Abstract: An analgesic which may be applied to wide variety of pain from various causes is disclosed.

Abstract: Crystalline particles of N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 ?m, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 ?m, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.

Abstract: Crystalline particles of N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 ?m, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 ?m, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.

Abstract: A method of inhibiting or reducing occurrence or intensity of pruritus including administering to a patient an effective amount of one or more of the morphinan derivative having a nitrogen-containing cyclic group of the Formula (Ia): wherein R1 is cyclopropylmethyl; R2 and R3 are independently hydrogen, hydroxy, C1-C5 alkoxy, C3-C7 alkenyloxy, C7-C13 aralkyloxy or C1-C5 alkanoyloxy; and the Formula (Ia) includes (+), (?) and (±) isomers or the pharmaceutically acceptable acid addition salt thereof.

Abstract: A novel antipruritic useful for the treatment of pruritus accompanying various diseases is disclosed. The antipruritic comprises a specific morphinan derivative having a nitrogen-containing cyclic group or the pharmaceutically acceptable acid addition salt thereof such as N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-phthalimide hydrochloric acid salt or N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt.

Abstract: The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.

Abstract: An analgesic which may be applied to wide variety of pain from various causes is disclosed.

Abstract: The invention provides a morphinan derivative of the Formula (I): (wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like) or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.