Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them
申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0002097A1
公开(公告)日:1979-05-30
1-p-Aminoalkoxy phenyl-1-p-hydroxyphenyl-2-phe- nylalk-1-ene derivatives of the formula:
R, = H, lower alkyl
R2 = loweralkyl
or R, and R2 forms a heterocyclic radical with the adjacent N-atom
R3 = halogen or lower alkyl
R4 = H, halogen, OH, lower alkyl or forms with the benzene ring a naphthyl radical
n = 2,3,4,5,6
Possess anti-oestrogenic activity and are useful in the treatment of anovulatory infertility and of breast tumours. Representative of the compounds is I-(p-β-dimethylaminoethoxyphenyl)-trans-I-p-hydroxyphenyl-2-p-tolylbut-I-ene.
式中的 1-对氨基烷氧基苯基-1-对羟基苯基-2-己基烷-1-烯衍生物: R, = H、低级烷基 R2 = 低级烷基或 R,且 R2 与相邻 N 原子形成杂环基 R3 = 卤素或低级烷基 R4 = H、卤素、OH、低级烷基或与苯环形成萘基 n = 2、3、4、5、6 具有抗雌激素活性,可用于治疗无排卵性不孕症和乳腺肿瘤。 其中具有代表性的化合物是 I-(p-β-二甲基氨基乙氧基苯基)-反式-I-对羟基苯基-2-对甲苯丁-I-烯。