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    • 57. 发明专利
    • JPS5186449A
    • 1976-07-29
    • JP15066575
    • 1975-12-19
    • HOECHST AG
    • GERUHARUTO BETSUKUURURITSUHI RERUHIKARURU ZEEGAAHERUMAN TOIFUERU
    • C07C67/00C07C401/00C07C405/00C07D307/935C07D309/12C07F9/38C07F9/40
    • Prostaglandin analogues of formula (I) in the natural, optically active configuration or as racemic cpds.: (where R1 + R2 is O, or one of R1 and R2 is H and the other is OH; one of R3 and R4 is H and the other is OH; is 1-5C straight or branched alkyl, or phenyl or benzyl opt. mono- di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy; R5, when X is 1-5C alkyl, is a diphenyl ether gp. opt. mono- di- or tri-substd. in either or both nuclei by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy or a phenoxy-(2-5 C straight chain or 3-6C branched chain alkyl) opt. mono-di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy, or, when X is opt. substd. phenyl, a benzyl residue opt. mono- di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy, or, when X is opt. substd. benzyl, a phenyl residue opt. mono-, di- or tri-substd. by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy; and the C-atoms in the 5- and 6-positions and the 13- and 14-positions are all linked by single bonds or all linked by double bonds), e.g. 9-oxo-11 alpha, 15-dihydroxy-16-methyl-16-(3-chloro-4-(4-chlorophenoxy)-phenoxy)-- 5-cis-13-trans-tetranorprostadienoci acid, their physiologically tolerable salts with organic and inorganic bases, and their esters with 1-8C aliphatic, cycloaliphatic and araliphatic alcohols are new. (I) can be used as pharmaceuticals with hypotensive, diuretic, antithrombotic labour-inducing, abortifacient, contraceptive, gastric secretion inhibiting, antiulcer and antiasthmatic activity. They are particularly useful as contraceptives for use in humans and as agents for synchronising oestrus in various animal species. They are more potent and longer-acting than natural prostaglandins.