| 摘要 |
<p>The invention relates to 11β-aryl-substituted 14,17-ethano-oestratriens of general formula (I), in which R1 is a hydrogen atom, a C¿1?-C12-alkanoyl-, a benzoyl-, a straight-chain or branched C1-C12-alkyl-, a C3-C7-cycloalkyl- or a C4-C8-alkyl cycloalkyl group, which can all optionally be substituted; R?2¿ is a hydrogen atom or an optionally substituted C¿1?-C12-alkanoyl group; R?3¿ stands for a group in which n = 4, 5, 6, or 7; m = 0, 1 or 2; R4 or R5 are, independently of each other, a hydrogen atom or a straight-chain or branched, optionally substituted C¿1?-C8-alkyl group, which can also be partially or completely fluorinated, or R?4 and R5¿ together mean a methylene to pentamethylene group -(CH¿2?)p-(p=1-5); and R?6¿ is the same as R4 or R5, or is an optionally substituted aryl or aryl alkyl radical, whereby said alkyl radical can have up to 6 carbon atoms, and the aryl radical, on its own or in the aryl alkyl radical, is a 5 or 6-link monocyclic ring or a condensed 8-10-link ring system, and the aryl radical can have one or more heteroatoms selected from oxygen, nitrogen, and sulphur. The new compounds are selective oestrogens whose effect is tissue-selective. In particular, the oestrogenic effect occurs on bone, in the cardiovascular system and in the central nervous system. However, it has little or no oestrogenic effect on the uterus and the liver. The compounds are suitable for producing medicaments which are used in many indications (for example, for hormone replacement therapy, prevention and treatment of osteoporosis).</p> |
