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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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2.发明授权GESCHÜTZTE 3,5-DIHYDROXY-2,2-DIMETHYL-VALERONITRILE FÜR DIE SYNTHESE VON EPOTHILONEN- UND DERIVATEN UND VERFAHREN ZUR HERSTELLUNG UND DIE VERWENDUNG 有权受保护的3.5二羟基-2,2-二甲基戊腈的EPOTHILONEN-及其衍生物和方法的生产和使用合成
公开(公告)号：EP1412323B1
公开(公告)日：2009-09-30
申请号：EP02794553.4
申请日：2002-08-05
IPC分类号： C07C255/13 , C07C255/12 , C07C255/20 , C07C253/30 , C07D319/06
CPC分类号： C12P13/004 , C07C253/30 , C07C255/12 , C07C255/13 , C07C255/20 , C07D319/06 , C07F7/1852 , C12P41/004 , Y02P20/55
摘要： The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
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3.发明公开5-SUBSTITUIERTE CHINOLIN- UND ISOCHINOLIN-DERIVATE; EIN VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ENTZÜNDUNGSHEMMER 有权5-取代的喹啉和异喹啉衍生物; 其制备方法及其用作抗抑制剂
公开(公告)号：EP1844039A1
公开(公告)日：2007-10-17
申请号：EP05808294.2
申请日：2005-11-11
发明人： JAROCH, Stefan , REHWINKEL, Hartmut , SCHÄCKE, Heike , SCHMEES, Norbert , SKUBALLA, Werner , SCHNEIDER, Matthias , HÜBNER, Jan , PETROV, Orlin , DINTER, Christian
IPC分类号： C07D405/12 , C07D307/79 , C07D307/83 , C07C69/68 , A61K31/47 , A61P29/00
CPC分类号： C07D307/79 , C07C69/732 , C07C69/734 , C07D307/83 , C07D405/12
摘要： The invention relates to compounds of general formulas (IIa) or (IIb) and to their use as medicaments.
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4.发明授权CHIRAL HEPTYNE DERIVATIVES FOR THE PREPARATION OF EPOTHILONES AND PROCESSES FOR THEIR PREPARATION 有权用于制备硬脂酸的手性庚环衍生物及其制备方法
公开(公告)号：EP1758875B1
公开(公告)日：2007-10-03
申请号：EP05740374.3
申请日：2005-04-21
发明人： PLATZEK, Johannes , PETROV, Orlin , WILLUHN, Marc, c/o Zimmer , GRASKE, Klaus-Dieter , SKUBALLA, Werner
IPC分类号： C07D309/12
CPC分类号： C07D309/12 , C07D313/00 , C07D409/12 , C07D493/04 , Y02P20/55
摘要： The invention relates to a new synthetic process for the production of key intermediates useful in the synthesis of epothilones or epothilone derivatives, to certain compounds used to produce these key intermediates and to a process to produce said compounds. The intermediates used are represented by formulae II and III, wherein R is selected from H, alkyl and substituded alkyl and X1 is an oxygen protecting group.
摘要翻译： 本发明涉及用于生产用于合成埃博霉素或埃坡霉素衍生物的关键中间体的新合成方法，涉及用于生产这些关键中间体的某些化合物以及生产所述化合物的方法。 所用的中间体由式II和III表示，其中R选自H，烷基和取代的烷基，X1是氧保护基。
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5.发明公开11.BETA.-FLUORO-3-ACETOXYESTRA-3,5-DIEN-17-ON UND VERFAHREN ZU SEINER HERSTELLUNG 有权11.BETA.Fluoro-3-ACETOXYESTRA-3,5-DIEN-17-ON UND VERFAHREN ZU SEINER HERSTELLUNG
公开(公告)号：EP2215104A1
公开(公告)日：2010-08-11
申请号：EP08843298.4
申请日：2008-10-18
IPC分类号： C07J1/00
CPC分类号： C07J1/0059
摘要： The present invention relates to 11β-fluoro-3-acetoxyestra-3,5-diene-17-on as suitable intermediate preparation for the production of 11-fluoro-sbustituted steroids and to the method for the production thereof. For this purpose, 11α-hydroxyestr-4-en-3,17-dion is reacted in an organic non-protic solvent with 1 to 3 equivalents of n-nonafluorobutanesulfonyl fluoride and 3 to 5 equivalents of diazabicycloundecene (DBU) at -40 to -20°C and, after an aqueous processing step, 5 to 10 equivalents of acetic acid anhydride and 0.01 to 1 equivalent of a strong acid are added. The desired product precipitates immediately from the reaction solution and is obtained in a very high purity by filtration. The method is characterized by a very high yield, avoidance of a chromatographic purification of the product, a lower amount of waste, and considerably increased process throughput. The method according to the invention is thus particularly suitable for the production of 11β-fluoro-3-acetoxyestra-3,5-diene-17-on on a large technical scale.
摘要翻译： 本发明涉及11β-氟-3-乙酰氧基雌甾-3,5-二烯-17-酮作为合适的用于生产11-氟 - 取代的类固醇的中间体制备物及其生产方法。 为此，将11α-羟基雌-4-烯-3,17-二酮在有机非质子溶剂中与1-至3当量的正九氟丁烷磺酰氟和3-5当量的二氮杂双环十一碳烯（DBU）在-40至 -20℃，在水处理步骤后，加入5至10当量的乙酸酐和0.01至1当量的强酸。 所需产物立即从反应溶液中沉淀出来并通过过滤以非常高的纯度获得。 该方法的特征在于产率非常高，避免了产物的色谱纯化，较少量的废物和显着增加的工艺产量。 因此，根据本发明的方法特别适用于大规模技术生产11β-氟-3-乙酰氧基雌甾-3,5-二烯-17-酮。
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6.发明授权LITHIUM-KOMPLEXE VON N-(1-HYDROXYMETHYL-2,3-DIHYDROXYPROPYL)-1,4,7-TRISCARBOXYMETHYL-1,4,7,10-TETRAAZACYCLODODECAN, DEREN HERSTELLUNG UND VERWENDUNG 有权N-（1-羟基甲基-2,3-二羟基丙基）-1,4,7- triscarboxymethyl-1,4,7,10-四，其生产和使用的锂复合
公开(公告)号：EP1343770B1
公开(公告)日：2009-05-06
申请号：EP01991788.9
申请日：2001-12-05
IPC分类号： C07D257/00
CPC分类号： C07D257/02
摘要： The invention relates to crystalline lithium complexes of N-(1-hydroxymethyl-2,3-dihydroxypropyl)-1,4,7-triscarboxymethyl-1,4,7,10 tetraazacyclododecane of formula (I), wherein: all of the three X's represent n lithium ions and m hydrogen atoms, whereby n and m each represent numbers from 0 to 3, preferably from 0.8 to 2.2, and the sum of n and m equals 3, and; Y represents chloride and bromide. The invention relates to the preparation of the inventive complexes and to production of the salt-free gadolinium complex of N-(1-hydroxymethyl-2,3-dihydroxypropyl)-1,4,7-triscarboxymethyl-1,4,7,10 tetraazacyclododecane from the same without involving the use of ion exchangers.
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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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8.发明授权5-SUBSTITUIERTE CHINOLIN- UND ISOCHINOLIN-DERIVATE; EIN VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ENTZÜNDUNGSHEMMER 有权5-取代的喹啉和异喹啉衍生物; 其制备方法及其用作抗抑制剂
公开(公告)号：EP1844039B1
公开(公告)日：2009-07-15
申请号：EP05808294.2
申请日：2005-11-11
发明人： JAROCH, Stefan , REHWINKEL, Hartmut , SCHÄCKE, Heike , SCHMEES, Norbert , SKUBALLA, Werner , SCHNEIDER, Matthias , HÜBNER, Jan , PETROV, Orlin , DINTER, Christian
IPC分类号： C07D405/12 , C07D307/79 , C07D307/83 , C07C69/68 , A61K31/47 , A61P29/00
CPC分类号： C07D307/79 , C07C69/732 , C07C69/734 , C07D307/83 , C07D405/12
摘要： The invention relates to compounds of general formulas (IIa) or (IIb) and to their use as medicaments.
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9.发明公开OPTICALLY ACTIVE, HETEROAROMATIC BETA-HYDROXY ESTERS, PROCESSES FOR THEIR PREPARATION FROM BETA-KETO ESTERS AND PROCESSES FOR THE PREPARATION OF THESE BETA-KETO ESTERS 审中-公开旋光，杂β-羟基酯，METHOD FORβ-酮酯的呈现，AND METHOD FOR DISPLAYING THISβ-酮酯
公开(公告)号：EP2113031A1
公开(公告)日：2009-11-04
申请号：EP04804342.6
申请日：2004-12-21
发明人： KLAR, Ulrich , PLATZEK, Johannes , ZORN, Ludwig , BUCHMANN, Bernd , SKUBALLA, Werner , PETROV, Orlin
IPC分类号： C12P41/00 , C07D215/14 , C07D217/16 , C07D235/06 , C07D263/56 , C07D277/64 , C07D277/62
CPC分类号： C07D263/56 , C07D215/14 , C07D217/16 , C07D235/06 , C07D277/62 , C07D277/64 , C12P17/12 , C12P17/14
摘要： The present invention relates to optically active heteroaromatic β -hydroxy esters of formula (I) useful in the synthesis of epothilone derivatives, to beta-keto esters of formula (IV) used to produce these intermediates by means of an asymmetric hydrogenation with a chiral metal catalyst or microbiological or enzymatic reduction, as well as to processes for their production (I), wherein: A is a bicyclic heteroaromatic residue of formula (A), wherein “heteroaromatic” stands for a 5-or 6-membered heteroaromatic ring having up to 2 heteroatoms selected from oxygen, nitrogen or sulphur, which is optionally substituted with one or two substituents selected from alkyl, optionally protected hydroxyalkyl, halo-alkyl, halogen or CN, and R is a straight-chain or branched, optionally saturated alkyl chain, which optionally contains 1-3 oxygen atoms; phenyl: cyclohexyl; or benzyl residue (IV).
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10.发明授权17ALPHA-ALKYL-17BETA-OXY-ESTRATRIENE UND ZWISCHENPRODUKTE ZU DEREN HERSTELLUNG, VERWENDUNG DER 17ALPHA-ALKYL-17BETA-OXY-ESTRATRIENE ZUR HERSTELLUNG VON ARZNEIMITTELN SOWIE PHARMAZEUTISCHE PRÄPARATE 有权17α-乙烯烷基17β-OXY-三烯和生产中间产品，17α-乙烯烷基17β-OXY-三烯的药物和药物制剂的生产中使用
公开(公告)号：EP1448591B1
公开(公告)日：2008-05-21
申请号：EP02795080.7
申请日：2002-11-27
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 , C07J43/00 , A61K31/567 , A61P5/32
CPC分类号： C07J43/003 , C07J41/0072
摘要： The invention relates to 17 alpha -alkyl-17 beta -oxy-estra-1,3,5(10)-trienes having an anti-oestrogen action, of general formula (I). The invention also relates to 17-oxo-estra-1,3,5(10)-trienes and 17 beta -hydroxy-estra-1,3,5(10)-trienes as intermediates for producing the inventive estratrienes. The invention further relates to the use of 17 alpha -alkyl-17 beta -oxy-estratrienes for the production of medicaments and pharmaceutical preparations containing at least one 17 alpha -alkyl-17 beta -oxy-estratriene and at least one pharmaceutically acceptable carrier.
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