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1. 发明申请

WO2002081444A1 1-INDOLYLDERIVATE, DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN, EIN VERFAHREN ZUR HERSTELLUNG DER 1-INDOLYLDERIVATE SOWIE 1-INDOLYLDERIVATE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 审中-公开
标题翻译： 1-吲哚基，它们在药物的生产，方法1-吲哚基和1-吲哚基药物制剂的生产
公开(公告)号：WO2002081444A1
公开(公告)日：2002-10-17
申请号：PCT/EP2002/003646
申请日：2002-04-03
申请人： SCHERING AKTIENGESELLSCHAFT , ANGERER VON, Erwin , HOFFMANN, Jens , BOHLMANN, Rolf , JAUTELAT, Rolf , HEINRICH, Nicolaus , LICHTNER, Rosemarie , GOLOB, Thomas , WALTER, Georg
发明人： ANGERER VON, Erwin , HOFFMANN, Jens , BOHLMANN, Rolf , JAUTELAT, Rolf , HEINRICH, Nicolaus , LICHTNER, Rosemarie , GOLOB, Thomas , WALTER, Georg
IPC分类号： C07D209/12
CPC分类号： C07D401/06 , A61K31/40 , A61K31/404 , C07D209/12 , C07D209/56
摘要： Die Erfindung betrifft neuartige 1-Indolylderivate mit der allgemeinen Formel (II) mit antiestrogener Wirkung, wobei R 1 , R 2 , R 3 , R 4 sowie U, V, W, X, Y und Z die in der Beschreibung angegebenen Bedeutungen haben, sowie ein Verfahren zur Herstellung der 1-Indolylderivate, deren Verwendung zur Herstellung von Arzneimitteln sowie 1-Indolylderivate enthaltende pharmazeutische Präparate.
摘要翻译：本发明涉及一种具有抗雌激素作用的通式（II），其中R <1>，R <2>，R <3>，R <4>和U，V，W，X，Y和Z新颖的1-吲哚衍生物具有说明书中给出的含义，以及用于制备1吲哚基衍生物，涉及它们用于制备药物的用途以及1-吲哚衍生物含有它们的药物组合物的方法。

2. 发明申请

WO2003074053A1 USE OF EPOTHILONES IN THE TREATMENT OF BRAIN DISEASES ASSOCIATED WITH PROLIFERATIVE PROCESSES 审中-公开
标题翻译： EPOTHILONES在治疗与增殖过程相关的脑疾病中的应用
公开(公告)号：WO2003074053A1
公开(公告)日：2003-09-12
申请号：PCT/EP2003/002085
申请日：2003-02-28
申请人： SCHERING AG , LICHTNER, Rosemarie , ROTGERI, Andrea , KLAR, Ulrich , HOFFMANN, Jens , BUCHMANN, Bernd , SCHWEDE, Wolfgang , SKUBALLA, Werner
发明人： LICHTNER, Rosemarie , ROTGERI, Andrea , KLAR, Ulrich , HOFFMANN, Jens , BUCHMANN, Bernd , SCHWEDE, Wolfgang , SKUBALLA, Werner
IPC分类号： A61K31/428
CPC分类号： A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4427 , A61K31/4709
摘要： This invention provides the use of an Epothilone, which shows an average distribution coefficient between plasma and brain of 0.3 to 1.5 in the mouse intravenous bolus injection assay, for the preparation of a medicament for the treatment of a brain disease associated with proliferative processes.
摘要翻译：本发明提供了用于制备用于治疗与增殖过程相关的脑疾病的药物的埃坡霉素的用途，其在小鼠静脉推注注射测定中显示血浆和脑之间的平均分布系数为0.3至1.5。

3. 发明申请

WO2002094379A1 USE AND COMPOSITIONS OF ANTIPROGESTINS FOR TREATMENT OF PROSTATE DISEASES 审中-公开
标题翻译：用于治疗前列腺疾病的抗生素的使用和组合
公开(公告)号：WO2002094379A1
公开(公告)日：2002-11-28
申请号：PCT/EP2002/005819
申请日：2002-05-27
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： HOFFMANN, Jens , FUHRMANN, Ulrike , LICHTNER, Rosemarie , SCHNEIDER, Martin , SIEMEISTER, Gerhard
IPC分类号： A61P35/00
CPC分类号： A61K31/567
摘要： The present invention relates to methods and uses for preventing and treating prostate diseases, in particular prostate cancer and benign prostate hyperplasia, in male mammals by antiprogestins, in particular antiprogestins, in particular antirogestin 11ß-(4- acetylphenyl)-17ß-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof. The invention further relates to pharmaceutical compositions comprising said antiprogestin.
摘要翻译：本发明涉及用于预防和治疗由抗孕激素，特别是抗孕激素，特别是抗孕激素11β-（4-乙酰基苯基）-17β-羟基-17的雄激素的前列腺疾病，特别是前列腺癌和良性前列腺增生的方法和用途 α-（1,1,2,2,2-五氟乙基） - 雌-4,9-二烯-3-酮或其药学上可接受的衍生物或类似物。本发明还涉及包含所述抗孕激素的药物组合物。

4. 发明申请

WO2003045972A1 17α-ALKYL-17β-OXY-ESTRATRIENE UND ZWISCHENPRODUKTE ZU DEREN HERSTELLUNG, VERWENDUNG DER 17α-ALKYL-17β-OXY-ESTRATRIENE ZUR HERSTELLUNG VON ARZNEIMITTELN SOWIE PHARMAZEUTISCHE PRÄPARATE 审中-公开
标题翻译： 17的α-烷基-β-17氧基 - 雌三烯和中间产品FOR THEIR，采用17的α-烷基-β-17氧基 - 雌三烯药物和药物制剂的生产
公开(公告)号：WO2003045972A1
公开(公告)日：2003-06-05
申请号：PCT/EP2002/013484
申请日：2002-11-27
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： BOHLMANN, Rolf , HEINRICH, Nikolaus , JAUTELAT, Rolf , KROLL, Jorg , PETROV, Orlin , REICHEL, Andreas , HOFFMANN, Jens , LICHTNER, Rosemarie
IPC分类号： C07J41/00
CPC分类号： C07J43/003 , C07J41/0072
摘要： Die Erfindung betrifft antiestrogen wirksame 17α-Alkyl-17β-oxy-estra-1,3,5(10)-triene mit der allgemeinen Formel I. Ausserdem betrifft die Erfindung auch 17-Oxo-estra-1,3,5(10)-triene sowie 17β-Hydroxy-estra-1,3,5(10)-triene als Zwischenprodukte bei der Herstellung der erfindungsgemässen Estratriene. Ferner betrifft die Erfindung die Verwendung der 17α-Alkyl-17β-oxy-estratriene zur Herstellung von Arzneimitteln sowie pharmazeutische Präparate, enthaltend mindestens ein 17α-Alkyl-17β-oxy-estratrien sowie mindestens einen pharmazeutisch verträglichen Träger.
摘要翻译：本发明涉及有效的抗雌激素17的α-烷基 - 17的β氧 - 雌-1,3,5（10）通式I的 - 三烯本发明还涉及到17-氧代 - 雌-1,3,5（ 10） - 三烯和17的β - 羟基 - 雌-1,3,5（10） - 三烯如在本发明的雌三烯的制备中间体。此外，本发明涉及使用17的α-烷基 - 17的β氧 - 雌三烯用于生产含有至少一种17的α-烷基 - 17的β氧 - 雌三烯和至少一种药学上可接受的载体的药物和药物制剂。

5. 发明申请

WO1998007740A1 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES, PROCESS FOR PREPARING THE SAME, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES AND THEIR USE FOR PREPARING MEDICAMENTS 审中-公开
标题翻译： 7ALPHA-（XI-氨基烷基） - 雌三烯，制造方法药物制剂THAT THIS 7ALPHA-（XI-氨基烷基） - 雌三烯容纳和它们在药物的生产
公开(公告)号：WO1998007740A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004517
申请日：1997-08-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , BOHLMANN, Rolf , BITTLER, Dieter , HEINDI, Josef , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KÜNZER, Hermann , SAUER, Gerhard , HEGELE-HARTUNG, Christa , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
IPC分类号： C07J53/00
CPC分类号： C07J53/008 , C07J41/0072 , C07J43/006 , C07J53/002
摘要： The present invention describes new substituted 7α-(κ-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 or 2; A is a hydrogen atom or a C1-5-alkyl group; B and D represent each a hydrogen atom, or A and B represent together an alkylene group -(CH2)p- where p = 2, 3, 4 or 5 and D is a hydrogen atom, or A and D form together an alkylene group -(CH2)q- where q = 2, 3 or 4 and B is a hydrogen atom; and E is a non-substituted ethyl radical or an ethyl radical fluorinated one to five times; or the terminal substituent -(CH2)3-E in the side chain is substituted by an optionally substituted aryl or heteroaryl radical bonded to the sulphur atom directly or by a mono-, di- or trimethylene group; R3 is a hydrogen atom, a hydrocarbon radical with up to 8 carbon atoms or a radical of partial formula R3'-C(O)-, where R3' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms or a phenyl radical; R11 is a hydrogen atom, a halogen atom or a nitrooxy group -O-NO¿2?, R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom or R?14 and R15α¿ are an additional bond or a methylene bridge, or R15β is a methyl group and R15α is a hydrogen atom, R?15α and R15β¿ represent each a methyl group, or R?15β and R16β¿ form together a methylene bridge, or R?16α or R16β¿ are a halogen atom or R?16α and R16β¿ form together a methylidene group, and the remaining substitutents R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom, R17' at the α- or β-position is a hydrogen atom, a C¿1-5? alkyl, C2-5 alkenyl or C2-5 alkinyl group or a trifluoromethyl group; and R?17'¿ is a hydrogen atom or a radical of partial formula R17'''-C(O)-, where R17''' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms, or when R17' is at the α-position, R17' forms together with R14 an ethano bridge, provided that when A and B do not stand together for -(CH¿2?)p- or A and D stand together for -(CH2)q-, at least one of the substituents R?11, R14, R15α, R15β, R16α and R16b¿ be not a hydrogen atom. Also disclosed are the physiologically tolerable addition salts of these compounds with organic and inorganic acids. These new compounds have a very strong anti-estrogenic activity. Some of them are pure anti-estrogenes, others are anti-estrogenes with a partial estrogenic effect. Because of their spectrum of activity, these new compounds are most suitable for preparing medicaments for tumor therapy and hormone substitution therapy.

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