Retinoid-like compounds

Details Retinoid-like compounds Retinoid-like compounds

C - Chemistry, Metallurgy

07

C

C07C 233/81 (2006.01) A61K 31/19 (2006.01) A61K 31/24 (2006.01) C07C 17/16 (2006.01) C07C 45/41 (2006.01) C07C 45/45 (2006.01) C07C 45/59 (2006.01) C07C 45/63 (2006.01) C07C 45/64 (2006.01) C07C 45/67 (2006.01) C07C 47/548 (2006.01) C07C 49/67 (2006.01) C07C 49/683 (2006.01) C07C 49/697 (2006.01) C07C 49/747 (2006.01) C07C 49/798 (2006.01) C07C 63/49 (2006.01) C07C 63/66 (2006.01) C07C 63/74 (2006.01) C07C 65/00 (2006.01) C07C 65/26 (2006.01) C07C 65/36 (2006.01) C07C 69/00 (2006.01) C07C 69/618 (2006.01) C

Patent

CA 2138000

The present invention relates to a compound of formula I Image 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?C-, -CH2-NH-, -COCH2 -, -NHCS-, -CH2S-, -CH20-, -OCH2-, -NHCH2- or -CR5=CR6-; Rm and Rk are independently hydrogen, halogen, C1-6alkyl, hydroxy, C1-6alkyloxy or nitro; n is zero or one; R4 is -(CH2)t-Y, C1-6alkyl, or C3-6cycloalkyl; R1 is -CO2Z, C1-6alkyl, CH2OH, -CONHRY, or CHO; R2 and R3 are independently hydrogen or C1-6alkyl; Ra and Rb are independently hydrogen or C1-6alkyl; but when n is one, Ra and Rb together can form a radical of the formula Image ; 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; R5, R6 and RY 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).

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