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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
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

EP3171855A4 HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF 有权
公开(公告)号：EP3171855A4
公开(公告)日：2018-04-04
申请号：EP15824579
申请日：2015-07-23
申请人： SPHAERA PHARMA PVT LTD
发明人： DUGAR SUNDEEP , MAHAJAN DINESH , SCHREINER GEORGE FREDERICK
IPC分类号： A61K8/63 , C07J1/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J17/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J73/00 , C12P33/08 , C12P33/20
CPC分类号： C07J73/005 , C07J1/0007 , C07J1/0011 , C07J1/0022 , C07J1/0037 , C07J1/004 , C07J1/0051 , C07J1/0055 , C07J1/007 , C07J1/0085 , C07J3/00 , C07J3/005 , C07J7/002 , C07J7/005 , C07J7/007 , C07J9/00 , C07J17/00 , C07J41/0011 , C07J41/0016 , C07J41/0038 , C07J41/0044 , C07J41/0066 , C07J41/0072 , C07J41/0088 , C07J43/003 , C07J51/00
摘要： The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

8. 发明授权

EP1298115B1 PROCESS FOR THE PREPARATION OF POLYHYDRIC ALCOHOLS 有权
标题翻译：用于生产多元醇
公开(公告)号：EP1298115B1
公开(公告)日：2009-08-26
申请号：EP01947836.1
申请日：2001-07-05
申请人： National Institute of Advanced Industrial Science and Technology , Otsuka Chemical Co., Ltd.
发明人： KATO, Syunsaku , SUZUKI, Daisuke, c/o Tokushima Lab. , SEO, Yoshiko, c/o Tokushima Lab.
IPC分类号： C07B41/02 , C07C37/055 , C07C39/12 , C07C39/14 , C07D213/69 , C07D239/52 , C07D239/60 , C07D251/16 , C07D253/04 , C07D253/06 , C07D309/30 , C07D311/30 , C07J1/00
CPC分类号： C07J1/0077 , C07B41/02 , C07C37/055 , C07C2603/42 , C07D213/69 , C07D309/30 , C07J1/00 , C07J1/0055 , C07J1/007 , Y02P20/55 , C07C39/14 , C07C39/12 , C07C39/10
摘要： A process for the preparation of polyhydric alcohols which comprises subjecting a polyhydric alcohol whose hydroxyl groups are protected to irradiation with microwave in the presence of either a basic compound or an acid exhibiting at 25°C an acid dissociation constant (pKa) of -8 to 3 to thereby conduct deblocking. According to this process, polyhydric alcohols whose hydroxyl groups are protected can be easily deblocked to thereby attain industrially advantage preparation of polyhydric alcohols.

9. 发明公开

EP1298115A4 PROCESS FOR THE PREPARATION OF POLYHYDRIC ALCOHOLS 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG MEHRWERTIGER ALKOHOLE
公开(公告)号：EP1298115A4
公开(公告)日：2005-11-16
申请号：EP01947836
申请日：2001-07-05
申请人： NAT INST OF ADVANCED IND SCIEN , OTSUKA CHEMICAL CO LTD
发明人： KATO SYUNSAKU , SUZUKI DAISUKE , SEO YOSHIKO
IPC分类号： C07B41/02 , C07C37/055 , C07D213/69 , C07D309/30 , C07J1/00 , C07C39/12 , C07C39/14 , C07D239/52 , C07D239/60 , C07D251/16 , C07D253/04 , C07D253/06 , C07D311/30
CPC分类号： C07J1/0077 , C07B41/02 , C07C37/055 , C07C2603/42 , C07D213/69 , C07D309/30 , C07J1/00 , C07J1/0055 , C07J1/007 , Y02P20/55 , C07C39/14 , C07C39/12 , C07C39/10
摘要： A process for the preparation of polyhydric alcohols which comprises subjecting a polyhydric alcohol whose hydroxyl groups are protected to irradiation with microwave in the presence of either a basic compound or an acid exhibiting at 25°C an acid dissociation constant (pKa) of -8 to 3 to thereby conduct deblocking. According to this process, polyhydric alcohols whose hydroxyl groups are protected can be easily deblocked to thereby attain industrially advantage preparation of polyhydric alcohols.
摘要翻译：根据本发明的制备多元醇的方法包括在具有酸解离指数（pKa）的碱性化合物或酸的存在下，使具有被保护的羟基的多元醇化合物进行微波照射 -8至3在25℃下除去多元醇化合物的羟基的保护基。本发明可以通过容易地从多元醇化合物的被保护的羟基中除去保护基来提供工业上有利的制备多元醇的方法。

10. 发明授权

EP0811006B1 BENZOPYRAN-CONTAINING COMPOUNDS AND METHOD FOR THEIR USE 失效
标题翻译：苯并吡喃含氮化合物及使用方法
公开(公告)号：EP0811006B1
公开(公告)日：2003-05-02
申请号：EP96902191.4
申请日：1996-02-20
申请人： ENDORECHERCHE INC.
发明人： LABRIE, Fernand , MERAND, Yves , GAUTHIER, Sylvain
IPC分类号： C07D311/60 , A61K31/35
CPC分类号： 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 , C07D295/088 , C07D295/096 , C07D295/185 , C07D311/60 , C07D335/06 , C07J1/0055 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J1/0085 , C07J17/00 , C07J21/006 , C07J21/008 , C07J41/0072 , C07J41/0094 , C07J51/00 , C07J53/008 , C07J71/001 , C07J71/0021
摘要： Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailibility, and preferred stereoisomers are shown to be more effective than racemic mixtures.

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