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    ANTITUMOR WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE
    63.
    发明公开
    ANTITUMOR WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE 有权
    抗氧剂WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE

    公开(公告)号：EP1418921A1

    公开(公告)日：2004-05-19

    申请号：EP02762422.0

    申请日：2002-08-01

    申请人： Schering AG

    发明人： SCHERLITZ-HOFMANN, Ina ,  HOFFMANN, Jens ,  HILLISCH, Alexander ,  UNGER, Eberhard ,  NEUMANN, Tobias ,  SCHWARZ, Sigfrid ,  PETERS, Olaf ,  MICHEL, Thomas

    IPC分类号： A61K31/565 ,  C07J31/00 ,  A61P35/00

    CPC分类号： A61K31/565 ,  C07J31/006

    摘要： The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In said formula, R?1 and R2¿ independently of one another represent H, methyl, C¿1?-C4 acyl or benzyl, R?3¿ represents C¿1?-C4 alkyl, or a group of formula CnFmHo, where n = 1, 2, 3, 4, 5 or 6, m > 1 and m + o = 2n + 1, R?4 and R5¿ independently represent H, or together represent a methylene group or an additional bond, R6 represents H and R7 represents OH, OC¿1?-C4 alkyl, OC1-C11 acyl or OSO2NR?1R2¿, whereby in the B and C ring of the steroid skeleton the broken lines can additionally represent up to two double bonds. The inventive compounds are characterised by a 2-alkoxy substitution in conjunction with a 17-hydroxy substitution. They exhibit the specific activity of inhibiting tubulin polymerisation and can be used, for example, for treating prostatic carcinoma.

    摘要翻译： 本发明涉及通式（I）的2-烷氧基雌激素氨基磺酸酯在制备用于治疗肿瘤疾病的药物中的用途，所述肿瘤疾病受抑制微管蛋白聚合的积极影响。 在所述式中，R 1和R 2彼此独立地表示H，甲基，C 1 -C 4酰基或苄基，R 3'表示C 1 -C 4烷基或式C n F m H o的基团，其中 n = 1,2,3,4,5或6，m> 1和m + o = 2n + 1，R 4和R 5独立地代表H，或一起代表亚甲基或另外的键，R 6代表H 并且R 7代表OH，OC 1 -C 4烷基，OC 1 -C 11酰基或OSO 2 NR 1 R 2，其中在类固醇骨架的B和C环中，虚线可另外代表至多两个双键。 本发明化合物的特征在于2-烷氧基取代与17-羟基取代一起。 它们表现出抑制微管蛋白聚合的特异性活性，并且可以用于例如治疗前列腺癌。

    Neuroactive 3.alpha.-hydroxy-steroids of the androstane and pregnane series
    65.
    发明公开
    Neuroactive 3.alpha.-hydroxy-steroids of the androstane and pregnane series 失效
    Neuroaktive 3.alpha.-Androstan und-Pseudan Steroide

    公开(公告)号：EP1288220A2

    公开(公告)日：2003-03-05

    申请号：EP02025321.7

    申请日：1996-06-06

    申请人： Purdue Pharma Ltd.

    发明人： Upasani, Ravindra B. ,  Hogenkamp, Derk J. ,  Fick, David B. ,  Lan, Nancy C.

    IPC分类号： C07J1/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00

    CPC分类号： C07J31/006 ,  C07J1/0007 ,  C07J1/0029 ,  C07J1/0055 ,  C07J1/0077 ,  C07J17/00 ,  C07J21/00 ,  C07J41/0005 ,  C07J41/005 ,  C07J43/003

    摘要： The invention relates to a 3α-hydroxy, 17-(un)substituted derivatives of the androstane series and 3α-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at the recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having general structural formula (I), wherein R, R 1 , R 2 , R 3 ,R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes pregnanes (R 4 = methyl), 19-norandrostanes, and norpregnanes (R 4 =H).

    摘要翻译： 本发明涉及雄甾烷基系列的3α-羟基，17-（未）取代的衍生物和孕烷系列的3α-羟基，21-取代衍生物。 这些衍生物能够在最近识别的GRC位点起作用，从而以减轻压力，焦虑，失眠，舒适于GRC活性剂（如抑郁症）和癫痫发作活动的情绪障碍的方式调节脑兴奋性。 本发明的类固醇衍生物是具有通式结构式（I）的那些，其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在本文中进一步定义，虚线是单或双 债券。 该结构包括雄甾烷孕烷（R 4 =甲基），19-去雄孕烷和诺孕烷（R4 = H）。

    NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDUNG ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN
    66.
    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.