Patent IL-118076-A (IL)
Title: Cosmetic and pharmaceutical compositions containing 2-[7-(1-adamantyl) naphthyl] aryl derivatives for treatment of ailments involving retinoid acid receptors and hypervitaminosis a and some new such compounds
IPC: C07D295/092
Filed: 1996-04-29
Abstract: A cosmetic or pharmaceutical composition for the treatment of disorders or aliments related to an overregulation of RARs and/or to hypervitaminosis A, comprising as an active agent a pharmaceutically effective amount of at least one compound of retinoid type of general formula 2134 כ" ה באלול התשס" א - September 13, 2001 in which -R1 represents (i) the -CH3 radical, (ii) the -CH2OH radical, (iii) the -O-R3 radical, (iv) the -CO-R4 radical, R3 and R4 having the meanings given below, Ar is a radical of formula: R5 having the meaning given below, R2 represents: (a) an -(X)n-(CH2)p-R6 radical, (b) an - (X)n-(CH2)q-R7 radical, (c) a -CH=CH-(CH2)s-R6 radical, (d) a -CH=CH-(CH2)t-R7 radical, R6, R7, X, n p , q, s and t having the meanings given below, it being understood that: R3 represents a hydrogen atom, a lower alkyl radical or a -(CH2)m-(CO)n-R8 radical, R8, m and n having the meanings given below, R4 represents: (a) a hydrogen atom, (b) a lower alkyl radical, (c) a radical of formula: (d) an -OR9 radical, R(, R) and R9 having the meanings given below, R5 represents a hydrogen or halogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, a hydroxyl 2135 כ" ה באלול התשס" א - September 13, 2001 radical or an -OR10 or O , -O-C-R10 radical, R10 having the meaning given below, R6 represents a hydrogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, an alkenyl radical or an alkynyl radical, R7 represents an aryl radical, a mono- or polyhydroxyalkyl radical in which the hydroxyls are optionally protected in the methoxy or acetoxy or acetonide form, an aminoalkyl radical in which the amine functional group is optionally substituted by one or two lower alkyl groups, a polyether radical, a -COR4 radical, a saturated or unsaturated heterocycycle radical or alternatively an aminoaryl radical, R8 represents a lower alkyl radical or a saturated heterocycle, R9 represents a hydrogen atom, a linear or branched alkyl radical having from 1 to 20 carbon atoms, an alkenyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl or aralkyl radical or a sugar residue or an amino acid or peptide residue, R10 represents a lower alkyl radical, X represents an oxygen atom or an -S(O)r radical, R( and R), which are identical or different, represent a hydrogen atom, a lower alkyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl radical or an amino acid, peptide or sugar residue or alternatively, taken together, form a saturated heterocycle, m is an integer between 1 and 3 inclusive, n is an integer between 0 and 1 inclusive, p is an integer between 5 and 12 inclusive, q is an integer between 0 and 12 inclusive, r is an integer between 0 and 2 inclusive, s is an integer between 3 and 10 inclusive, t is an integer between 0 and 10 inclusive, as well as their salts and their chiral analogues. Claimed as new are compounds, characterized in that they have the formula (I), as defined above in which R7 is a polyether radical having a carbon in the position a to the carbon which is in the 6-position of the naphthyl radical.