THROMBOXANE ANTAGONISTS IN THE TREATMENT OF HORMONE-DEPENDENT NEOPLASIAS

摘要

Compounds having thromboxane antagonistic activity are useful in the treatment of hormone dependent neoplasias, for example estrogen dependent neoplasias. Particularly indicated thromboxane antagonists are compounds of formula (I) in which formula (II) represents one of the bivalent cyclic groups (III), the letters a and b indicating in each case the points of attachment of the substituents R1 and CV ( R2) -NV'R, respectively R1 is a 6-carboxyhex-2-enyl group or a modification thereof in which the group is modified by one, or an appropriate combination of two or more, of the following factors: a) modification of the position of the double bond, b) reduction of the latter, c) modification of the length of the chain by means of a reduction of one or two methylene groups or of an increase of one to six groups methylene, d) replacement of one or two methylene groups each separately with an oxygen or sulfur atom provided that in the modified group, no oxygen or sulfur atom is in an alpha position with respect to either double bond carbon atom either to the carboxy group or one of its derivatives, and that at least two carbon atoms separate any pair of oxygen and / or sulfur atoms; and e) forming an amide, ester or salt derivative of the carboxy group; V and V 'each separately are hydrogen, or together are the second bond of a carbon-nitrogen double bond; R2 is hydrogen, an aliphatic hydrocarbon group, or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulfur atom; and R is a group -NH.CO.NH-R3 or -NH.CS.NH-R3 where R3 is a group of aliphatic hydrocarbons, an aromatic group or a group of aliphatic hydrocarbons substituted by one or more aromatic groups directly or through an oxygen or sulfur atom.