Substituted (5,6)-dihydronaphthalenyl compounds having retinoid-like activity.

摘要

The present invention relates to a compound of formula I or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in which X is -O-CO-, -NH-CO-, -CS-NH-, -CO-O-, -CO-NH-, -COS-, -SCO-, -SCH2-, -CH2-CH2-, -C IDENTICAL C-, -CH2-NH-, -COCH2-, -NHCS-, -CH2S-, -CH2O-, -OCH2-, -NHCH2- or -CR<5>=CR<6>-; R and R are independently hydrogen, halogen, C1-6alkyl, hydroxy, C1-6alkyloxy or nitro; n is zero or one; R<4> is -(CH2)t-Y, C1-6alkyl, or C3-6cycloalkyl; R<1> is -CO2Z, C1-6alkyl, CH2OH, -CONHR, or CHO; R<2> and R<3> are independently hydrogen or C1-6alkyl; R and R are independently hydrogen or C1-6alkyl; but when n is one, R and R together can form a radical of the formula Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C1-6alkyl or halogen; Z is hydrogen or C1-6alkyl; R<5>, R<6> and R are independently hydrogen or C1-6alkyl; and t is zero to six. Also provided by this invention are methods for preventing and/or treating tumors and non-malignant skin disorders comprising administering a compound of formula I to a mammal. Further provided is a pharmaceutical formulation (composition) comprising a compound of formula I in admixture with (a) pharmaceutically acceptable excipient(s).