Patent ID: 6677324
Filing Date: 2004-01-13
Classification: A61K,A61P

Abstract:
Combination preparation of an oestrogen and an antioestrogen, characterized in that the oestrogen is selected from the group consisting of 17-&bgr;-oestradiol, 17-&agr;-ethynyloestradiol, oestriol, oestrone, oestrone sulphate, oestrogen sulphamates, 17&agr;-oestradiol, mestranol, stilbestrol, esters of 17&bgr;-oestradiol,oestradiol valerate and naturally conjugated oestrogens and in that the antioestrogen is a substituted 7&agr;-(&xgr;-aminoalkyl)oestratriene of the general formula I â€ƒin which the side chain SK is a radical of the subformula where m is 4, 5 or 6, n is 0, 1 or 2, x is 0, 1 or 2, A is a hydrogen atom or a C1-5-alkyl group, B and D are each a hydrogen atom, or A and B together are an alkylene group â€”(CH2)pâ€” with p=2, 3, 4 or S and D is a hydrogen atom or A and D together are an alkylene group â€”(CH2)q- with q=2, 3 or 4 and B is a hydrogen atom, and E is an unsubstituted or mono- to pentafluorinated ethyl radical, or the terminal substituent â€”(CH2)3â€”E in the side chain is replaced by an optionally substituted aryl or heteroaryl radical which is bonded to the sulphur atoms directly or via a mono-, di- or trimethylene group, R3 is a hydrogen atom, a hydrocarbon radical having up to 8 carbon atoms or a radical of the subformula R3â€²â€”C(O)â€”, in which R3â€² is a hydrogen atom or a hydrocarbon radical having up to 8 carbon atoms or a phenyl radical, R11 is a hydrogen atom, a halogen atom or a nitrooxy group â€”Oâ€”NO2, R14, R15&agr;, R15&bgr;, R16&agr; and R16&bgr; are each a hydrogen atom or R14 and R15&agr; are an additional bond or a methylene bridge, or R15&bgr; is a methyl group and R15&agr; is a hydrogen atom, or R15&agr; and R15&bgr; are each a methyl group, or R15&bgr; and R16&bgr; together are a methylene bridge, or R16&agr; or R16&bgr; is a halogen atom or R16&agr; and R16&bgr; together are a methylidene group and the remaining substituents R14, R15&agr;, R15&bgr;, R16&agr; and R16&bgr; are each a hydrogen atom, R17â€² in the &agr;- or &bgr;-position is a hydrogen atom, a C1-5-alkyl, C2-5-alkenyl or C2-5-alkynyl group or a trifluoromethyl group and R17â€³ is a hydrogen atom or a radical of the subformula R17â€²â€³â€”C(O)â€”, in which R17â€²â€³ is a hydrogen atom or a hydrocarbon radical having up to 8 carbon atoms, or, if R17â€² is located in the &agr;-position, R17â€² additionally together with R14 is an ethanobridge, with the proviso that, if A and B together are not â€”(CH2)pâ€” or A and D together are not â€”(CH2)qâ€”, at least one of the substituents R11, R14, R15&agr;, R15&bgr;, R16&agr; and R16&bgr; is not a hydrogen atom, and their physiologically tolerable addition salts with organic and inorganic acids.