| 摘要 |
The use of an effective quantity of at least one retinoid of formula (I), their salts and chiral analogues, in a cosmetic or pharmaceutical composition for the treatment of a disorder or disease due to over-activity of RARs (retinoic acid receptors) and/or the presence of an abnormal amount of vitamin A or its metabolites, is new. R1 = Me, CH2OH, OR3, or COR4; Ar = a group of formula (a)-(d); R2 = (X)n(CH2)pR6, (X)n(CH2)qR7, CH=CH(CH2)sR6, or CH=CH(CH2)tR7; R3 = H, lower alkyl or (CH2)m(CO)nR8; R4 = H, lower alkyl, N(R')R" or OR9; R5 = H, halo, 1-20C alkyl, OH, OR10 or OCOR10; R6 = H, 1-20C alkyl, alkenyl or alkynyl; R7 = aryl, mono- or poly-hydroxyalkyl (the OH groups of which may be protected as methoxy, acetoxy or acetonide), aminoalkyl (the amino group of which may be substituted by one or more lower alkyl), polyether, COR4, opt. unsatd heterocycle, or amino-aryl; R8 = lower alkyl or satd heterocycle; R9 = H, 1-20C alkyl, alkenyl, mono- or poly-hydroxyalkyl, opt. substd aryl or aralkyl, or a sugar, aminoacid or peptide residue; R10 = lower alkyl; X = O, S, SO, or SO2; R', R" = H, lower alkyl, mono- or poly-hydroxyalkyl, opt. substd aryl, or a sugar, aminoacid or peptide residue; or R'+R" = a satd heterocycle; m = 1-3; n = 0 or 1; p = 5-12; q = 0-12; s = 3-10; and t = 0-10. Compounds of formula (I) where R7 = polyether having a carbon atom alpha to the carbon in position 6 of the naphthyl radical, i.e. (IA), are new. |
