Title:
【発明の名称】新規7-アルファおよび17-アルファ-ビス-アルキル化テストステロン誘導体とアンドロゲン依存疾患の長期療法へのその使用
Document Type and Number:
Japanese Patent JP2002533471
Kind Code:
A
Abstract:
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.
Inventors:
Kleve, Albert
Sauer, Gerhard
Hoube, Christoph
Parzic, Karlsten
Hoffman, Jens
Schneider, martin
Sauer, Gerhard
Hoube, Christoph
Parzic, Karlsten
Hoffman, Jens
Schneider, martin
Application Number:
JP2000591059A
Publication Date:
October 08, 2002
Filing Date:
December 23, 1999
Export Citation:
Assignee:
Schering Actien Gezel Shaft
International Classes:
A61K31/565; A61P5/28; A61P17/14; A61P35/00; C07J1/00; C07J7/00; C07J17/00; C07J31/00; A61K31/569; C07J33/00; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): C07J1/00; A61K31/569; A61P5/28; A61P17/14; A61P35/00; C07J7/00; C07J17/00; C07J31/00
Attorney, Agent or Firm:
Takashi Ishida (4 others)