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    • 59. 发明申请
    • 2-OXA-BICYCLO[2.2.1]HEPTANE DERIVATIVES AND DRUGS CONTAINING SAID COMPOUNDS
    • 2-OXA-BICYCLO [2.2.1] HEPTANE衍生物和含有化合物的药物
    • WO1990002740A1
    • 1990-03-22
    • PCT/DE1989000585
    • 1989-09-07
    • SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMENKLAR, UlrichVORBRÜGGEN, HelmutREHWINKEL, HartmutTHIERAUCH, Karl-HeinzSTÜRZEBECHER, Claus-Steffen
    • SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
    • C07D307/00
    • C07D307/00C07D405/06C07D405/12C07F7/1804
    • 2-oxa-bicyclo[2.2.1]heptane derivatives according to formula (I) and their enantiomers, where for example A represents -(CH2)n-, (E)-CH=CH- or (Z)-CH=CH-, -C=C, -O- or -S-; B represents hydrogen, C1-C10 alkyl, -OR , halogen, C=N, -N3, -COOR ; R represents oxygen or a -CH2 group; R represents (a), (b), -COOR , Z represents -(CH2)p-, (E)-CH=CH-, -C=C-; W represents a direct bond, a free or functionally altered hydroxymethylene group or a free or functionally altered group (c), where the OH-group can be in the alpha or beta position; D represents a direct bond, a saturated alkylene group with 1 to 5 C atoms, a branched saturated or a linear or branched unsaturated alkylene group with 2 to 5 C atoms; E represents a direct bond, -C=C- or -CH=CR -; R represents hydrogen, C1-C10 alkyl, C3-C10-cycloalkyl, optionally substituted C6-C12-aryl or a 5 or 6 member heterocyclic residue; and if R represents hydrogen, their salts with physiologically suitable bases, as well as the alpha -, beta - or gamma -cyclodextrinclathrates, as well as compounds of formula (I) encapsulated with liposomes; process for producng them and drugs containing said compounds.
    • (I)的2-氧杂双环[2.2.1]庚烷衍生物及其对映异构体,其中例如A表示 - (CH 2)n - ,(E)-CH = CH-或(Z)-CH = CH - , - C = C,-O-或-S-; B表示氢,C 1 -C 10烷基,-OR 2,卤素,C = N,-N 3,-COOR 3; R 1表示氧或-CH 2基; R 4表示(a),(b),-COOR 5,Z表示 - (CH 2)p - ,(E)-CH = CH-,-C = C-; W表示直接键,游离或功能改变的羟基亚甲基或游离或功能改变的基团(c),其中OH基可以在α或β位; D表示直接键,具有1至5个C原子的饱和亚烷基,具有2至5个C原子的支链饱和或直链或支链不饱和亚烷基; E表示直接键,-C = C-或-CH = CR 7 - ; R 8表示氢,C 1 -C 10烷基,C 3 -C 10 - 环烷基,任选取代的C 6 -C 12 - 芳基或5或6元杂环残基; 并且如果R 5代表氢,它们与生理学上适合的碱的盐,以及α,β或γ-环糊精,以及用脂质体包封的式(I)化合物; 生产它们的方法和含有所述化合物的药物。