Modulating body/cranial hair growth

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing

Reexamination Certificate

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C514S169000, C514S712000, C514S715000, C514S717000, C514S880000, C548S100000, C562S400000, C424S070100, C554S001000

Reexamination Certificate

active

06465421

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention generally relates to modifying the growth of body and/or head hair, and, more especially, to a treatment which, depending essentially on the nature of the compositions employed therefor, permits either promoting the growth and/or limiting the loss of body and/or head hair, or, contrariwise, reducing or preventing the growth of this hair.
The present invention also relates to such compositions, per se, and specific hair growth-modulating applications thereof.
2. Description of the Prior Art
It is known to the art that certain polyunsaturated fatty acids, in particular those containing 20 carbon atoms, such as arachidonic acid, dihomo-&ggr;-linolenic acid, or, alternatively, eicosapentaenoic acid, may be converted, in vivo, under the action or influence of certain specific enzymes present in living cells, in particular in epithelial cells, into certain other compounds of eicosanoid type which are useful to the organism.
Thus, it too is known that the enzymes designated cyclooxygenases generate, from the various fatty acids indicated above, eicosanoids of prostaglandin and thromboxane type, and that the enzymes designated lipoxygenases are themselves responsible for the formation of eicosanoids of leukotriene type and other hydroxylated acyclic acids containing 20 carbon atoms. This same specific polyunsaturated fatty acid (or substrate) may initiate, depending on the nature of the enzyme with which it is first reacted, the formation of several different metabolites, for example prostaglandins and leukotrienes.
Polyunsaturated fatty acids, in particular C
20
acids (reactive starting materials), which are known to be metabolized under the specific action of the cyclooxygenase and lipoxygenase enzymes, are generally supplied to the living organism via certain foods, in particular certain natural oils of animal or vegetable origin. This food supply may either be in a direct form (which is, for example, the case for arachidonic acid, which is present as is in egg whites), or indirectly in the form of precursor compounds (compounds which are also deemed “essential fatty acids,” themselves generally C
18
-C
22
unsaturated fatty acids, such as linoleic acid, &agr;-linolenic acid and &ggr;-linolenic acid) which are converted via human metabolism, according to complex mechanisms which will not be repeated here, into suitable substrates (namely, metabolizable) for cyclooxygenases and lipoxygenases.
SUMMARY OF THE INVENTION
After considerable research efforts, it has now unexpectedly and surprisingly been found that the enzymatic conversions described above, and the various reaction products resulting therefrom, exert a significant influence on the mechanisms for the growth of body and/or head hair; thus, by favoring (according to techniques more fully described below) one or the other of the two cyclooxygenase or lipoxygenase enzymatic cascades in skin cells, it has now surprisingly been determined that the growth of body and/or head hair can be substantially modified.
Briefly, the present invention features promoting the growth of body and/or head hair and/or combatting the loss of such hair via cyclooxygenase treatment, as well as, contrariwise, retarding and/or preventing the growth of body/cranial hair via lipoxygenase treatment.
DETAILED DESCRIPTION OF BEST MODE AND PREFERRED EMBODIMENTS OF THE INVENTION
More particularly according to the present invention, from a practical standpoint, eliciting one or the other enzymatic response can be carried out via several different techniques, more fully described below. Each such technique is bottomed on the same basic principle, namely, to supply the organism, in particular the skin cells thereof, with compounds intended either to inhibit or, to the contrary, to stimulate the action or influence of cyclooxygenase or lipoxygenase enzymes, the selection of which obviously being made depending on the particular pharmacological effect sought to be attained.
Thus, if it is desired to promote the growth and/or to limit the loss of body and/or head hair (or conversely, if it is desired to retard and/or to prevent the growth of such hair), and taking account of the fact that it is appropriate, in this instance, as indicated above, to favor the cyclooxygenase route (or, conversely, to favor the lipoxygenase route), it is then possible to adopt, as desired, at least one of the following techniques: either employing one or more lipoxygenase inhibitors (or, conversely, one or more cyclooxygenase inhibitors), or employing one or more cyclooxygenase stimulators or agonists (or, conversely, one or more lipoxygenase stimulators or agonists), or employing one or more lipoxygenase inhibitors (or, conversely, one or more cyclooxygenase inhibitors) in combination with one or more cyclooxygenase stimulators or agonists (or, conversely, one or more lipoxygenase stimulators or agonists), or, alternatively, employing one or more active agents having the property of being both lipoxygenase inhibitors (or, conversely, cyclooxygenase inhibitors) and cyclooxygenase stimulators or agonists (or, conversely, lipoxygenase stimulators or agonists) simultaneously.
Stated differently, it is thus possible to elicit a given enzymatic response by direct stimulation of one particular route and/or via inhibition of the “contrary” route. The best results are typically attained by combining the two routes.
The present invention also features, both in a therapeutic regimen for promoting the growth of body and/or head hair and in a competing therapeutic regimen for limiting such hair growth, whether employing said inhibitors and stimulators or agonists of the aforesaid enzymatic routes, combining therewith treatment with at least one substrate which is directly metabolizable by lipoxygenases and cyclooxygenases and or with at least one precursor of said at least one substrate (synergistic or superadditive effect).
As utilized herein, by the term “substrate” suitable for lipoxygenase and cyclooxygenase is intended any substance which may be metabolized directly, as is in vivo, both by lipoxygenase enzymes and cyclooxygenase enzymes.
By the term lipoxygenase and cyclooxygenase substrate “precursor” is intended any substance which may be metabolized in vivo by the organism into a suitable substrate for lipoxygenases and cyclooxygenases, as well as any substance inducing the formation of polyunsaturated fatty acids in living tissues (this may be determined by gas chromatography or by any other standard technique, such as those described by Pelick et al, P23 “Analysis of lipids and lipoproteins”, Perkin's American Oil Chemist Society editions, Champaign, Ill., U.S.A.).
By the term lipoxygenase and cyclooxygenase “inhibitor” is intended any substance which makes it possible, in vivo, to limit or to inhibit totally the enzymatic activity of one or the other of the aforesaid enzymes.
By the term lipoxygenase and cyclooxygenase “stimulator” or “agonist” is intended any substance which elicits, in vivo, an increase in the enzymatic activity of one or the other of these enzymes, the term “agonist” being included in the general designation “stimulator”.
By “topical route” is intended any conventional technique for administration of an active agent by direct application thereof to a superficial (or external) parts of the body, such as skin, hair, etc.
And by “systemic route” is intended any conventional technique for administration of an active agent into the circulation via a route other than the topical route, for example, via the oral and/or parenteral route.
Thus, in a first embodiment of the present invention, an in vivo regimen is provided for modifying the growth of body and/or head hair, such regimen comprising administering to a mammalian organism, notably a human being, via a topical and/or systemic route, at least one lipoxygenase or cyclooxygenase inhibitor, or at least one lipoxygenase or cyclooxygenase stimulator or agonist.
In the event that the subject regimen/treatment is more particularly intended t

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