Estrogen receptor alpha and beta ligands, methods of their preparation, and pharmaceutical composition containing them.
Abstract
Estradiol derivatives of general formula II are described, wherein R5 is H, C1-8 aryl or C(O)R group, wherein R is C1-8 alkyl or C6-14 aryl, R4 is H or C1-8 alkyl and X is e.g. C, N, O.
These derivatives are ligands for estrogen receptors alpha and beta and are effective e.g. in hormonal substitution therapy of in treatment of tumour or inflammatory diseases. Further, methods of preparation of these ligands by cyclo-trimerization of ethynylestradiol in organic solvent with an appropriate diyne are described together with the pharmaceutical composition containing them.