| 摘要 |
The use of substituted mono- or polyhydroxy-chromen-4-one derivatives of formula (I) (or (I)-containing preparations) for care, preservation or improvement of general condition of the skin or hair and preventing and/or inhibiting premature skin aging, skin diseases associated with keratinization or benign or malignant growths of the dermis or epidermis is new. The use of chromenones of formula (I) (or (I)-containing preparations) is claimed for: (1) care, preservation or improvement of general condition of the skin or hair; (2) production of preparations for preventing and/or inhibiting premature skin aging; (3) production of preparations for the prophylaxis and/or treatment of skin diseases associated with keratinization; or (4) production of preparations for the prophylaxis and/or treatment of benign or malignant growths of the dermis or epidermis. R 1>, R 2> : H, COR 7>, COOR 7>, 1-20C alkyl, 3-20C alkenyl, 1-20C hydroxyalkyl (where the OH groups are bonded to primary or secondary C-atoms and the chain is optionally interrupted by O); or 3-10C cycloalkyl or 3-10C cycloalkenyl (both optionally over-bridged by (CH 2) n); n : 1-3; R 3> : H or 1-20C alkyl; R 4> : H or OR 8>; R 5>, R 6> : H, OH, 1-20C alkyl, 3-20C alkenyl or 1-20C hydroxyalkyl (where the OH groups are bonded to primary or secondary C-atoms and the chain is optionally interrupted by O); R 7> : H, 1-20C alkyl or the residue of a polyhydroxy compound (preferably an ascorbic acid or glycoside residue); and R 8> : H or 1-20C alkyl. Provided that at either (i) at least two of R 1>, R 2>and R 4>- R 6>are other than H or (ii) at least one of R 1>and R 2>= COR 7>or COOR 7>. Independent claims are included for: (1) preparations containing at least one compound (I), at least one skin-care component (II) and a carrier for topical application; and (2) the production of preparations containing (I), by mixing (I) with a cosmetic, dermatological or foodstuff carrier. [Image] ACTIVITY : Dermatological; antiseborrheic; antiinflammatory; immunosuppressive; antiallergic; antipsoriatic; antirheumatic; cytostatic; virucide; antipruritic; vulnerary; ophthalmological; antialopecia; antiarthritic; cardiant; antiarteriosclerotic; hypotensive; antidiabetic; vasotropic; anorectic. MECHANISM OF ACTION : Protein kinase inhibitor; elastase inhibitor; aldose reductase inhibitor; hyaluronidase inhibitor; catechol-O-methyl transferase inhibitor; AMP phosphodiesterase inhibitor; antioxidant; antiradical. 5,7-Dihydroxy-2-methyl-chromen-2-one (Ia) had IC 5 020 mM for inhibition of hyaluronidase. |
