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    • 2. 发明申请
    • 6-OXOPROSTAGLANDIN-E DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND THEIR PHARMACEUTICAL APPLICATION
    • 6-OXOPROSTAGLANDIN-E衍生物,其生产方法及其药物应用
    • WO1988007037A1
    • 1988-09-22
    • PCT/DE1988000151
    • 1988-03-11
    • SCHERING AKTIENGESELLSCHAFTKLAR, UlrichSKUBALLA, WernerVORBRÜGGEN, HelmutSTÜRZEBECHER, Claus-SteffenTHIERAUCH, Karl-HeinzSCHILLINGER, Ekkehard
    • SCHERING AKTIENGESELLSCHAFT
    • C07C177/00
    • C07C405/00
    • 6-Oxoprostaglandin-E, derivatives having the formula (I), in which R signifies the residue COOR where R signifies a hydrogen atom, a C1-10 alkyl, a C5-6 cycloalkyl, a C6-C10 aryl group, a heterocyclic residue or the residue CONHSO2R where R signifies a C1-10 alkyl, C5-6 cycloalkyl or C6-10 aryl; A signifies a CH=CH or a -C=C- group in an E configuration; W signifies a free or functionally modified hydroxymethylene group or a free or functionally modified group having the formula (II), in which the group OH may be either alpha - or beta - permanent; D signifies a straight-chain or branched-chain alkylene group with between 1 and 5 C atoms; E signifies a -C=C- group or a C2-C4 alkenyl group; R signifies a C1-C10 alkyl group, a C3-C10 cycloalkyl group or a C6-C10 aryl -C=C- group which may have been substituted, or a heterocyclic group; R signifies a free or functionally modified hydroxy and R and, where R signifies a hydrogen atom, the salts of said group with physiologically compatible bases; also the alpha -, beta - or gamma - cyclodextrinclothrate of the compounds having the formula (I). Process for their production and their pharmaceutical application.
    • 6-氧前列腺素E,具有式(I)的衍生物,其中R 1表示残基COOR 2,其中R 2表示氢原子,C1-10烷基,C5-6环烷基, C 6 -C 10芳基,杂环残基或残基CONHSO 2 R 5,其中R 5表示C1-10烷基,C5-6环烷基或C6-10芳基; A表示E配置中的CH = CH或-C = C-基团; W表示游离或官能改性的羟基亚甲基或具有式(II)的游离或官能改性基团,其中基团OH可以是α-或β-永久的; D表示具有1至5个C原子的直链或支链亚烷基; E表示-C = C-基或C 2 -C 4烯基; R 3表示可以被取代的C1-C10烷基,C3-C10环烷基或C6-C10芳基-C = C-基或杂环基; R 4表示游离或官能改性的羟基和R 4,并且其中R 2表示氢原子,所述基团的盐与生理上相容的碱基相同; 还有具有式(I)的化合物的α,β或γ-环糊精碱。 生产过程及其药物应用。