| 摘要 |
The present invention relates to a compound of formula (see formula) 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-O-, -CO-NH-, -COS-, -SCO-, -SCH2-, -CH2-CH2-, -C(C-, -CH2,-NH-, -COCH2-, -NHCS-, -NHCS-, -CH2S-; -CH2O-, -OCH2-, -NHCH2- or -CR5=CR6-; Rm and Rk are independently hydrogen, halogen, C1-6 alkyl, hydroxy, C1-6 alkyloxy or nitro; n is zero or one; R4 is -(CH2)t-Y, C1-6 alkyl, or C3-6 cycloalkyl; R1 is -CO2Z, C1-6alkyl, CH2OH, -CONHRy , or CHO; R2 and R3 are independently hydrogen or C1-6 alkyl alkyl; Ra and Rb are independently hydrogen or C1-6 alkyl; but when n is one, Ra and Rb together can form a radical of the formula (see formula); Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C1-6 alkyl or halogen; Z is hydrogen or C1-6 alkyl;R5, R6 and Ry are independently hydrogen or C1-6 alkyl; and t is zero to six. Also porivided by this invention are methods for preventing and/or treating tumors, arthritis and nonmalignant skin disorders comprising administering a compound of formula Y to a mammal. Further provided is a pharmaceutical formulation (composition) comprising a compound of formula Y in admixture with (a) pharmaceutically acceptable excipient (s). |
