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Stable solid preparation containing a 4,5-epoxymorphinan derivative
专利权人:
TORAY INDUSTRIES, INC.;MARUHO CO., LTD.
发明人:
TAKAKI, SUGURU,OHTA, KOTOE,HORIUCHI, YASUHIDE,KOBAYASHI, MASATO,KAWASAKI, JUNKO,HORISAWA, EIJIRO
申请号:
ES08752145
公开号:
ES2381056T3
申请日:
2008.04.25
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
Stable solid preparation, comprising as an effective ingredient a 4,5-epoxymorphinan derivative represented by the general formula (I): in which a double line formed by a dashed line and a solid line represents a double bond or a single bond; R1 represents an alkyl having 1 to 5 carbon atoms, a cycloalkylalkyl having 4 to 7 carbon atoms, a cycloalkenyl alkyl having 5 to 7 carbon atoms, an aryl having 6 to 12 carbon atoms, an aralkyl having 7 to 13 carbon atoms, an alkenyl having 4 to 7 carbon atoms, an allyl, a furan-2-ylalkyl having 1 to 5 carbon atoms or a thiophene-2-ylalkyl that it has 1 to 5 carbon atoms; R2 represents hydrogen, hydroxy, nitro, an alkanoyloxy having 1 to 5 carbon atoms, an alkoxy having 1 to 5 carbon atoms, an alkyl having 1 to 5 carbon atoms or -NR7R8; R7 represents hydrogen or an alkyl having 1 to 5 carbon atoms; R8 represents hydrogen, an alkyl having 1 to 5 carbon atoms or -C (= O) R9-; R9 represents hydrogen, phenyl or an alkyl having 1 to 5 carbon atoms; R3 represents hydrogen, hydroxy, an alkanoyloxy having 1 to 5 carbon atoms or an alkoxy having 1 to 5 carbon atoms; A represents -N (R4) C (= X) -, -N (R4) C (= X) Y-, -N (R4) - or -N (R4) SO2-, where X and Y each independently represent NR4, S or O, and R4 represents hydrogen, a linear or branched alkyl having 1 to 5 carbon atoms or an aryl having 6 to 12 carbon atoms, and the R4 of the formulas may be the same or different; B represents (i) a valence bond, (ii) a linear or branched alkylene having 1 to 14 carbon atoms, which may be substituted, at least, with one or more substituents selected from the group consisting of an alkoxy that it has 1 to 5 carbon atoms, an alkanoyloxy having 1 to 5 carbon atoms, hydroxy, fluorine, chlorine, bromine, iodine, amino, nitro, cyano, trifluoromethyl, trifluoromethoxy and phenoxy, in which 1 to 3 alkylene methylene groups (ii) may be substituted with carbonyl groups, (iii) a linear or branched unsaturated acyclic hydrocarbon containing 1 to 3 double
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