- DERMATOLOGICAL COMPOSITIONS COMPRISING RETINOIDS, DISPERSED BENZOYL PEROXIDE AND CARRAGEENANS
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Dermatological compositions containing, in a physiologically acceptable medium, at least one retinoid, dispersed benzoyl peroxide and at least one gelling agent of the family of the carrageenans, are useful for treating dermatological conditions and afflictions linked to disorders of cell differentiation and/or proliferation and/or keratinization, notably for treating acne vulgaris.
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- Cream gels comprising at least one retinoid and benzoyl peroxide
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The invention relates to a composition in the form of a cream gel comprising, in a physiologically acceptable medium, at least one dispersed retinoid and dispersed benzoyl peroxide, to its process of preparation and to its use in cosmetics and in dermatology.
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- Emulsions comprising at least one retinoid and benzoyl peroxide
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Stable dermatological/cosmetic emulsions useful, e.g., for the treatment of acne vulgaris, contain, formulated into a physiologically acceptable medium, a homogeneous dispersion of at least one dispersed retinoid, dispersed benzoyl peroxide, at least one fatty phase, at least one hydrophilic phase and at least one emulsifier.
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- Phenolic/naphtholic retinoids for promoting skin/exoskeleton pigmentation
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Pigmentation of the skin, hair and/or nails of individuals is promoted by administering thereto, advantageously topically and advantageously in combination with enzymes exhibiting tyrosinase activity, effective pigmentation-promoting amounts of at least one retinoid compound which comprises a phenolic or naphtholic functional group.
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- Retinoid inhibition of expression of VEGF
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The retinoids, in particular the anti-AP-1 retinoids, effectively inhibit the expression of VEGF, and thus are useful for the therapeutic treatment of disease states manifesting an overexpression of VEGF.
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- Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes
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The retinoic acid receptors (RARs) transduce retinoid dependant gene regulation, and many biological effects of retinoids are mediated through binding and activation of three closely related receptor subtypes (RARα, RARβ, and RARγ). In order to investigate the role of receptor subtypes, we have carried out a chemical synthesis program to seek selective retinoids for these receptors. We measured receptor binding affinity using recombinant RARα, -β, and -γ proteins and assessed cellular differentiating activity in F9 murine teratocarcinoma cells (F9 cells). This research has identified the 4-substituted-3-(1-adamantyl)phenyl moiety as a new pharmacophore which can replace the β-cyclogeranylidene ring of the naturally ocurring all- trans-retinoic acid. Two chemical series derived from the general structures 6-(3-tertioalkyl-phenyl)-2-naphthoic acid (series I) and 4-[(E)-2-(3- tertioalkylphenyl)propenyl]benzoic acid (series II) were developed. In particular, we have obtained the RARγ selective derivatives 6-[3-(1- adamantyl)-4-hydroxyphenyl]-2-naphthoic acid (7) [K(i)(RARα) = 6500 nM, Ki(RARβ) = 2480 nM, K(i)(RARγ) = 77 nM] and 4-[(E)-2-[3-(1-adamantyl)-4- hydroxyphenyl]propenyl]benzoic acid (19) [K(i)(RARα) = 1 144 nM, K(i)(RARβ) = 1245 nM, K(i)(RARγ) = 53 nM]. In series I, the presence of a phenol group, irrespective of the nature of tertioalkyl group, imparted at least partial RARγ selectivity, whereas in series II, the presence of both adamantyl and phenol groups is needed to confer RARγ selectivity. The RARγ selective ligands induce differentiation in F9 cells (7, AC50 = 33 nM; 19, AC50 = 66 nM). From series I, a mixed RARβ-γ agonist with potent cellular differentiating activity was selected for development as a topical antiacne agent, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (5, CD 271) [K(i)(RARα) = 1100 nM, K(i)-(RARβ) = 34 nM, K(i)(RARγ) = 130 nM, AC50(F9) = 37 nM]. Finally, from series II, we have obtained a weak antagonist in the F9 cellular differentiation assay, 4-[(E)-2-(3-tert-butyl- 4-hydroxyphenyl)propenyl]benzoic acid (15, IC50 = 700 nM).
- Charpentier,Bernardon,Eustache,Millois,Martin,Michel,Shroot
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p. 4993 - 5006
(2007/10/03)
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- Benzonaphthalene derivatives and compositions
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A benzonaphthalene compound has the formula STR1 wherein R1 represents (i) STR2 or (ii) --CH2 OH; R6 represents STR3 or OR7 wherein R7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH3)2 --R8 wherein R8 represents lower alkyl; and R4 and R5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy. This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues. The compound also possesses anti-tumor activity.
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