abstract |
The compounds are useful for the preparation of drugs intended for tumor and hormonal therapy. They exhibit very strong anti-estrogenic action. Some of these are pure anti-estrogens, some of which have partially estrogenic effects. The substituted 7 - (- aminoalkyl) -estratrienes have the formula wherein the side chain SK represents a residue of formula - (CH2) m --N - CH2 --CH - (CH2) n --Box - (CH2) 3-EA D wherein 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 C 1-5 alkyl group, B and D are always hydrogen or A and B together represent an alkylene group - (CH 2) p - c, p is 2, 3, 4 or 5 and a hydrogen atom or A and D together represent an alkylene group - (CH 2) q - , q is 2, 3 or 4, and B is a hydrogen atom, and E is unsubstituted or one or five times fluorinated ethyl, or the terminal substituent - (CH 2) 3- of the side chain is optionally substituted with a substituted aryl or heteroaryl moiety which is attached directly or via a mono-, di- or trimethylene group to the sulfur atom, R3 represents a hydrogen atom, a hydrocarbon residue of up to 8 carbon atoms, or a residue of the formula R3 -C (O) -, wherein R 3 is a hydrogen or hydrocarbon atom of up to 8 carbon atoms or is a phenyl radical, R 11 is hydrogen, a halogen atom or a nitrooxy group -O-NO 2, R 14, R 15, R 15, R 16 and R 16 always represent a hydrogen atom or R14 and R15 signify an additional bond or a methylene bridge or R15 means a methylene group and R15 represents a hydrogen atom, and |