provide new processes for the preparation of these medicamnents.
The present in vention relates to the compounds corresponding to the following general formula (I): ##STR2## in which: R.sub.1 and R.sub.2, in dependently of each other, represent an alkyl group with 1 to 3 carbon atoms, or a group of formula --CH.sub.2 --OR.sub.a, R.sub.a representing a hydrogen atom or a methyl group, carbon atoms, in particular a methoxy group, or particular chlorine, or ##STR3## in which: R.sub.3 and R.sub.5, independently of each other, represent a hydrogen atom, or an --OH group, or an --OCH.sub.3 group, representing a hydrogen atom or a methyl group, or R.sub.4 represents a group of formula --OR.sub.c, R.sub.c representing a group of formula --CH.sub.2 --CO--C.sub.6 H.sub.4 R' in which R' represents a hydrogen atom, --CN or --OCH.sub.3, hydrogen atom or a methyl group, when R.sub.7 and R.sub.8 combine to form a double
REFERENCES:
patent: 4263322 (1981-04-01), van't Riet et al.
patent: 4956372 (1990-09-01), Kojima et al.
patent: 5124325 (1992-06-01), Kojima et al.
Fleury Maurice-Bernard
Largeron Martine
Maurette Jean-Marc
Laboratories Pharmascience
Raymond Richard L.
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