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    • 57. 发明授权
    • Prostaglandins
    • 前列腺素
    • US4902717A
    • 1990-02-20
    • US913672
    • 1986-09-03
    • Judith SeniorKay M. Troughton
    • Judith SeniorKay M. Troughton
    • C07C281/06A61K31/175A61K31/557C07C67/00C07C239/00C07C313/00C07C323/44C07C325/00C07C337/06C07C405/00C07D493/00
    • C07C405/0091A61K31/175A61K31/557
    • Compounds having thromboxane antagonist activity are of use in the treatment of hormone-dependent neoplasias for example oestrogen-dependent neoplasias. Thromboxane antagonists of particular value are compounds of formula (I) ##STR1## wherein ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)--NV'R, respectively; R.sup.1 is a 6-carboxyhex-2-enyl group or a modification thereof in which the group is altered by one, or an appropriate combination of two or more, of the following: (a) alteration of the position of the double bond, (b) reduction of the double bond, (c) alteration of the chain length through a decrease of one or two methylene groups or an increase of one to six methylene groups, (d) replacement of one or two methylene groups each separately by an oxygen or sulphur atom with the proviso that in the modified group no oxygen or sulphur atom is in an alpha position relative to either a doubly bonded carbon atom or to the carboxy group or a derivative thereof and that at least 2 carbon atoms separate any pair of oxygen and/or sulphur atoms; and (e) formation of an amide, ester or salt derivative of the carboxy group; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --NH.CO.NH--R.sup.3 or --NH.CS.NH--R.sup.3 wherein R.sup.3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom.