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    • 4. 发明申请
    • CYCLODEXTRINCLATHRATES OF CARBACYCLINE DERIVATIVES AND THEIR USE AS MEDICINAL DRUGS
    • 碳水化合物衍生物及其作为药物使用的环孢菌素
    • WO1987005294A1
    • 1987-09-11
    • PCT/DE1987000106
    • 1987-03-09
    • SCHERING AKTIENGESELLSCHAFT
    • SCHERING AKTIENGESELLSCHAFTSKUBALLA, WernerVORBRÜGGEN, HelmutDAHL, HelmutSTÜRZEBECHER, Claus-SteffenTHIERAUCH, Karl-Heinz
    • C07C177/00
    • B82Y5/00A61K47/6951C07C405/0083C08B37/0015
    • Cyclodextrinclathrates of carbacycline analogs have general formula (I) in which: R1 is an atom of hydrogen or a straight chain or branched alkyl rest with up to 10 C atoms, A is a trans-CH=CH or -C=C group, W is a free or functionally transformed hydroxymethylene group or a free or functionnally transformed group (II), where the OH group can be alpha or beta stable, D is the group (III) a straight chain, saturated alkylene group with 1-5 C atoms, a branched or a straight chain or a branched unsaturated alkylene group with 2-5 C atoms, which can be if necessary substituted with fluorine atoms, m can represent the numbers 1, 2 or 3, E is a direct link, a -C=C group or a -CR4=CR5 group, in which R4 represents hydrogen or an alkyl group with 1-5 C atoms and R5 represents hydrogen, halogen or an alkyl group with 1-5 C atoms, R2 is an alkyl group with 1-10 C atoms, a cycloalkyl group with 3-10 C atoms or a possibly substituted aryl group with 6-10 C atoms or an heterocyclic group and R3 represents a free or functionally transformed hydroxyl group, n can represent the numbers 1, 2, 3, 4 or 5 and X a -CH2 group or an atom of oxygen.
    • 通式Ⅰ的碳霉酸类似物的环糊精包合物其中R 1是氢,至多10个碳原子的烷基或链烯基,A是-CH 2 CH 2 - ,反式-CH = CH-或-C 3位C- 基团,W是游离或官能改性的羟基亚甲基基团或游离或官能改性的“IMAGE”,其中OH基团可以在α或β-位,D是亚烷基,或不饱和亚烷基,其各自可以 任选被氟原子取代,m为1,2或3,E为直接键,-C 3位C基或-CR 4 = CR 5 - 基,其中R 4为氢或1-5碳烷基 原子,R5为氢或1-5个碳原子的烷基,R5为氢,卤素或1-5个碳原子的烷基,R2为至多10个碳原子的烷基或烯基,环烷基为3 -10个碳原子或任选取代的6-10个碳原子的芳基或杂环基,R3是游离或官能改性的羟基,n是1,2,3,4或5,X是-CH 2 - 或氧作为有价值的结晶药物。