New7amp;agr;, 17amp;agr;-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases

摘要

The invention relates to new 7&agr;, 17&agr;, 17&bgr;-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-alkoxybonyl)methyl group, a cyan group, a carboxy group, an azide group, a hydroxy group, a halogen atom or a rest of the formula C_nF_mH_o, in which n is 1, 2, 3 or 4, m1 and m+o=2n+1.