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    NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDUNG ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN
    1.
    发明授权
    NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDUNG ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN 有权
    NEW 7-α，17-α-二TO-烷基化睾酮衍生物及其使用雄激素依赖性疾病的长期治疗

    公开(公告)号：EP1140972B1

    公开(公告)日：2003-03-05

    申请号：EP99967003.7

    申请日：1999-12-23

    申请人： Schering Aktiengesellschaft

    发明人： CLEVE, Arwed ,  SAUER, Gerhard ,  HUWE, Christoph ,  PARCZYK, Karsten ,  HOFFMANN, Jens ,  SCHNEIDER, Martin

    IPC分类号： C07J1/00 ,  A61K31/565 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J33/00 ,  C07J51/00

    CPC分类号： C07J51/00 ,  C07J1/0033 ,  C07J1/0037 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0038 ,  C07J41/0094 ,  C07J43/003

    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.

    NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDING ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN
    3.
    发明公开
    NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDING ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN 有权
    NEW 7-α，17-α-二TO-烷基化睾酮衍生物及其VERWENDING长期治疗雄激素依赖性疾病

    公开(公告)号：EP1140972A1

    公开(公告)日：2001-10-10

    申请号：EP99967003.7

    申请日：1999-12-23

    申请人： Schering Aktiengesellschaft

    发明人： CLEVE, Arwed ,  SAUER, Gerhard ,  HUWE, Christoph ,  PARCZYK, Karsten ,  HOFFMANN, Jens ,  SCHNEIDER, Martin

    IPC分类号： C07J1/00 ,  A61K31/565 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J33/00 ,  C07J51/00

    CPC分类号： C07J51/00 ,  C07J1/0033 ,  C07J1/0037 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0038 ,  C07J41/0094 ,  C07J43/003

    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.

    ANTIGESTAGEN WIRKSAME STEROIDE MIT FLUORIERTER 17ALPHA-ALKYLKETTE
    6.
    发明公开
    ANTIGESTAGEN WIRKSAME STEROIDE MIT FLUORIERTER 17ALPHA-ALKYLKETTE 失效

    公开(公告)号：EP0970103A1

    公开(公告)日：2000-01-12

    申请号：EP98905419.2

    申请日：1998-02-09

    申请人： Schering Aktiengesellschaft

    发明人： SCHWEDE, Wolfgang ,  CLEVE, Arwed ,  KLAR, Ulrich ,  NEEF, Günter ,  CHWALISZ, Kristof ,  SCHNEIDER, Martin ,  FUHRMANN, Ulrike ,  HESS-STUMPP, Holger

    IPC分类号： C07J41/00 ,  A61K31/56 ,  C07J53/00 ,  C07J1/00 ,  C07J43/00

    CPC分类号： C07J1/0033 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J53/002

    摘要： New 17α-fluoralkyl steroids have general formula (I), in which R1 stands for a methyl or ethyl group; R2 for a radical of formula C¿n?FmHo, in which n equals 2, 3, 4, 5 or 6, m⊃1 and m+o = 2n+1; R?3¿ stands for a free, etherified or esterified hydroxy group; R?4 and R5¿ stand each for a hydrogen atom, or together for an additional bond or a methylene group; St stands for a steroidal ABC ring system of partial formulas (A), (B) or (C), in which R6 stands for a hydrogen atom, a straight chain C¿1?-C4- or branched chain C3-C4-alkyl group or a halogen atom; R?7¿ stands for a hydrogen atom, a straight chain C¿1?-C4- or branched chain C3-C4-alkyl group or, when St stands for a steroidal ABC ring system of formulas (A) or (B), R?6 and R7¿ can form together an additional bond; X stands for an oxygen atom, an hydroxyimino group =N∩OH or two hydrogen atoms; R8 stands for a radical Y or for an aryl radical optionally substituted several times with a group Y, in which Y stands for a hydrogen atom, a halogen atom, an -OH, -NO¿2?, -N3, -CN, -NR?9aR9b¿, -NHSO¿2?R?9, -CO¿2R9, C1-C10-alkyl, C1-C10-alkoxy, C1-C10-alcanoyloxy, benzoyloxy, C1-C10-alkanoyl, C1-C10-hydroxyalkyl or benzoyl group, and R?9a and R9b¿ are the same or different and like R9 represent a hydrogen atom or a C¿1?-C10-alkyl group. Also disclosed are the physiologically admissible salts of these steroids with acids, when they contain the radicals NR?9aR9b¿, and their physiologically admissible salts with bases, when they contain the radicals -CO¿2R?9, in which R9 stands for hydrogen. These new compounds display an extraordinarily strong antigestagenic activity and are suitable for preparing pharmaceutical compositions.

    摘要翻译： 新的17α-氟烷基甾族化合物具有通式（I），其中R 1代表甲基或乙基; R2代表式C≡nFmHo的基团，其中n等于2,3,4,5或6，m⊃1和m + o = 2n + 1; R 3'代表游离的醚化或酯化的羟基; R 4和R 5分别代表氢原子或一起代表另外的键或亚甲基; St表示部分式（A），（B）或（C）的甾族ABC环系，其中R 6代表氢原子，直链C 1 -C 4或支链C 3 -C 4烷基 基团或卤素原子; R 7代表氢原子，直链C 1 -C 4 - 或支链C 3 -C 4 - 烷基，或当St代表式（A）或（B）的甾体ABC环系时， R 6和R 7可以一起形成另外的键; X代表氧原子，羟基亚氨基=N∩OH或两个氢原子; R 8代表基团Y或任选用基团Y取代若干次的芳基，其中Y代表氢原子，卤素原子，-OH，-NO 2，-N 3，-CN， - -NR 9 R 9，-CO 2 R 9，C 1 -C 10烷基，C 1 -C 10烷氧基，C 1 -C 10烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟基烷基 或苯甲酰基，而R 9a和R 9b可以相同或不同，和R 9一样代表氢原子或C 1 -C 10烷基。 还公开了当这些甾族化合物含有基团-NR9aR9b'时，这些甾族化合物与酸的生理上可接受的盐，以及当它们含有基团-CO2R9，其中R9代表氢时，它们与碱的生理上可接受的盐。 这些新化合物表现出非常强的抗孕激素活性并且适用于制备药物组合物。