New7&agr;, 17&agr;-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases

US6767903B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Arwed Cleve · Berlin, DE
• Gerhard Sauer · Berlin, DE
• Christoph Huwe · Berlin, DE
• Karsten Parczyk · Berlin, DE
• Jens Hoffmann · Mühlenbeck, DE
• Martin Schneider · Remchingen, DE

Key dates

• Filing date: Jun 22, 2001
• Grant date: Jul 27, 2004
• Expiry date: Jun 22, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J5/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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-membere…