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    • 7. 发明授权
    • 1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    • 1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖庚因-10-ols
    • US06455538B1
    • 2002-09-24
    • US09523473
    • 2000-03-10
    • Matthias GrauertAdrian CarterWolf-Dietrich BechtelThomas WeiserRainer PallukUwe Pschorn
    • Matthias GrauertAdrian CarterWolf-Dietrich BechtelThomas WeiserRainer PallukUwe Pschorn
    • A61K31439
    • C07D221/26
    • Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.
    • 通式I的化合物,其中X是单键,-O-,C-C4-亚烷基或具有1至8个碳原子的亚烷基桥,其可以是支链或非支链的,并且任选地在一个或多个氧原子中具有一个或两个氧原子 桥梁 R1是氢,甲基,乙基或苯基; R2是氢或甲基; R3是氢,氟,氯,溴,羟基,甲基或甲氧基; R4是氢,甲基或乙基; R5是氢,甲基或乙基; R6是氢,甲基或乙基; R 7是叔丁基,环己基,任选被R 9和R 10取代的苯基,其可以相同或不同,或者R 8是氢或C 1 -C 4 - 烷基; Z是氧,NH或硫; R9是氢,甲基,氟,氯,溴或甲氧基; R 10为氢,甲基,氟,氯,溴或甲氧基; 任选以各种旋光异构体的形式,各个对映异构体或外消旋体的混合物,以及游离碱的形式或与药学上可接受的酸的相应的酸加成盐。