Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-02-14
2002-04-23
Criares, Theodore J. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06376498
ABSTRACT:
OBJECT OF THE INVENTION
The present invention relates to a pharmaceutical, cosmetic and/or foodstuff composition intended in particular for the prevention and/or treatment of diseases associated with pro-oxidizing agents.
The present invention also relates to the use of the pharmaceutical, cosmetic and/or foodstuff composition according to the invention.
TECHNOLOGICAL BACKGROUND AND PRIOR ART
Patent Application WO96/28160 describes a pharmaceutical, cosmetic and/or foodstuff composition having antioxidizing properties and comprising a pyrazine derivative or a precursor thereof, the derivatives being imidazolopyrazines, such as coelenterazine.
This document also describes the use of such a pharmaceutical, cosmetic and/or foodstuff composition for treatment of diseases associated with the action of pro-oxidizing agents, such as inflammatory diseases, or the use of the said composition for treatment of cancerous tumours.
Antioxidizing molecules, such as vitamins, such as vitamin E (soluble in lipids), or cysteine derivatives (soluble in water) have also already been used in cosmetic, pharmaceutical and/or foodstuff applications. However, such antioxidizing molecules are characterized either by a low solubility in water or by a high toxicity, by too low an efficacy or by a low stability with respect to oxygen.
OBJECT OF THE INVENTION
The object of the present invention is to obtain a pharmaceutical, cosmetic and/or foodstuff composition which allows bonding of pro-oxidizing agents and should not have the disadvantages of the prior art.
A particular object of the present invention is to obtain a pharmaceutical, cosmetic and/or foodstuff composition advantageously allowing the prevention and/or treatment of diseases associated with pro-oxidizing agents.
Another object of the present invention is to provide a pharmaceutical, cosmetic and/or foodstuff composition which is characterized by an improved stability with respect to products of the prior art, by a low toxicity or an absence of toxicity, and by a significant solubility in a large number of solvents and/or lipids.
Characteristic Elements of the Present Invention
The present invention relates to a pharmaceutical, cosmetic and/or foodstuff composition comprising a pyrazine derivative of the formula
in which the radicals R
1
to R
9
are H, radicals chosen from the group consisting of alkyl, alkenyl, alkinyl, aryl, arylalkyl, alkylaryl, heteroaryl, heteroalkyl and hetero-(alkylaryl and arylalkyl), preferably having 1 to 20 carbon atoms and optionally containing 1 to 10 heteroatoms, the carbon atoms of which can optionally be substituted by any element of the Mendeleev table, preferably an element chosen from the group consisting of H, B, N, O, F, P, S, Cl, As, Se, Br, Te and I, or chains of the formula (R
5
×R
6
)
n
, where n≧1, x represents one or more heteroatoms and R
5
and R
6
are radicals chosen from the group consisting of alkyl, alkenyl, alkinyl, aryl, arylalkyl, alkylaryl, heteroaryl, heteroalkyl and hetero-(alkylaryl and arylalkyl) having 1 to 20 carbon atoms and optionally containing 1 to 10 heteroatoms, the carbon atoms of which can optionally be substituted by any element of the Mendeleev table, preferably an element chosen from the group consisting of H, B, N, O, F, P, S, Cl, As, Se, Br, Te and I; and optionally a suitable pharmaceutical, cosmetic and/or foodstuff vehicle.
Preferably, in the pyrazine derivative according to the invention, the radicals R
2
to R
9
are H and the radical R
1
is a radical of the formula
and optionally a suitable pharmaceutical, cosmetic and/or foodstuff vehicle.
Another aspect of the present invention relates to the use of the composition according to the invention for bonding pro-oxidizing agents (activated forms of oxygen), such as peroxides, superoxides etc.
The present invention also relates to a process for bonding pro-oxidizing agents in which the pharmaceutical, cosmetic and/or foodstuff composition is brought into contact with the said pro-oxidizing agents.
The present invention also relates to a process for treatment and/or prevention of diseases associated with the action of pro-oxidizing agents, in particular inflammatory diseases, and a process for treatment and/or prevention of atherosclerosis, in which the pharmaceutical, cosmetic and/or foodstuff composition according to the present invention is administered to a patient (human or animal).
In the said processes, the pharmaceutical, cosmetic and/or foodstuff composition is combined with a therapeutic effect. However, the said composition can also be characterized as being a “functional” foodstuff composition.
A “functional foodstuff composition” is characterized in that it comprises one or more ingredients which are capable of having a beneficial physiological effect on the consumer, such as the prevention of an illness, the treatment of an illness or the activation of biorhythm or the immune system. Such a functional foodstuff composition can be incorporated into the normal diet of the consumer such that a general improvement in the health of the patient is obtained, or to obtain treatment or prevention of a particular illness, in as much as the said functional foodstuff composition has a significant effect on the consumer from both the preventive and the therapeutic point of view.
The said pharmaceutical, cosmetic and/or foodstuff composition will comprise a sufficient amount of the pyrazine derivative according to the invention to obtain a prevention or a significant therapeutic effect on the consumer.
The proportion of pyrazine derivative according to the invention in the pharmaceutical, cosmetic and/or foodstuff composition according to the invention will vary as a function of the daily amounts of the product absorbed, in accordance with suitable foodstuffs, cosmetics and pharmaceuticals legislation, sensory considerations and the secondary effects which may exist with the derivatives according to the invention and/or their pharmaceutical, cosmetic and/or foodstuff vehicles used.
The pharmaceutical, cosmetic and/or foodstuff vehicles of the compositions according to the invention are suitable vehicles in particular for oral administration, for example in the form of coated or non-coated tablets, pills, capsules, solutions, essential oils and/or syrups.
Other suitable pharmaceutical, cosmetic and/or foodstuff vehicles can be used, depending on the mode of administration chosen.
In particular, these pharmaceutical, cosmetic and/or foodstuff vehicles can be sun creams or oils well-known to the person skilled in the art, which may be smeared over various areas of the human or animal body in combination with other skin-protection agents.
In addition, the products of the invention can easily be incorporated into solvents (aqueous media, alcohols etc.) or lipids (for example in combination with foodstuff oils or sun-tanning oils).
The pharmaceutical, cosmetic and/or foodstuff compositions according to the invention are prepared by processes generally used by the person skilled in the art, in particular by pharmacists, and can comprise any pharmaceutically suitable, solid or liquid non-toxic vehicle or additive.
Incorporation of the derivatives according to the invention into a galenical medium may also be envisaged.
The percentage of active product (pyrazine derivative) in the pharmaceutical, cosmetic and/or foodstuff vehicle can vary within very wide ranges, which are generally limited by the tolerance and the level of acceptance of the composition by the consumer.
The limits are generally determined by the frequency of consumption of the composition by the consumer.
A last aspect of the present invention relates to the use of the composition according to the invention for the preparation of a medicament intended for prevention and/or treatment of diseases associated with the action of pro-oxidizing agents.
In particular, the present invention relates to the use of the composition according to the invention for the preparation of a medicament intended for prevention and/or treatment of inflammatory or carcino
Dubuisson Marléne
Rees Jean-Francois
Trouet Andre
Criares Theodore J.
Kim Jennifer
Knobbe Martens Olson & Bear LLP
Universite Catholique de Louvain
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