| 摘要 |
Cpds of formula (I), (where R1 is 2, 6, 6-trimethylcyclohex-1-en-1-yl, or a phenyl residue substd. in the 2- and 6-position by lower alkyl, lower alkoxy or halogen and in at least one of positions 3, 4 and 5 by OH, halogen, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, lower alkanoyloxy, NO2, amino, mono- or di(lower alkyl)amino, lower alkanoylamino or an N-heterocyclic residue, and R2 is formy formyl, hydroxymethyl, alkoxymethyl, alkanoyloxymethyl, carboxy , alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxy-carbonyl, carbamoyl, mono- or di(lower alkyl)carbamoyl or N-heterocyclylcarbonyl), e.g. 3, 7-dimethyl-9-(2, 6, 6-trimethyl-cyclohex-1-en-1-yl)-nona-2, 6, 8-trien-1-oic acid methyl ester, and their analogues are new dihydro-vitamin A derivs. They may be prepd. by e.g. reacting cpds. of formula (II) with cpds of formula (III), (in which one of A and B is oxo and the other is a gp -P(Y)3 circled positive Z circled negative, in which Y is aryl and Z is the anion of an (in)organic acid, and R3 is alkoxymethyl, dialkoxymethyl, alkanoyloxymethyl, alkoxycarbonyl, alkenyloxy-carbonyl or alkynyloxycarbonyl when B is oxo and is formyl, hydroxymethyl, alkoxymethyl, dialkoxymethyl, carboxy, alkoxycarbonyl, alkenyloxycarbonyl or alkynyloxy-carbonyl when A is oxo), an acetal obtained opt. being saponified. (I) can be used for the topical and systemic therapy and for the systemic and topical prophylaxis of such disorders. (I) can also be used for the systemic and topical therapy of acne, proriasis or other dermatoses associated with increased or pathologically altered cornification. |
