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公开(公告)号：EP1912970A2
公开(公告)日：2008-04-23
申请号：EP06776768.1
申请日：2006-08-08
发明人： WORTMANN, Lars , CLEVE, Arwed , MUHN, Hans-Peter , LANGER, Gernot , SCHREY, Anna , KÜHNE, Ronald , MENZENBACH, Bernd , KOPPITZ, Marcus , KOSEMUND, Dirk
IPC分类号： C07D401/12 , C07D405/14 , C07D209/14 , C07D405/12 , C07D409/12 , C07D417/14 , C07D403/12 , C07D413/12 , C07D215/52 , C07D405/04 , C07D307/79 , C07D333/32 , C07D215/50 , C07D417/04 , C07D317/60
CPC分类号： C07D413/12 , C07C65/24 , C07D209/14 , C07D213/79 , C07D215/50 , C07D215/52 , C07D235/06 , C07D239/28 , C07D239/74 , C07D277/56 , C07D307/79 , C07D317/60 , C07D333/32 , C07D333/38 , C07D333/70 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/14
摘要： The present patent application relates to acyltryptophanols of the general formula I, in which Q, X, Y, W, R1, R2, R3, R4, R5, R8 have the meanings stated in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本专利申请涉及通式I的酰基色氨酸，其中Q，X，Y，W，R 1，R 2，R 3，R 4，R 5，R 8具有说明书中所述的含义。 本发明化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：EP2081951B1
公开(公告)日：2010-04-21
申请号：EP07819866.0
申请日：2007-11-14
发明人： FUHRMANN, Ulrike , SCHMIDT, Anja , CLEVE, Arwed , PETROV, Orlin , GARKE, Gunnar , PRUEHS, Stefan , BRUDNY-KLOEPPEL, Margarete , ROTTMANN, Antje , HASSELMANN, Rainer , SCHULTZE-MOSGAU, Marcus , MOELLER, Carsten
IPC分类号： C07J1/00 , C07J21/00 , C07J51/00 , A61K31/567 , A61P5/36
CPC分类号： C07J1/0081 , C07J21/006 , C07J51/00
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3.发明公开SUBSTITUIERTE 2-ANILINOPYRIMIDINE ALS ZELLZYKLUS -KINASE ODER REZEPTORTYROSIN-KINASE INHIBITOREN, DEREN HERSTELLUNG UND VERWENDUNG ALS ARZNEIMITTEL 审中-公开取代的2-苯胺基嘧啶细胞周期激酶或受体酪氨酸激酶抑制剂，生产与应用，药物
公开(公告)号：EP1794134A1
公开(公告)日：2007-06-13
申请号：EP05793571.0
申请日：2005-09-27
发明人： CLEVE, Arwed , LÜCKING, Ulrich , WEST, Christopher , BRIEM, Hans , SIEMEISTER, Gerhard , KRÜGER, Martin , JAUTELAT, Rolf , LIENAU, Philip
IPC分类号： C07D239/48 , C07D239/46 , A61K31/505 , A61P35/00
CPC分类号： C07D239/47 , C07D239/48
摘要： The invention relates to pyrimidine derivatives of general formula (I), in which R1, R2, R3, R4, A and D are defined as cited in the description, said derivatives being used as inhibitors of cyclin-dependent kinases and VEGF receptor kinases. The invention also relates to the production of said substances and to their use as a medicament for treating various diseases. The inventive compounds have a reduced affinity to carbonic anhydrase 2.
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公开(公告)号：EP2081951A1
公开(公告)日：2009-07-29
申请号：EP07819866.0
申请日：2007-11-14
发明人： FUHRMANN, Ulrike , SCHMIDT, Anja , CLEVE, Arwed , PETROV, Orlin , GARKE, Gunnar , PRUEHS, Stefan , BRUDNY-KLOEPPEL, Margarete , ROTTMANN, Antje , HASSELMANN, Rainer , SCHULTZE-MOSGAU, Marcus , MOELLER, Carsten
IPC分类号： C07J1/00 , C07J21/00 , C07J51/00 , A61K31/567 , A61P5/36
CPC分类号： C07J1/0081 , C07J21/006 , C07J51/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.
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公开(公告)号：EP1622894B1
公开(公告)日：2009-01-14
申请号：EP04728552.3
申请日：2004-04-21
发明人： CLEVE, Arwed , SCHULZE, Volker , ZOPF, Dieter , HOFFMANN, Jens , REICHEL, Andreas , PARCZYK, Karsten
IPC分类号： C07D403/06 , A61P35/00 , A61K31/4164
CPC分类号： C07D233/86 , A61K31/4178 , C07D403/06
摘要： The invention relates to substituted antiadrogenic pyrrolidines N-[φ-[3-[4-cyan-3-(trifluoromethyl)-phenyl]-5.5-dimethyl-4-oxo2-thioxoimidazoline-1-yle]alkyl] of formula (I) having a salient antiproliferative effect profile. Said invention also relates to a method for producing compounds of the formula (I), pharmaceutical preparations and to the use thereof for producing drugs.
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6.发明公开KRISTALLINE FORMEN VON 11BETA-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAFLUOR-17ALPHA- HYDROXY-19-NOR-17 -PREGNA-4,9-DIEN-3-ON 审中-公开11BETA-（4-乙酰基苯基）-20,20,21,21,21五氟17ALPHA-羟基-19-去甲-17-孕-4,9-二烯-3-酮结晶形式
公开(公告)号：EP2024383A2
公开(公告)日：2009-02-18
申请号：EP07725692.3
申请日：2007-05-31
发明人： BECKMANN, Wolfgang , WINTER, Gabriele , KRÄMER, Edda , GINKO, Thomas , AMOULONG, Evelin , CLEVE, Arwed
IPC分类号： C07J1/00 , A61P5/36 , A61K31/567
CPC分类号： C07J1/0081
摘要： The present invention relates to crystalline forms of 11 ß-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. In particular, the invention relates to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example, methanol and ethanol solvates of 11 ß-(4-acetylphenyl)- 20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one, as precursors for the preparation of these two polymorphs I and II. Processes are described for the preparation of polymorph I by means of displacement crystallization or by means of extraction. The choice of the last solvent, before the ansolvate formation can take place, on the basis of the differences in the purification ratios of the individual solvates of 11 ß-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one is described. Polymorph I, according to the invention, is particularly suitable for the preparation of drugs.
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