摘要:
The invention relates to new 7α, 17α, 17β-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.
摘要:
This invention provides a pharmaceutically acceptable salt of 5α-pregn-16-en-3β-ol-20-one 3-sulfate ester, which is useful as a progestational agent.
摘要:
This invention provides estra-5(10),7-dien-3β-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3β-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3α-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3β-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3β-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3α-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.
摘要:
This invention presents alkali metal salts of 8,9 dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.