Patent EP-1733731-A1 (EP)
Inventor: ZECHES-HANROT MONIQUE
IPC: A61K8/60
Filed: 2006-06-09
Abstract: Use of a glycerol compounds (I) is claimed for the preparation of a cosmetic composition, a pharmaceutical composition for the treatment of cancers not involving Epstein-Barr virus, particularly for treating melanoma or for treating oral inflammation, or a nutritive composition. (I) Is a compound of the family of di-galactosyl-di-glyceride compounds (II). The composition contains a second compound (II) different from (I), where (I) does not affect fibronectin activity. Use of a glycerol compounds of formula R3O-CH2-CH(OR2)-CH2-OR1 (I) is claimed for the preparation of a cosmetic composition, a pharmaceutical composition for the treatment of cancers not involving Epstein-Barr virus, particularly for treating melanoma or for treating oral inflammation, or a nutritive composition. (I) Is a compound of the family of di-galactosyl-di-glyceride compounds of formula (II). The composition contains a second compound (II) different from (I), where (I) does not affect fibronectin activity. R1, R5a, R8, R5, R7H or optionally saturated 2-20C acyl; R2R1 or 2,6-dimethyl-tetrahydro-pyran group of formula (i); R4, R6R1 or 2,6-dimethyl-tetrahydro-pyran group of formula (ii), and R3H or 2,6-dimethyl-tetrahydro-pyran group of formula (iii), provided that in (I), when R1 and R2 are H, then R3 is (iii) and when R1 and R2 are acyl, then R3 is (iii). Independent claims are included for: (1) a topical cosmetic composition comprising (I) in combination with a carrier, and (2) preparation of a cosmetic composition containing a lipidic fraction enriched in (I) or sub-fractions containing (I), which comprises enriching a concentrated oil in (I), at a rate of 50-95%, by elimination of at least a part of the non-polar compounds e.g. triglycerides, sterols, waxes, fatty acids and other insaponifiable fractions, preferably by liquid-liquid partition of the concentrated oil, using a biphasic solvent system or simple dephasing in a hydroalcoholic mixture, optionally in the presence of an organic solvent e.g. chloroform or methyl tert-butyl ether to obtain a liquid phase enriched in the non-polar compound and a lipid fraction liquidate enriched in (I), preferably free of triglycerides and optionally in addition, by elimination of the polar compounds e.g. sugar residue, preferably by liquid-liquid partition of the lipidic fraction enriched in (I), using a biphasic solvent system or by simple dephasing in a hydroalcoholic mixture, optionally in the presence of an organic solvent e.g. chloroform or methyl tert-butyl ether to obtain a lipid fraction enriched in (I), free from sugars, where the order of the elimination of the non-polar compounds and the polar compounds can be reversed, and optionally a fractionation stage of the lipid fraction enriched in (I) or the lipid fraction enriched in (I), free from sugars, preferably by chromatography on silica gel, preferably liquid chromatography on solid support or centrifugal partition chromatography, optionally by supercritical fluids to isolate the sub-fractions containing (I). [Image] [Image] ACTIVITY : Cytostatic; Dermatological; Antiinflammatory; Vulnerary. MECHANISM OF ACTION : Matrix metalloproteinase inhibitor; Collagenase inhibitor; Plasmin inhibitor. In an in vitro assay used to determine inhibition of matrix metalloproteinase, results showed that (I) exhibited a median inhibitory concentration value of 26.31 mu g/ml.