Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
1998-02-11
2002-10-22
Celsa, Bennett (Department: 1627)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S002600, C514S880000, C530S328000, C424S070100, C424S401000
Reexamination Certificate
active
06468972
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the use, as active principle, in a physiologically acceptable medium, in a cosmetic composition or for the preparation of a medicinal product, of an effective amount of at least one bradykinin antagonist which is intended to induce and/or stimulate hair growth and/or delay hair loss.
BACKGROUND OF THE INVENTION
In human beings, hair growth and its renewal are mainly determined by the activity of the hair follicles. Their activity is cyclical and comprises essentially three phases, namely the anagenic phase, the catagenic phase and the telogenic phase.
The active anagenic phase or growth phase, which lasts several years and during which the hair grows longer, is followed by a very short and transitory catagenic phase, which lasts a few weeks, and then by a resting phase, known as the telegenic phase, which lasts a few months.
At the end of the resting period, the hair falls out and another cycle recommences. The head of hair is thus constantly renewed and, of the approximately 150,000 hairs which a head of hair contains, at each instant, approximately 10% of them are at rest and will therefore be replaced in a few months.
In a significant number of cases, early hair loss takes place in subjects who are genetically predisposed to it and it affects men in particular. It is more particularly androgenetic in character or is referred to as androgenic alopecia or alternatively androgeno-genetic alopecia.
This alopecia is essentially due to a disturbance in hair renewal which results, at first, in an acceleration in the frequency of the cycles at the expense of the quality of the hair and then of its amount. A progressive thinning of the head of hair takes place by regression of the so-called “terminal” hairs to the downy stage. Regions are preferentially affected, in particular the temple or frontal bulbs in men and, in women, a diffuse alopecia of the vertex is observed.
The term alopecia covers a whole family of complaints of the hair follicle, whose final consequence is the partial or general permanent loss of the hair. Mention may be made, for example, of androgenic alopecia.
A search has been under way for many years in the cosmetic or pharmaceutical industry for substances which make it possible to suppress or reduce the effect of alopecia and in particular to decrease hair loss or to induce or to stimulate its growth.
In this perspective, a large number of very diverse active compounds have, admittedly, already been proposed, such as, for example 2,4-diamino-6-piperidinopyrimidine 3-oxide or “Minoxidil” described in U.S. Pat. No. 4,596,812, or alternatively the many derivatives thereof such as those described, for example, in patent applications EP 0,353,123, EP 0,356,271, EP 0,408,442, EP 0,522,964, EP 0,420,707, EP 0,459,890 and EP 0,519,819.
Mention may also be made of 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine and the derivatives thereof, which are described more particularly in patent U.S. Pat. No. 4,139,619.
BRIEF DESCRIPTION OF THE INVENTION
It generally remains that it would be advantageous and useful to have available active compounds other than those already known, that are potentially more active and/or less toxic.
Bradykinin is a peptide of plasma origin released from a kininogen precursor by a plasma protease known as kallikrein (EC 3.4.21.24). This nanopeptide is one of the key mediators of inflammation and has mitogenic properties. The receptors for this kinin are divided into two main subtypes, B1 and B2. Bradykinin acts in particular on the B2 receptor and causes the stimulation of many second messenger production systems including the hydrolysis of inositol phosphates, the metabolism of arachidonic acid, the phosphorylation of tyrosine residues and the depolarization or hyperpolarization of the cell membrane.
The activation of certain receptors causes the activation of phospholipase C and thus the production of inositol 1,4,5-triphosphate (IP3) and of diacylglycerol (DAG). IP3 is known to cause the release of calcium from intercellular storage sites in cells, including keratinocytes. Calcium is described as an activator and regulator of many enzymes (proteases, phospholipases) and plays an important part in regulating the differentiation and proliferation of keratinocytes.
Bradykinin is involved in a large number of physiopathological disorders including: hypotension, contraction of the smooth muscles the digestive and respiratory tracts and in the uterus, pain, the proliferation of connective tissue and the release of different inflammation mediators: cytokines, leukotrienes and prostaglandins.
To date, to the Applicant's knowledge, it has neither been envisioned or even suggested that bradykinin receptors exist in the hair follicle, nor that bradykinin plays a part in the phenomena resulting in hair loss and/or hair growth.
Surprisingly and unexpectedly, the Applicant has just discovered that Minoxidil, which is known for its effects on regrowth of the hair and on the storage and/or release of calcium by cells (Matsumoto et al., Nippon Hifuka Gakkai Zasshi (1993), 103(2), 103-15), blocks the increase in the calcium concentration of the intracellular medium induced by bradykinin. The Applicant has also shown that this is likewise the case for Minoxidil sulphate for which there is general agreement in the prior art that this is probably the active derivative of Minoxidil in regrowth of the hair in vivo.
Thus, Minoxidil or derivatives thereof can act as a bradykinin antagonist.
The term bradykinin antagonist is understood to refer to any compound which is capable of partially, or even totally, inhibiting the biological effect of bradykinin, except for the compounds known to have an effect on the storage and/or release of calcium in the cell, such as Minoxidil and derivatives thereof.
Particularly, for a substance to be recognized as a bradykinin antagonist, it must induce a coherent pharmacological response which may or may not include its binding to the bradykinin receptor.
Thus, any compound which can interfere with the effects of bradykinin by binding to the bradykinin receptor (B1 or B2) and/or any compound which, independently of binding to the receptor(s), will induce by whatever mechanism an effect contrary to that known for bradykinin (for example interfering with bradykinin synthesis) falls within this definition.
The use of a bradykinin antagonist can thus be one of the effective routes for controlling hair loss and/or for promoting regrowth of the hair.
This discovery forms the basis of the present invention.
Thus, the invention relates to the use, in a cosmetic composition or for the preparation of a medicinal product, of an effective amount of at least one bradykinin antagonist, this antagonist or the medicinal product being intended to induce and/or stimulate hair growth and/or slow down hair loss.
According to the invention, it is possible to use a single bradykinin antagonist or several together. For example, it is possible to use a release antagonist and/or a synthesis antagonist in combination with a B1 and/or B2 receptor antagonist, for example.
As has been pointed out above, according to the invention, the term bradykinin antagonist is understood to refer to any compound which is capable of partially, or even totally, inhibiting the biological effect of bradykinin, except for the compounds known to have an effect on the storage and/or release of calcium in the cell, such as Minoxidil and derivatives thereof.
Among the bradykinin antagonists, it is preferred to use, for example, compounds which inhibit the synthesis and/or accelerate the catabolism of bradykinin, brady-kinin neutralizers, bradykinin receptor blockers such as those which interfere with the effects of bradykinin by binding to its receptor (B1 or B2), compounds which inhibit the synthesis of bradykinin receptors or compounds involved in modulating the signal transduced by bradykinin. These compounds can be of natural or synthetic origin.
Among the bradykinin antagonists, mention may be made more par
Boyera Nathalie
Duranton Albert
Gautier Brigitte
Pruche Francis
Celsa Bennett
Societe L'Oreal S.A.
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