WO2007068577A1 - Use of naveglitazar for preparing a pharmaceutical composition for use in the treatment of dermatological conditions - Google Patents
Use of naveglitazar for preparing a pharmaceutical composition for use in the treatment of dermatological conditions Download PDFInfo
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- WO2007068577A1 WO2007068577A1 PCT/EP2006/068970 EP2006068970W WO2007068577A1 WO 2007068577 A1 WO2007068577 A1 WO 2007068577A1 EP 2006068970 W EP2006068970 W EP 2006068970W WO 2007068577 A1 WO2007068577 A1 WO 2007068577A1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- the present invention relates to the field of skin treatment.
- the invention aims to provide novel pharmaceutical compositions, and more particularly dermatological compositions, in particular for the treatment of dermatological conditions, particularly for the treatment of acne and / or psoriasis, comprising a compound of formula (I) as a that active agent.
- Psoriasis is a chronic inflammatory skin disease affecting about 5% of the French population. This disease can be manifested by red patches covered with whitish films that are detached from the skin: these are the dander. Psoriasis plaques are often located on the elbows, scalp and knees, but can also reach other parts of the body such as the face, hands, feet and mucous membranes. Psoriasis can occur at any age, however the first flares appear mostly between 10 and 30 years of age. It is a chronic disease whose evolution is unpredictable: in phases of recurrence succeeds phases of remission. While this disease rarely endangers a person's life, it can have a strong impact on their quality of life, given its unsightly appearance and chronicity. Some people have a single plaque of psoriasis located in a specific area of the body while others are prone to extensive psoriasis throughout the body.
- Acne also affects a large part of the population. It frequently causes unsightly lesions that can in some cases be durable. These lesions can have a significant impact on the quality of life, both in terms of discomfort and aesthetics.
- compositions intended for the treatment of dermatological conditions in particular psoriasis and / or acne, which make it possible to at least partially solve the problems mentioned above.
- composition allows the treatment of dermatological conditions, in particular psoriasis and / or acne.
- the subject of the invention is the use of at least one compound chosen from the compound corresponding to the following formula (I):
- optical isomers in particular the enantiomeric forms of the compound of formula (I).
- the carrier carbon of the methoxy group at the 2-position of propanoic acid is asymmetric, and can therefore be of R or S configuration, which corresponds to the two possible enantiomers of the molecule.
- pharmaceutically acceptable salt in particular an alkali metal salt, or an alkaline earth salt, or an organic amine salt.
- compositions according to the invention may be suitable for prevention and / or treatment: 1) at least one dermatological disorder related to a disorder of keratinization relating to differentiation and proliferation, in particular chosen from the group comprising vulgar, comedonal, polymorphic acne, nodulocystic acne, conglobata, senile acnes, secondary acne, such as solar acne, medicated or occupational, rosacea, and / or
- At least one dermatological condition with an inflammatory immunoallergic component with or without a cell proliferation disorder, especially chosen from the group comprising psoriasis, in particular cutaneous, mucous or ungual, or even psoriatic arthritis, or cutaneous atopy, such as eczema or respiratory atopy or gingival hypertrophy.
- At least one disorder of the sebaceous function especially chosen from the group comprising acne hyperseborrhoea, simple seborrhea, or seborrheic dermatitis.
- the administration of the pharmaceutical composition according to the invention may be carried out orally, parenterally, topically or ocularly.
- the pharmaceutical composition is packaged in a form suitable for topical application.
- the composition may be in the form of tablets, capsules, dragees, syrups, suspensions, solutions, powders, granules, emulsions, microspheres or nanospheres. or lipid or polymeric vesicles for controlled release.
- the composition may be in the form of solutions or suspensions for infusion or injection.
- the compounds according to the invention are generally administered at a daily dose of about 0.001 mg / kg to 100 mg / kg of body weight, in 1 to 3 doses.
- the compounds are used systemically at a concentration generally of between 0.001 and 10% by weight, preferably between 0.01 and 1% by weight, relative to the weight of the composition.
- the pharmaceutical composition according to the invention is more particularly intended for the treatment of the skin and mucous membranes and may be in the form of ointments, creams, milks, ointments, powders, soaked swabs, syndets, solutions, gels, sprays, foams, suspensions, stick lotions, shampoos, or washing bases. It may also be in the form of suspensions of microspheres or nanospheres or lipid or polymeric vesicles or polymeric patches and hydrogels allowing controlled release.
- This topical composition may be in anhydrous form, in aqueous form or in the form of an emulsion.
- the composition may comprise a content of compound of formula (I), its isomers and / or its salts ranging from 0.001 to 10% by weight, especially from 0.01 to 5% by weight relative to the total weight of the composition.
- the composition further comprises at least one other agent capable of increasing the effectiveness of the treatment or of reducing certain undesirable effects.
- This agent may be chosen from the group comprising antibiotics, antibacterials, antivirals, antiparasitics, antifungals, anesthetics, antiallergics, retinoids, anti-free radicals, antipruritic agents, keratolytics, antiseborrhoeics, antihistamines, immunosuppressive and antiproliferative products.
- the composition may also comprise at least one additive usually used in the pharmaceutical and dermatological field, compatible with the compound of formula (I), its optical isomers and its salts.
- the additive may be selected from the group consisting of sequestering agents, antioxidants, sunscreens, preservatives, especially DL-alpha-tocopherol, fillers, electrolytes, humectants, dyes, bases or usual acids, minerals or organic, fragrances, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, especially DHA, soothing and protective agents for the skin, such as allantoin, propenetrating agents, gelling agents and mixtures thereof.
- these optional compound (s) complement (s) such that the advantageous properties of the composition according to the invention are not, or substantially not, altered.
- the composition may comprise from 0.0001 to 20% by weight, especially from 0.01 to 10% by weight, and in particular from 0.1 to 5% by weight of additive relative to the total weight of the composition.
- sequestering agents mention may be made of ethylenediamine tetracetic acid (EDTA), as well as its derivatives or its salts, dihydroxyethylglycine, citric acid, tartaric acid, and mixtures thereof.
- the preservative may be selected from the group consisting of benzalkonium chloride, phenoxyethanol, benzyl alcohol, diazolidinyl urea, parabens, and mixtures thereof.
- Humectants include glycerin and sorbitol.
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Abstract
The invention relates to the use of at least one compound chosen from 2-methoxy-3-[4-[3-(4-phenoxyphenoxy)propoxy]phenyl]propanoic acid, one of its isomers, in particular optical isomers, and/or its pharmaceutically acceptable salts, for preparing a pharmaceutical composition for use in treating dermatological conditions.
Description
UTILISATION DU NAVEGLITAZAR POUR LA PRÉPARATION D'UNE USE OF NAVEGLITAZAR FOR THE PREPARATION OF
COMPOSITION PHARMACEUTIQUE DESTINÉE AU TRAITEMENT DESPHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF
AFFECTIONS DERMATOLOGIQUESDERMATOLOGICAL DISEASES
La présente invention concerne le domaine du traitement de la peau. L'invention vise à fournir de nouvelles compositions pharmaceutiques, et plus particulièrement dermatologiques, en particulier pour le traitement des affections dermatologiques, tout particulièrement pour le traitement de l'acné et/ou du psoriasis, comprenant un composé de formule (I) en tant qu'agent actif.The present invention relates to the field of skin treatment. The invention aims to provide novel pharmaceutical compositions, and more particularly dermatological compositions, in particular for the treatment of dermatological conditions, particularly for the treatment of acne and / or psoriasis, comprising a compound of formula (I) as a that active agent.
Un très grand nombre de personnes souffrent d'affections dermatologiques, parmi lesquelles on peut tout particulièrement citer l'acné et le psoriasis.A very large number of people suffer from dermatological conditions, among which we can particularly mention acne and psoriasis.
Le psoriasis est une maladie inflammatoire chronique de la peau qui touche environ 5% de la population française. Cette maladie peut se manifester par des plaques rouges recouvertes de pellicules blanchâtres qui se détachent de la peau : ce sont les squames. Les plaques de psoriasis se localisent souvent aux coudes, cuir chevelu et genoux, mais peuvent aussi atteindre d'autres parties du corps comme le visage, les mains, les pieds et les muqueuses. Le psoriasis peut survenir à tout âge, cependant les premières poussées apparaissent la plupart du temps entre 10 et 30 ans. C'est une maladie chronique dont l'évolution est imprévisible : aux phases de récidives succèdent des phases de rémission. Si cette maladie met rarement en danger la vie d'une personne, elle peut en revanche avoir un fort impact sur sa qualité de vie, étant donné son aspect inesthétique et sa chronicité. Certaines personnes présentent une seule plaque de psoriasis localisée dans une région bien précise du corps tandis que d'autres sont sujettes à un psoriasis étendu à l'ensemble du corps.Psoriasis is a chronic inflammatory skin disease affecting about 5% of the French population. This disease can be manifested by red patches covered with whitish films that are detached from the skin: these are the dander. Psoriasis plaques are often located on the elbows, scalp and knees, but can also reach other parts of the body such as the face, hands, feet and mucous membranes. Psoriasis can occur at any age, however the first flares appear mostly between 10 and 30 years of age. It is a chronic disease whose evolution is unpredictable: in phases of recurrence succeeds phases of remission. While this disease rarely endangers a person's life, it can have a strong impact on their quality of life, given its unsightly appearance and chronicity. Some people have a single plaque of psoriasis located in a specific area of the body while others are prone to extensive psoriasis throughout the body.
L'acné affecte également une grande partie de la population. Elle provoque fréquemment des lésions inesthétiques qui peuvent dans certains cas être durables. Ces lésions peuvent notamment avoir un effet important sur la qualité de vie, tant en terme d'inconfort que d'esthétique.Acne also affects a large part of the population. It frequently causes unsightly lesions that can in some cases be durable. These lesions can have a significant impact on the quality of life, both in terms of discomfort and aesthetics.
Il existe de nombreux traitements pour les affections dermatologiques, et notamment pour le psoriasis et l' acné ; cependant ces traitements peuvent présenter des effets secondaires indésirables, ne sont pas forcément efficaces pour tous les patients présentant ces pathologies, ou encore ne sont pas forcément efficaces sur ces types d'affections dermatologiques.
II subsiste donc un besoin de disposer de compositions destinées au traitement d'affections dermatologiques, notamment le psoriasis et/ou l'acné, qui permettent de résoudre au moins partiellement les problèmes cités ci-dessus.There are many treatments for dermatological conditions, including psoriasis and acne; however, these treatments may have undesirable side effects, are not necessarily effective for all patients with these conditions, or are not necessarily effective on these types of dermatological conditions. There remains therefore a need for compositions intended for the treatment of dermatological conditions, in particular psoriasis and / or acne, which make it possible to at least partially solve the problems mentioned above.
Les inventeurs ont ainsi découvert qu'une composition spécifique permettait le traitement d'affections dermatologiques, notamment du psoriasis et/ou de l'acné.The inventors have thus discovered that a specific composition allows the treatment of dermatological conditions, in particular psoriasis and / or acne.
Ainsi, selon un premier aspect, l'invention a pour objet l'utilisation d'au moins un composé choisi parmi le composé répondant à la formule (I) suivante :Thus, according to a first aspect, the subject of the invention is the use of at least one compound chosen from the compound corresponding to the following formula (I):
Formule IFormula I
appelé acide 2-methoxy-3-[4-[3-(4-phenoxyphenoxy)propoxy]phényl]propanoique, un de ses isomères, notamment optiques, et/ou ses sels pharmaceutiquement acceptables, pour la préparation d'une composition pharmaceutique destinée à traiter et/ou à prévenir des affections dermatologiques.2-methoxy-3- [4- [3- (4-phenoxyphenoxy) propoxy] phenyl] propanoic acid, one of its isomers, in particular optical isomers, and / or its pharmaceutically acceptable salts, for the preparation of a pharmaceutical composition intended to treat and / or prevent dermatological conditions.
Parmi les composés de formule (I) on peut citer plus particulièrement l'acide (2S)-2-methoxy- 3-[4-[3-(4-phenoxyphenoxy)propoxy]phényl]propanoique (ou Naveglitazar) correspondant.Among the compounds of formula (I), mention may be made more particularly of (2S) -2-methoxy-3- [4- [3- (4-phenoxyphenoxy) propoxy] phenyl] propanoic acid (or Naveglitazar) corresponding thereto.
Par isomères optiques, on entend notamment les formes énantiomères du composé de formule (I). En effet, le carbone porteur du groupe methoxy en position 2 de l'acide propanoïque est asymétrique, et peut donc être de configuration R ou S, ce qui correspond aux 2 énantiomères possibles de la molécule.By optical isomers is meant in particular the enantiomeric forms of the compound of formula (I). Indeed, the carrier carbon of the methoxy group at the 2-position of propanoic acid is asymmetric, and can therefore be of R or S configuration, which corresponds to the two possible enantiomers of the molecule.
Par sel pharmaceutiquement acceptable, on entend notamment un sel de métal alcalin, ou un sel alcalino-terreux, ou un sel d'aminé organique.By pharmaceutically acceptable salt is meant in particular an alkali metal salt, or an alkaline earth salt, or an organic amine salt.
Les compositions selon l'invention peuvent convenir à la prévention et/ou au traitement :
1) d'au moins une affection dermatologique liée à un désordre de la kératinisation portant sur la différenciation et sur la prolifération, notamment choisie dans le groupe comprenant les acnés vulgaires, comédoniennes, polymorphes, les acnés nodulokystiques, conglobata, les acnés séniles, les acnés secondaires, telles que l'acné solaire, médicamenteuse ou professionnelle, la rosacée, et/ouThe compositions according to the invention may be suitable for prevention and / or treatment: 1) at least one dermatological disorder related to a disorder of keratinization relating to differentiation and proliferation, in particular chosen from the group comprising vulgar, comedonal, polymorphic acne, nodulocystic acne, conglobata, senile acnes, secondary acne, such as solar acne, medicated or occupational, rosacea, and / or
2) d'au moins une affection dermatologique avec une composante immuno-allergique inflammatoire, avec ou sans trouble de la prolifération cellulaire, notamment choisie dans le groupe comprenant le psoriasis, en particulier cutané, muqueux ou unguéal, voire le rhumatisme psoriasique, ou encore l'atopie cutanée, telle que l'eczéma ou l'atopie respiratoire ou encore l'hypertrophie gingivale.2) at least one dermatological condition with an inflammatory immunoallergic component, with or without a cell proliferation disorder, especially chosen from the group comprising psoriasis, in particular cutaneous, mucous or ungual, or even psoriatic arthritis, or cutaneous atopy, such as eczema or respiratory atopy or gingival hypertrophy.
3) d'au moins un trouble de la fonction sébacée notamment choisi dans le groupe comprenant l'hyperséborrhée de l'acné, la séborrhée simple, ou la dermite séborrhéique.3) at least one disorder of the sebaceous function, especially chosen from the group comprising acne hyperseborrhoea, simple seborrhea, or seborrheic dermatitis.
L'administration de la composition pharmaceutique selon l'invention peut être effectuée par voie orale, parentérale, topique ou oculaire. De préférence, la composition pharmaceutique est conditionnée sous une forme convenant à une application par voie topique.The administration of the pharmaceutical composition according to the invention may be carried out orally, parenterally, topically or ocularly. Preferably, the pharmaceutical composition is packaged in a form suitable for topical application.
Par voie orale, la composition, plus particulièrement la composition pharmaceutique, peut se présenter sous formes de comprimés, de gélules, de dragées, de sirops, de suspensions, de solutions, de poudres, de granulés, d'émulsions, de microsphères ou nanosphères ou vésicules lipidiques ou polymériques permettant une libération contrôlée. Par voie parentérale, la composition peut se présenter sous forme de solutions ou suspensions pour perfusion ou pour injection. Les composés selon l'invention sont généralement administrés à une dose journalière d'environ 0,001 mg/kg à 100 mg/kg de poids corporel, en 1 à 3 prises.Orally, the composition, more particularly the pharmaceutical composition, may be in the form of tablets, capsules, dragees, syrups, suspensions, solutions, powders, granules, emulsions, microspheres or nanospheres. or lipid or polymeric vesicles for controlled release. Parenterally, the composition may be in the form of solutions or suspensions for infusion or injection. The compounds according to the invention are generally administered at a daily dose of about 0.001 mg / kg to 100 mg / kg of body weight, in 1 to 3 doses.
Les composés sont utilisés par voie systémique à une concentration généralement comprise entre 0,001 et 10% en poids, de préférence entre 0,01 et 1% en poids, par rapport au poids de la composition.The compounds are used systemically at a concentration generally of between 0.001 and 10% by weight, preferably between 0.01 and 1% by weight, relative to the weight of the composition.
Par voie topique, la composition pharmaceutique selon l'invention est plus particulièrement destinée au traitement de la peau et des muqueuses et peut se présenter sous forme d'onguents, de crèmes, de laits, de pommades, de poudres, de tampons imbibés, de syndets, de solutions, de gels, de sprays, de mousses, de suspensions, de lotions de sticks, de shampoings, ou de base lavantes. Elle peut également se présenter sous forme de suspensions de
microsphères ou nanosphères ou vésicules lipidiques ou polymériques ou de patchs polymériques et d'hydrogels permettant une libération contrôlée. Cette composition par voie topique peut se présenter sous forme anhydre, sous forme aqueuse ou sous la forme d'une émulsion.Topically, the pharmaceutical composition according to the invention is more particularly intended for the treatment of the skin and mucous membranes and may be in the form of ointments, creams, milks, ointments, powders, soaked swabs, syndets, solutions, gels, sprays, foams, suspensions, stick lotions, shampoos, or washing bases. It may also be in the form of suspensions of microspheres or nanospheres or lipid or polymeric vesicles or polymeric patches and hydrogels allowing controlled release. This topical composition may be in anhydrous form, in aqueous form or in the form of an emulsion.
La composition peut comprendre une teneur en composé de formule (I), ses isomères et/ou ses sels allant de 0,001 à 10 % en poids, notamment de 0,01 à 5 % en poids par rapport au poids total de la composition.The composition may comprise a content of compound of formula (I), its isomers and / or its salts ranging from 0.001 to 10% by weight, especially from 0.01 to 5% by weight relative to the total weight of the composition.
Selon un mode de réalisation avantageux, la composition comprend en outre au moins un autre agent susceptible d'augmenter l'efficacité du traitement ou de diminuer certains effets indésirables. Cet agent peut être choisi dans le groupe comprenant les antibiotiques, les antibactériens, les antiviraux, les antiparasitaires, les antifongiques, les anesthésiques, les antiallergiques, les rétinoïdes, les anti-radicaux libres, les antiprurigineux, les kératoly tiques, les antiséborrhéiques, les antihistaminiques, les produits immunosuppresseurs et antiprolifératifs.According to an advantageous embodiment, the composition further comprises at least one other agent capable of increasing the effectiveness of the treatment or of reducing certain undesirable effects. This agent may be chosen from the group comprising antibiotics, antibacterials, antivirals, antiparasitics, antifungals, anesthetics, antiallergics, retinoids, anti-free radicals, antipruritic agents, keratolytics, antiseborrhoeics, antihistamines, immunosuppressive and antiproliferative products.
La composition peut également comprendre au moins un additif usuellement utilisé dans le domaine pharmaceutique, dermatologique, compatible avec le composé de formule (I) ses isomères optiques et ses sels. L'additif peut être choisi dans le groupe comprenant les séquestrants, les antioxydants, les filtres solaires, les conservateurs, notamment la DL-alpha- tocophérol, les charges, les électrolytes, les humectants, les colorants, les bases ou acides usuels, minéraux ou organiques, les parfums, les huiles essentielles, les actifs cosmétiques, les hydratants, les vitamines, les acides gras essentiels, les sphingolipides, les composés autobronzants, notamment la DHA, les agents apaisants et protecteurs de la peau, comme l'allantoïne, les agents propénétrants, les gélifiants et leurs mélanges. Bien entendu l'homme du métier veillera à choisir ce ou ces éventuel(s) composé(s) complémentaire(s), et/ou leur quantité, de manière telle que les propriétés avantageuses de la composition selon l'invention ne soient pas, ou substantiellement pas, altérées.The composition may also comprise at least one additive usually used in the pharmaceutical and dermatological field, compatible with the compound of formula (I), its optical isomers and its salts. The additive may be selected from the group consisting of sequestering agents, antioxidants, sunscreens, preservatives, especially DL-alpha-tocopherol, fillers, electrolytes, humectants, dyes, bases or usual acids, minerals or organic, fragrances, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, especially DHA, soothing and protective agents for the skin, such as allantoin, propenetrating agents, gelling agents and mixtures thereof. Of course those skilled in the art will take care to choose this or these optional compound (s) complement (s), and / or their quantity, such that the advantageous properties of the composition according to the invention are not, or substantially not, altered.
La composition peut comprendre de 0,0001 à 20% en poids, notamment de 0,01 à 10% en poids, et en particulier de 0,1 à 5 % en poids d'additif par rapport au poids total de la composition.
Parmi les agents séquestrants, on peut citer l'acide éthylènediamine tétracétique (EDTA), ainsi que ses dérivés ou ses sels, la dihydroxyéthylglycine, l'acide citrique, l'acide tartrique, et leurs mélanges.The composition may comprise from 0.0001 to 20% by weight, especially from 0.01 to 10% by weight, and in particular from 0.1 to 5% by weight of additive relative to the total weight of the composition. Among the sequestering agents, mention may be made of ethylenediamine tetracetic acid (EDTA), as well as its derivatives or its salts, dihydroxyethylglycine, citric acid, tartaric acid, and mixtures thereof.
Le conservateur peut être choisi dans le groupe comprenant le chlorure de benzalkonium, le phénoxyéthanol, l'alcool benzylique, la diazolidinylurée, les parabènes, et leurs mélanges.The preservative may be selected from the group consisting of benzalkonium chloride, phenoxyethanol, benzyl alcohol, diazolidinyl urea, parabens, and mixtures thereof.
Comme agents humectants on peut citer la glycérine et le sorbitol.Humectants include glycerin and sorbitol.
D'autres avantages et caractéristiques de l'invention apparaîtront des exemples ci-après. Ces exemples sont donnés à titre illustratif et nullement limitatif de l'invention.Other advantages and characteristics of the invention will become apparent from the examples below. These examples are given by way of illustration and in no way limit the invention.
Exemples de CompositionsExamples of Compositions
A- VOIE ORALEA- ORAL WAY
Comprimé de 0,2 s,Tablet of 0.2 s,
- Naveglitazar 0,001 g- Naveglitazar 0.001 g
- Amidon 0,114 g- 0.114 g starch
- Phosphate bicalcique 0,020 g- Dicalcium phosphate 0.020 g
- Silice 0,020 g- Silica 0.020 g
- Lactose 0,030 g- Lactose 0.030 g
- Talc 0,010 g- Talc 0.010 g
- Stéarate de magnésium 0,005 g- magnesium stearate 0.005 g
B- VOIE TOPIOUEB- TOPIOUE ROUTE
(a) Onguent(a) Ointment
-Naveglitazar 0,300 g-Naveglitazar 0.300 g
- Vaseline blanche codex qsp 100 g- white Vaseline codex qs 100 g
(b) Lotion
- Naveglitazar 0,100 g(b) Lotion - Naveglitazar 0.100 g
- Polyéthylène glycol (PEG 400) 69,900 g- Polyethylene glycol (PEG 400) 69.900 g
- Ethanol à 95% 30,000 g
- 95% ethanol 30,000 g
Claims
REVENDICATIONS
1) Utilisation d'au moins un composé choisi parmi l'acide 2-methoxy-3-[4-[3-(4- phenoxyρhenoxy)propoxy]phényl]propanoique de formule (I) suivante :1) Use of at least one compound chosen from 2-methoxy-3- [4- [3- (4-phenoxyphenoxy) propoxy] phenyl] propanoic acid of formula (I) below:
Formule I un de ses isomères, notamment optiques et ses sels pharmaceutiquement acceptables, pour la préparation d'une composition pharmaceutique destinée à traiter des affections dermatologiques.Formula I one of its isomers, especially optical and its pharmaceutically acceptable salts, for the preparation of a pharmaceutical composition for treating dermatological conditions.
2) Utilisation selon la revendication 1 , caractérisée en ce que le composé de formule (I) est l'acide (2S)-2-methoxy-3-[4-[3-(4-phenoxyphenoxy)propoxy]phényl]propanoique (Naveglitazar).2) Use according to claim 1, characterized in that the compound of formula (I) is (2S) -2-methoxy-3- [4- [3- (4-phenoxyphenoxy) propoxy] phenyl] propanoic acid ( Naveglitazar).
3) Utilisation selon la revendication 1 ou 2, caractérisée en ce que les affections dermatologiques sont choisies parmi les affections liées à un désordre de la kératinisation portant sur la différenciation et sur la prolifération, les affections avec une composante immuno- allergique inflammatoire et les troubles de la fonction sébacée.3) The use as claimed in claim 1 or 2, characterized in that the dermatological affections are chosen from disorders linked to a keratinization disorder relating to differentiation and proliferation, affections with an inflammatory immuno-allergic component and disorders. of the sebaceous function.
4) Utilisation selon la revendication 3, caractérisée en ce que les affections dermatologiques liées à un désordre de la kératinisation portant sur la différenciation et sur la prolifération sont choisies parmi les acnés vulgaires, comédoniennes, polymorphes, les acnés nodulokystiques, conglobata, les acnés séniles, les acnés secondaires telles que l'acné solaire, médicamenteuse ou professionnelle et la rosacée.4) Use according to claim 3, characterized in that the dermatological disorders related to a disorder of keratinization on differentiation and proliferation are selected from vulgar acne, comedon, polymorphic, nodulocystic acne, conglobata, senile acnes , secondary acne such as solar acne, medicated or professional and rosacea.
5) Utilisation selon la revendication 3, caractérisée en ce que les affections dermatologiques avec une composante immuno-allergique inflammatoire sont choisies parmi le psoriasis, le rhumatisme psoriasique, l'atopie cutanée, l'atopie respiratoire et l'hypertrophie gingivale.
6) Utilisation selon la revendication 3, caractérisée en ce que les troubles de la fonction sébacée sont choisis parmi l'hyperséborrhée de l'acné, la séborrhée simple, et la dermite séborrhéique.5) The use according to claim 3, characterized in that dermatological conditions with an inflammatory immuno-allergic component are chosen from psoriasis, psoriatic arthritis, cutaneous atopy, respiratory atopy and gingival hypertrophy. 6) Use according to claim 3, characterized in that the disorders of the sebaceous function are selected from acne hyperseborrhoea, simple seborrhea, and seborrheic dermatitis.
7) Utilisation selon la revendication 5, caractérisée en ce que le psoriasis est choisi parmi le psoriasis cutané, muqueux et unguéal.7) Use according to claim 5, characterized in that the psoriasis is selected from cutaneous psoriasis, mucous and nail.
8) Utilisation selon la revendication 5, caractérisée en ce que l'atopie cutanée est l' eczéma.8) Use according to claim 5, characterized in that the cutaneous atopy is eczema.
9) Utilisation selon l'une quelconque des revendications 1 à 8, caractérisée en ce que la composition est destinée à une application topique.9) Use according to any one of claims 1 to 8, characterized in that the composition is intended for topical application.
10) Utilisation selon l'une quelconque des revendications 1 à 8, caractérisée en ce que la composition est destinée à une administration orale.10) Use according to any one of claims 1 to 8, characterized in that the composition is intended for oral administration.
11) Utilisation selon l'une quelconque des revendications 1 à 10, caractérisée en ce que la composition comprend une teneur en composé de formule (I), ou ses isomères ou ses sels allant de 0,001 à 10 % en poids, notamment de 0,01 à 5 % en poids par rapport au poids total de la composition.11) Use according to any one of claims 1 to 10, characterized in that the composition comprises a content of compound of formula (I), or its isomers or its salts ranging from 0.001 to 10% by weight, in particular from 0, 01 to 5% by weight relative to the total weight of the composition.
12) Utilisation selon l'une quelconque des revendications 1 à 11, caractérisée en ce que ladite composition comprend au moins un agent choisi dans le groupe comprenant les antibiotiques, les antibactériens, les antiviraux, les antiparasitaires, les antifongiques, les anesthésiques, les antiallergiques, les rétinoïdes, les anti-radicaux libres, les antiprurigineux, les kératoly tiques, les antiséborrhéiques, les antihistaminiques, les produits immunosuppresseurs et antiprolifératifs.12) Use according to any one of claims 1 to 11, characterized in that said composition comprises at least one agent selected from the group comprising antibiotics, antibacterials, antivirals, antiparasitics, antifungals, anesthetics, antiallergics retinoids, anti-free radicals, antipruritic drugs, keratolytics, antiseborrhoeic agents, antihistamines, immunosuppressive and antiproliferative products.
13) Utilisation selon l'une quelconque des revendications 1 à 12, caractérisée en ce que la composition comprend au moins un additif choisi dans le groupe comprenant les séquestrants, les antioxydants, les filtres solaires, les conservateurs, les charges, les électrolytes, les humectants, les colorants, les bases ou acides usuels, minéraux ou organiques, les parfums, les huiles essentielles, les actifs cosmétiques, les hydratants, les vitamines, les acides gras essentiels, les sphingolipides, les composés autobronzants, les agents apaisants et protecteurs de la peau, les agents propénétrants, les gélifiants et leurs mélanges.
13) Use according to any one of claims 1 to 12, characterized in that the composition comprises at least one additive selected from the group comprising sequestering agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, bases or usual acids, mineral or organic, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, sphingolipids, self-tanning compounds, soothing and protective agents skin, penetrating agents, gelling agents and mixtures thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0512613A FR2894477A1 (en) | 2005-12-13 | 2005-12-13 | USE OF NAVEGLITAZAR FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DERMATOLOGICAL DISEASES |
| FR0512613 | 2005-12-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2007068577A1 true WO2007068577A1 (en) | 2007-06-21 |
Family
ID=36577575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2006/068970 WO2007068577A1 (en) | 2005-12-13 | 2006-11-28 | Use of naveglitazar for preparing a pharmaceutical composition for use in the treatment of dermatological conditions |
Country Status (2)
| Country | Link |
|---|---|
| FR (1) | FR2894477A1 (en) |
| WO (1) | WO2007068577A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010084066A1 (en) * | 2009-01-23 | 2010-07-29 | F. Hoffmann-La Roche Ag | Pharmaceutical composition comprising aleglitazar |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004073622A2 (en) * | 2003-02-17 | 2004-09-02 | Smithkline Beecham Corporation | Novel therapeutic method and compositions for topical administration |
| WO2004110375A2 (en) * | 2003-06-06 | 2004-12-23 | Merck & Co., Inc. | Combination therapy for the treatment of diabetes |
-
2005
- 2005-12-13 FR FR0512613A patent/FR2894477A1/en active Pending
-
2006
- 2006-11-28 WO PCT/EP2006/068970 patent/WO2007068577A1/en active Application Filing
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004073622A2 (en) * | 2003-02-17 | 2004-09-02 | Smithkline Beecham Corporation | Novel therapeutic method and compositions for topical administration |
| WO2004110375A2 (en) * | 2003-06-06 | 2004-12-23 | Merck & Co., Inc. | Combination therapy for the treatment of diabetes |
Non-Patent Citations (1)
| Title |
|---|
| KUENZLI S ET AL: "EFFECT OF TOPICAL PPARBETA/DELTA AND PPARGAMMA AGONISTS ON PLAQUE PSORIASIS A PILOT STUDY", DERMATOLOGY, XX, XX, vol. 206, no. 3, 2003, pages 252 - 256, XP009061119, ISSN: 1018-8665 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010084066A1 (en) * | 2009-01-23 | 2010-07-29 | F. Hoffmann-La Roche Ag | Pharmaceutical composition comprising aleglitazar |
| CN102292074A (en) * | 2009-01-23 | 2011-12-21 | 霍夫曼-拉罗奇有限公司 | pharmaceutical composition comprising aleglitazar |
| CN102292074B (en) * | 2009-01-23 | 2013-08-21 | 霍夫曼-拉罗奇有限公司 | Pharmaceutical composition comprising aleglitazar |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2894477A1 (en) | 2007-06-15 |
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