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1. A morphinan derivative represented by the following formula (I): wherein R1 represents hydrogen, C1-10 alkyl, C6-10 aryl, C2-6 alkenyl, cycloalkylalkyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms), aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, C3-6 cycloalkyl, or heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms, R2 represents hydrogen, C1-10 alkyl, C3-6 cycloalkyl, C6-10 aryl, heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms, aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms, cycloalkylalkyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, C2-6 alkenyl, arylalkenyl in which the aryl moiety has 6 to 10 carbon atoms and the alkenyl moiety has 2 to 6 carbon atoms, heteroarylalkenyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms; and the alkenyl moiety has 2 to 6 carbon atoms, cycloalkylalkenyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkenyl moiety has 2 to 6 carbon atoms, C4-6 cycloalkenyl, cycloalkenylalkyl in which the cycloalkenyl moiety has 4 to 6 carbon atoms; and the alkylene moiety has 1 to 5 carbon atoms, or cycloalkenylalkenyl in which the cycloalkenyl moiety has 4 to 6 carbon atoms and the alkenyl moiety has 2 to 6 carbon atoms, R3, R4, and R5, which are the same or different, represent hydrogen, hydroxy, halogen, cyano, carbamoyl, C1-6 alkoxy, C6-10 aryloxy, C1-6 alkanoyloxy, nitro, amino, C1-6 alkylamino, C6-10 arylamino, or acylamino in which the acyl moiety has 2 to 6 carbon atoms, R6a and R6b, which are the same or different, represent hydrogen, fluorine or hydroxy, or R6a and R6b combine together to represent ═O, R7 and R8, which are the same or different, represent hydrogen, fluorine or hydroxy, R9 and R10, which are the same or different, represent hydrogen, C1-6 alkyl, C6-10 aryl, heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms, aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms, cycloalkylalkyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, or C2-6 alkenyl, X represents O or CH2, and Y represents C═O, C═S, SO2, C(═O)O, C(═O)NR11, C(═S)NR11, or an atomic bond, where R11 represents hydrogen, C1-6 alkyl, aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms, or cycloalkylalkyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, or may form a 4- to 7-membered ring together with the N atom to which R11 bonds and R2, where the 4- to 7-membered ring may contain heteroatom(s) selected from N, O, and S atoms as a ring-constituting atom other than the N atom to which R11 binds, and may have 1 to 3 substituents selected from halogen, hydroxy, C1-6 alkyl, aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, C2-6 acyl, and oxo group, provided that the C1-10 alkyl as R1 or R2, the alkylene moiety and the cycloalkyl moiety of the cycloalkylalkyl in which the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms) as R1 or R2, the alkylene moiety of the aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms as R1 or R2, as well as the alkylene moiety of the heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms as R1 or R2, may be substituted with at least one substituent selected from 1 to 6 halogens, hydroxy, C1-6 alkoxy, C6-10 aryloxy, C1-6 alkanoyl, C1-6 alkanoyloxy, carboxyl, alkoxycarbonyl in which the alkoxy moiety has 1 to 6 carbon atoms, carbamoyl, alkylcarbamoyl in which the alkyl moiety has 1 to 6 carbon atoms, dialkylcarbamoyl in which each alkyl moiety has 1 to 6 carbon atoms, alkylsulfonyl in which the alkyl moiety has 1 to 6 carbon atoms, alkylthio in which the alkyl moiety has 1 to 6 carbon atoms, C1-6 alkoxy substituted with 1 to 6 halogens, arylcarbonyl, and oxetanyl, the aryl as R1, aryl moiety of the aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms as R1, the aryl as R2, the heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms as R2, or the aryl moiety of the aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms as R2, the heteroaryl moiety of the heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkylene moiety has 1 to 5 carbon atoms as R2, the aryl moiety of the arylalkenyl in which the aryl moiety has 6 to 10 carbon atoms and the alkenyl moiety has 2 to 6 carbon atoms as R2, the heteroaryl moiety of the heteroarylalkenyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms and the alkenyl moiety has 2 to 6 carbon atoms as R2, the aryl moiety of the C6-10 aryloxy as R3, R4, or R5, the aryl moiety of the C6-10 arylamino as R3, R4, or R5, the C6-10 aryl as R9 or R10, the heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms as R9 or R10, or the aryl moiety of the aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms as R9 or R10, and the heteroaryl moiety of the heteroarylalkyl in which the heteroaryl contains 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms, and the alkylene moiety has 1 to 5 carbon atoms as R9 or R10, may be substituted with at least one substituent selected from C1-6 alkyl, C1-6 alkoxy, C1-6 alkanoyloxy, hydroxy, alkoxycarbonyl in which the alkoxy moiety has 1 to 6 carbon atoms, carbamoyl, alkylcarbamoyl in which the alkyl moiety has 1 to 6 carbon atoms, dialkylcarbamoyl in which each alkyl moiety has 1 to 6 carbon atoms, halogen, nitro, cyano, C1-6 alkyl substituted with 1 to 3 halogens, C1-6 alkoxy substituted with 1 to 3 halogens, phenyl, heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S as ring-constituting atoms, phenoxy, phenylalkyl in which the alkyl has 1 to 3 carbon atoms, methylenedioxy, and NR12R13, where R12 and R13 independently represent hydrogen, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6 alkanoyl, or alkoxycarbonyl in which the alkoxy moiety has 1 to 6 carbon atoms, or R2 and R3 may form a 4- to 7-membered ring together with the N atom to which they bond, where the 4- to 7-membered ring may further contain heteroatom(s) selected from N, O, and S, and furthermore, the alkylene moiety of the aralkyl in which the aryl moiety has 6 to 10 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms as R1 or R2 may be substituted with at least one substituent selected from phenyl and C1-6 alkyl substituted with 1 to 3 halogens, or a pharmacologically acceptable acid addition salt thereof. |
