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1. 发明授权

EP1144431B1 16-HYDROXYESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE 有权
标题翻译： 16 hydroxyestratrienes有选择活性雌激素
公开(公告)号：EP1144431B1
公开(公告)日：2005-12-21
申请号：EP00907539.1
申请日：2000-02-09
申请人： Schering Aktiengesellschaft
发明人： KÜNZER, Hermann , KNAUTHE, Rudolf , LESSL, Monika , FRITZEMEIER, Karl-Heinrich , HEGELE-HARTUNG, Christa , BÖMER, Ulf , MÜLLER, Gerd , KOSEMUND, Dirk
IPC分类号： C07J53/00 , C07J1/00 , A61K31/565 , C07J31/00 , C07J41/00 , C07J33/00 , C07J15/00
CPC分类号： C07J41/0094 , C07J1/0055 , C07J1/0066 , C07J15/00 , C07J31/006 , C07J33/002 , C07J53/004
摘要： The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably have in vivo a preferential effect on bones as compared to the uterus and/or a marked effect with regard to the stimulation of the expression of the 5HT2a receptor and transporter. The invention also relates to the production and to the use in therapy of these compounds and to pharmaceutical administration forms containing said novel compounds. The novel compounds are 16 alpha and 16 beta hydroxy-estra,1,3,5(10)-estratriene which carry additional substituents at the steroid backbone and one or more additional double bonds on the B, C and/or D rings.

2. 发明授权

EP1517914B1 9-ALPHA-SUBSTITUIERTE ESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE 有权
标题翻译： 9-ALPHA-SUBSTITUIERTE ESTROGENE ALS SELEKTIV WIRKSAME ESTROGENE
公开(公告)号：EP1517914B1
公开(公告)日：2005-08-31
申请号：EP03757065.2
申请日：2003-06-11
申请人： Schering Aktiengesellschaft
发明人： KOSEMUND, Dirk , MÜLLER, Gerd , HILLISCH, Alexander , FRITZEMEIER, Karl-Heinrich , MUHN, Peter
IPC分类号： C07J1/00
CPC分类号： C07J1/0055 , C07J1/0066 , C07J41/0072 , C07J63/008
摘要： The invention relates to novel 9 alpha -substituted estratrienes of general formula (I) - wherein R3, R7, R7', R13, R16, R17 and R17' have the designations cited in the description, and R9 represents a linear-chain or branched-chain, optionally partially or fully halogenated alkenyl radical comprising between 2 and 6 carbon atoms, or an ethinyl radical or a prop-1-inyl radical - as pharmaceutical active ingredients which have, in vitro, a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparation of the rat uterus, and, in vivo, preferably a preferential action on the ovary compared to the uterus. The invention also relates to the production of said estratrienes, to the therapeutic application thereof and to pharmaceutical forms of administration containing the novel compounds. The invention further relates to the use of said compounds for treating illnesses and states related to estrogen deficiency.
摘要翻译：本发明涉及通式（I）的新型9α-取代的雌三烯 - 其中R 3，R 7，R 7'，R 13，R 16，R 17和R 17'具有说明书中引用的名称，并且R 9表示直链或支链 - 链，任选地包含2至6个碳原子的部分或完全卤代的烯基，或者乙炔基或丙-1-烯基 - 作为药物活性成分，其在体外对雌激素受体制剂具有较高的亲和力大鼠前列腺而不是大鼠子宫的雌激素受体制备，并且在体内优选对子宫相对于子宫的优先作用。本发明还涉及所述雌三烯的生产，其治疗应用以及含有所述新化合物的药物施用形式。本发明还涉及所述化合物用于治疗与雌激素不足有关的疾病和状态的用途。

3. 发明授权

EP0837874B1 NEUROACTIVE STEROIDS OF THE ANDROSTANE AND PREGNANE SERIES 失效
标题翻译： NEURO ACTIVE类固醇雄和孕
公开(公告)号：EP0837874B1
公开(公告)日：2004-12-15
申请号：EP96919372.1
申请日：1996-06-06
申请人： Euro-Celtique S.A.
发明人： UPASANI, Ravindra, B. , FICK, David, B. , HOGENKAMP, Derk, J. , LAN, Nancy, C.
IPC分类号： C07J1/00 , C07J43/00 , C07J41/00
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 3 alpha -hydroxy, 17-(un)substituted derivatives of the androstane series and 3 alpha -hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a 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, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes pregnanes (R4 = methyl), 19-norandrostanes, and norpregnanes (R4 = H).

4. 发明授权

EP0615448B1 SEX STEROID ACTIVITY INHIBITORS 失效
标题翻译： SEX STEROIDE INHIBITONEN
公开(公告)号：EP0615448B1
公开(公告)日：2002-05-02
申请号：EP92923641.2
申请日：1992-12-01
申请人： ENDORECHERCHE INC.
发明人： LABRIE, Fernand , MERAND, Yves
IPC分类号： A61K31/352 , A61K31/4433 , A61K31/4025 , C07D311/04
CPC分类号： C07D295/185 , A61K31/10 , A61K31/135 , A61K31/138 , A61K31/165 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , C07C215/64 , C07C217/18 , C07C235/34 , C07C317/18 , C07C2602/10 , C07D215/14 , C07D217/16 , C07D235/18 , C07D295/088 , C07D295/096 , C07D311/60 , C07D335/06 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0055 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J1/0081 , C07J1/0085 , C07J1/0096 , C07J17/00 , C07J21/006 , C07J21/008 , C07J41/0072 , C07J41/0094 , C07J51/00 , C07J53/008 , C07J71/001 , C07J71/0021
摘要： Inhibitors of sex steroid activity, for example those having general structure (A) may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
摘要翻译：性类固醇活性的抑制剂，例如具有一般结构的那些可以用作药物组合物的一部分，以提供抗雌激素作用和/或抑制雌激素合成。这样的药物组合物可用于治疗通过激活性类固醇受体来辅助其进展的乳腺癌或其它疾病。

5. 发明公开

EP0783513A4 NOVEL ESTRENES FOR INDUCING HYPOTHALAMIC EFFECTS 失效
标题翻译： ESTRENE ZUR INDUZIERUNG HYPOTHELAMISCHER EFFEKTE
公开(公告)号：EP0783513A4
公开(公告)日：2000-03-08
申请号：EP95935237
申请日：1995-09-29
申请人： PHERIN CORP
发明人： BERLINER DAVID L , ADAMS NATHAN W , JENNINGS-WHITE CLIVE L
IPC分类号： A61P25/00 , C07J1/00 , C07J3/00 , C07J13/00 , C07J31/00 , C07J41/00 , C07J53/00 , C07J71/00 , C07J75/00 , A61K31/56 , A61K31/565
CPC分类号： C07J1/0081 , C07J1/0007 , C07J1/0055 , C07J3/00 , C07J13/002 , C07J13/005 , C07J13/007 , C07J31/006 , C07J41/0005 , C07J71/001 , C07J75/005
摘要： The invention relates to estrene steroid, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. The figure illustrates the synthesis of 1,3,5(10),16-estratetraen-3-ol.
摘要翻译：本发明涉及与神经上皮受体结合的雌激素类固醇。类固醇优选以含有一种或多种药学上可接受的载体的药物组合物的形式施用。该图说明了1,3,5（10），16-雌三烯-3-醇的合成。

6. 发明授权

EP0363128B1 Anti-androgen compounds 失效转让
标题翻译：抗雄虫化合物
公开(公告)号：EP0363128B1
公开(公告)日：1993-09-01
申请号：EP89310063.6
申请日：1989-10-02
申请人： ARCH DEVELOPMENT CORPORATION
发明人： Liao. Shutsung , Harvey, Ronald, G , Pataki, John
IPC分类号： A61K31/56 , C07J1/00 , C07C49/225 , C07C33/34 , C07C69/017 , C07C39/17 , C07J63/00 , C07C49/237 , C07D303/04 , C07C33/36 , A61K31/045
CPC分类号： C07J63/008 , A61K31/045 , A61K31/05 , A61K31/12 , A61K31/22 , C07C39/17 , C07C45/513 , C07C45/516 , C07C49/657 , C07C49/665 , C07C49/747 , C07C49/753 , C07C49/792 , C07C2603/26 , C07J1/0055 , C07J1/0059 , C07J1/007 , C07J1/0088

7. 发明公开

EP0946583A1 BISSTEROIDAL COMPOUNDS AND THEIR USE FOR THE PREPARATION OF CHIRAL COMPLEXES 失效
标题翻译：类固醇二聚体化合物及其使用用于生产手性COMPLEXEN
公开(公告)号：EP0946583A1
公开(公告)日：1999-10-06
申请号：EP97954819.0
申请日：1997-12-18
申请人： Schering Aktiengesellschaft
发明人： MOHR, Jörg-Torsten , ENEV, Valentien , EWERS, Christian , HARRE, Michael , HICKISCH, Klaus
IPC分类号： C07J1 , C07J31 , C07J51
CPC分类号： C07J31/006 , C07J1/0055 , C07J1/0077 , C07J51/00
摘要： Bissteroidal compounds of general formula (I), in which R1 stands for hydrogen, alkyl, acyl, fluorine, and X1R5, where X1 stands for oxygen and sulfur and R5 can either be hydrogen, alkyl, aryl; R2 stands for hydrogen and alkyl; the stereochemistry of C-13, C-14 and C-17 may either be a or b; X stands for oxygen, hydroxyl, trifluormethylsulfonyloxy, or (R6)2P, where R6 can be aryl, alkyl and cycloalkyl; R3 stands for hydrogen, alkyl, aryl, trialkylsilyl, fluorine and X2R6, where X2 stands for oxygen and sulfur and R6 stands for hydrogen, trifluormethylsulfonyl, alkyl, cycloalkyl or aryl. R4 can either be a substituent in the 6 or 7 position of the steroid with the meaning of hydrogen, alkyl, aryl, fluorine, and X3R7, where X3 stands for oxygen, sulfur or trialkylsilyl and R7 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl, and the B-ring of the steroid contains none or two double bonds. Enantio- and Diastereomeric derivatives of compounds of general formula (I), metal complexes thereof and their use in enantioselective reactions.

8. 发明公开

EP0924219A2 Novel estrenes for inducing hypothalamic effects 失效
标题翻译： Estrene zur Induzierung hypothalamischer Effekte
公开(公告)号：EP0924219A2
公开(公告)日：1999-06-23
申请号：EP98203950.5
申请日：1995-09-29
申请人： PHERIN CORPORATION
发明人： Berliner, David L. , Adams, Nathan William , Jennings-white, Clive L.
IPC分类号： C07J1/00 , A61K31/565 , C07J3/00 , C07J31/00 , C07J53/00 , C07J13/00 , C07J41/00 , C07J71/00 , A61K31/56
CPC分类号： C07J1/0081 , C07J1/0007 , C07J1/0055 , C07J3/00 , C07J13/002 , C07J13/005 , C07J13/007 , C07J31/006 , C07J41/0005 , C07J71/001 , C07J75/005
摘要： The invention relates to estrene steroids, which bind to neuroepithelial cells in the human vomeronasal organ. The steroids are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Figure (1) illustrates the synthesis of 1,3,5(10), 16-estratetraen-3-ol.
摘要翻译：本发明涉及雌激素类固醇，其结合人类犁鼻器官中的神经上皮细胞。类固醇优选以含有一种或多种药学上可接受的载体的药物组合物的形式施用。图（1）说明1,3,5（10），16-雌四烯-3-醇的合成。

9. 发明公开

EP0849274A1 Bissteroidal compounds and their use for the preparation of chiral complexes 失效
标题翻译： Steroid-Dimer Verbindungen und ihre Verwendung zur Herstellung chiraler Komplexe
公开(公告)号：EP0849274A1
公开(公告)日：1998-06-24
申请号：EP96250295.1
申请日：1996-12-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： Mohr, Jörg-Torsten, Dr. , Enev, Valentien, Dr. , Ewers, Christian, Dr. , Harre, Michael, Dr. , Nickisch, Klaus, Dr.
IPC分类号： C07J1/00 , C07J31/00 , C07J51/00
CPC分类号： C07J31/006 , C07J1/0055 , C07J1/0077 , C07J51/00
摘要： Bissteroidal compounds of general formula I
in which

R 1 stands for hydrogen, alkyl, acyl, fluorine, and X 1 R 5 ,
where X 1 stands for oxygen and sulfur and
R 5 can either be hydrogen, alkyl, aryl,
R 2 stands for hydrogen and alkyl; the stereochemistry of C-13, C-14 and C-17 may either be α or β,
X stands for oxygen, trifluormethylsulfonyloxy, or (R 6 ) 2 P,
where R 6 can be aryl, alkyl and cycloalkyl,
R 3 stands for hydrogen, alkyl, aryl, trialkylsilyl, fluorine and X 2 R 6 ,
where X 2 stands for oxygen and sulfur and
R 6 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl.
R 4 can either be a substituent in the 6 or 7 position of the steroid with the meaning of hydrogen, alkyl, aryl, fluorine, and X 3 R 7 ,
where X 3 stands for oxygen, sulfur or trialkylsilyl and R 7 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl,
and the B-ring of the steroid contains none or two double bonds.
Enantio- and Diastereomeric derivatives of compounds of general formula I, metal complexes thereof and their use in enantioselective reactions.
摘要翻译：通式I 的双星型化合物，其中R1代表氢，烷基，酰基，氟和X1R5，其中X1代表氧和硫，R5可以是氢，烷基，芳基，R2代表氢和烷基; C-13，C-14和C-17的立体化学可以是α或β，X代表氧，三氟甲基磺酰氧基或（R6）2P，其中R6可以是芳基，烷基和环烷基，R3代表氢，烷基，芳基，三烷基甲硅烷基，氟和X2R6，其中X2代表氧和硫，R6代表氢，三氟甲磺酰基，烷基或芳基。 R4可以是类固醇的6或7位的取代基，具有氢，烷基，芳基，氟和X3R7的含义，其中X3表示氧，硫或三烷基甲硅烷基，R7表示氢，三氟甲磺酰基，烷基或芳基，并且类固醇的B环含有无或两个双键。通式I化合物的对映异构体和非对映体衍生物，其金属络合物及其在对映选择性反应中的用途。

10. 发明公开

EP0783513A1 NOVEL ESTRENES FOR INDUCING HYPOTHALAMIC EFFECTS 失效
标题翻译：新的诱导下丘脑作用的药物
公开(公告)号：EP0783513A1
公开(公告)日：1997-07-16
申请号：EP95935237.0
申请日：1995-09-29
申请人： PHERIN CORPORATION
发明人： BERLINER, David, L. , ADAMS, Nathan, W. , JENNINGS-WHITE, Clive, L.
IPC分类号： A61P25 , C07J1 , C07J3 , C07J13 , C07J31 , C07J41 , C07J53 , C07J71 , C07J75
CPC分类号： C07J1/0081 , C07J1/0007 , C07J1/0055 , C07J3/00 , C07J13/002 , C07J13/005 , C07J13/007 , C07J31/006 , C07J41/0005 , C07J71/001 , C07J75/005
摘要： The invention relates to estrene steroids, which bind to neuroepithelial cells in the human vomeronasal organ. The steroids are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Figure (1) illustrates the synthesis of 1,3,5(10),16-estratetraen-3-ol.
摘要翻译：本发明涉及与人犁鼻器官中的神经上皮细胞结合的雌激素类固醇。类固醇优选以含有一种或多种药学上可接受的载体的药物组合物的形式施用。图（1）说明了1,3,5（10），16-雌三烯-3-醇的合成。

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