7Alpha- (epsilon-aminoalkyl) -stratrienes processes for its preparation Pharmaceutical preparations containing these 7 alpha- (epsilon-aminoalkyl) - stratrienes as well as their use for the preparation of medicines

摘要

The compoundns can be applied for the preparation of medicamentous forms designed for tumour and hormonal therapy. They show very strong antistrogenous effect. Part of them are pure antiestrogens, and another part have partial estrogenous effect. The substituted 7 alpha-(epsilon-aminoalkyl)-estratrines have the formula where the side chain SK means a residue with the formula where m has the value of 4, 5 or 6, n - 0, 1 or 2, x - 0, 1 or 2, A means hydrogen atom or C1-5-alkyl group, B and D are always a hydrogen atom, or C1-5-alkyl group, B & D are always a hydrogen atom, or A & B together mean alkylene group -(CH2)p-c, p is 2,3,4 or 5 and D is hydrogen atom, or A & D together mean alkylene group -(CH2)q- c, q is 2, 3 or 4 and B means hydrogen atom and E is unsubstituted or one or five times fluorinated ethyl residue, or the end substitutent -(CH2)-2-E- of the side chain is optionally substituted by a substituted aryl and heteroaryl residue which is bound directly or by means of mono- di- or trimethylene group to the sulphur atom, R3 means hydrogen atom, carbon residue with up to 8 carbon atoms or residue with the formula where R3' is hydrogen or carbon atom with up to 8 carbon atoms or is phenyl residue, R11 is hydrogen, halogen atom or one nitrooxygroup -O-NO2, R14, R15 alpha,R15 beta, R16 alpha& R16 beta always mean hydrgoen atom or R14 & R15 alpha mean additional bond or methylene bridge, or R15 beta means methylene group and R15 alpha means hydrogen atom, or R15 alpha & R15 beta are alway a methylene group, or R15 beta and R16 beta together form methylene bridge, or R16 alpha or R16 beta means halgen atom or R16 alpha and R16 beta together mean methylidene group and the customary substitutents R14, R15 alpha, R15 beta, R16 alpha and R16 beta are always hydrogen atom, R17' means hydrogen atom in alpha- or beta- position means C1-5-alkyl, C2-5-alkylene or C2-5-alkynyl group or is trifluoromethyl group and R17" is hydrogen atom or residue with formula in which R17''' is hydrogen atom or carbon residue with up to 8 carbon atoms, or when R17' is in alpha- position, R17', together with R14 form ethanol bridge provided that A & B simultaneously do not mean -(CH2)p or A & D togehter do not mean -(CH2)q, at least one substituent of R11, R14, R15 alpha, R15 beta,R16 alpha & R16 beta is not a hydrogen atom. The invention also relates to the physiologically aceptable adjunctive salts of the compounds with organic and inorganic acids. 42 claims, 1 figure