Novel 7-alpha and 17-alpha-bis-alkylated testosterone derivatives and their use for long-term therapy of androgen-dependent diseases

摘要

The invention relates to new 7 alpha , 17 alpha , 17 beta -substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma. In the general formula (I) A is an unbranched C6-C13-alkylene group; B is an oxygen atom, -S(O)p- group, in which p is 0, 1 or 2, an iminocarbonyl group -C(O)N(Y)-, an imino group -N(Y)-, a carbonylimino group -N(Y)C(O)-, a sulfonylimino group -NN(Y)S(O)2-, where Y is a hydrogen atom or a C1-C8-alkyl group, a sulfonyloxy group -OS(O)2-, a dimethylsilyloxy group -O--Si(CH3)2- or a carbonylsulfanyl group -SC(O)- or a bond between A and C or, together with C, a bond between A and D; C is a bond between B and D or, together with B, a bond between A and D or an unbranched C1-C6-alkylene group, a phenylene group, a substituted phenylene group, a five-membered ring or six-membered ring heteroarylene group, a substituted five-membered ring or six-membered ring heteroarylene group or a five-membered ring or six-membered ring heteroarylene group fused with a phenyl ring; and D is a hydrogen atom, a C1-C4-alkyl group, a vinyl group, a C1-C4-alkoxy group, a C1-C4-alkoxycarbonyl group, a bis(C1-C4-alkoxycarbonyl)methyl group, an acetyl(C1-C4-alkoxycarbonyl)methyl group, a cyan group, a carboxy group, an azide group, a hydroxy group, a halogen atom or a rest of the formula CnFmHo, in which n is 1, 2, 3 or 4, m 1 and m+o = 2n+1.