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1.发明授权7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE ENTHALTEN SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效7ALPHA-（ε-己氨基烷基） - 雌三烯，PROCESS FOR PRODUCING药物制剂THAT THIS 7ALPHA-（ε-己氨基烷基） - 雌三烯容纳和它们在药物的生产
公开(公告)号：EP0920441B1
公开(公告)日：2003-01-29
申请号：EP97943814.0
申请日：1997-08-20
发明人： BOHLMANN, Rolf , BITTLER, Dieter , HEINDI, Josef , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KÜNZER, Hermann , SAUER, Gerhard , HEGELEHARTUNG, Christa , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
IPC分类号： C07J53/00 , A61K31/565 , C07J41/00 , C07J43/00 , A61K31/58
CPC分类号： C07J53/008 , C07J41/0072 , C07J43/006 , C07J53/002
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2.发明公开11BETA-LANGKETTIG-SUBSTITUIERTE ESTRATRIENE, VERFAHREN ZUR HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 11BETA-LANGKETTIG-SUBSTITUIERTEN ESTRATRIENE ENTHALTEN, SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 有权11β-长链取代的雌三烯，PROCESS FOR PRODUCING药物制剂THAT THIS11β-长链取代的雌三烯容纳和它们在药物的生产
公开(公告)号：EP1187846A2
公开(公告)日：2002-03-20
申请号：EP00947882.7
申请日：2000-06-26
发明人： BOHLMANN, Rolf , HEINRICH, Nikolaus , KROLL, Jorg , SAUER, Gerhard , FRITZEMEIER, Karl-Heinrich , HEGELE-HARTUNG, Christa , HOFFMANN, Jens , LICHTNER, Rosemarie , ZORN, Ludwig
CPC分类号： C07J1/00
摘要： The invention relates to novel 11β long-chain substituted estratrienes of general formula (I), wherein R11 is a long-chain residue with one nitrogen and optionally one sulfur atom, that can additionally be terminally functionalized with a perfluoroalkyl group or an optionally substituted aryl group. The inventive compounds are characterized by antiestrogenic or tissue-selective estrogenic properties and are useful in the production of medicaments.
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公开(公告)号：EP0839130A1
公开(公告)日：1998-05-06
申请号：EP96924891.0
申请日：1996-07-08
发明人： BOHLMANN, Rolf , HEINDL, Joseph , KÜNZER, Hermann , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
CPC分类号： C07C323/25 , C07C317/18 , C07C317/28 , C07C323/12 , C07C323/60 , C07D213/32 , C07D213/34
摘要： New triphenyl ethylenes have the general formula (I), in which n is an integer from 1 to 10, R' is a sulphur-containing organic rest, R'' is a hydrogen atom, an iodine atom or a hydroxyl group, E is a hydrogen atom, G is a hydrogen atom, or E and G form together a methylene bridge. These new compounds have strong anti-oestrogenic properties and are suitable for producing medicaments, for example for treating mammary carcinoma.
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4.发明公开$g(N)-FLUOROSULPHONIMIDES, METHOD OF PREPARING THEM AND THEIR USE AS FLUORINATION AGENTS 失效N-二fluorosulfonimides，生产方式及其作为氟化
公开(公告)号：EP0695290A1
公开(公告)日：1996-02-07
申请号：EP94915088.0
申请日：1994-04-20
发明人： BOHLMANN, Rolf
CPC分类号： C07D285/15 , C07B39/00 , C07C17/202 , C07C17/206 , C07C45/63 , C07C67/307 , C07C311/48 , C07C25/18 , C07C25/22 , C07C49/80 , C07C69/65
摘要： Described are Ξ-fluorosulphonimides of the general formula (I) (R1-SO2)2NF in which each R1 is a methyl group or the R1 groups together form a -(CH¿2?)n- group in which n=1, 2 or 3, in particular N-fluoromethansulphonimide, (CH3SO2)2NF, their preparation and their use in the electrophilic fluorination of activated C-H bonds in organic molecules.
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5.发明授权18-METHYL-19-NOR-17-PREGN-4-EN-21,17-CARBOLACTONE, SOWIE DIESE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权18-甲基-19-去甲-17-孕-4-烯21,17羧内酯，和药物制剂含有它们
公开(公告)号：EP1831240B1
公开(公告)日：2009-07-15
申请号：EP05850392.1
申请日：2005-12-30
发明人： BOHLMANN, Rolf , BITTLER, Dieter , KUENZER, Hermann , ESPERLING, Peter , MUHN, Hans-Peter , FRITZEMEIER, Karl-Heinrich , FUHRMANN, Ulrike , PRELLE, Katja , BORDEN (FRÜHER KURZ), Steffen
IPC分类号： C07J53/00 , A61K31/585 , A61P5/34
CPC分类号： C07J21/00 , C07J53/008
摘要： The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z = O, H 2 , =NOR or =NNHSO 2 R, where R = H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R 4 = H, halogen, methyl or trifluoromethyl, R 6 and/or R 7 can be a- or ß-positioned and independently = branched- or straight-chain 1-4 or 3-4 alkyl, or R 6 = H and R 7 = a- or ß-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R 6 and R 7 = H, or R 6 and R 7 together = a- or ß-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.
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6.发明公开VEGFR-2 UND VEGFR-3 INHIBITORISCHE ANTHRANYLAMIDPYRIDONE 审中-公开VEGFR-2 UND VEGFR-3抑制剂ANTHRANYLAMIDPYRIDONE
公开(公告)号：EP1633713A1
公开(公告)日：2006-03-15
申请号：EP04739742.7
申请日：2004-06-09
发明人： HUTH, Andreas , KRUEGER, Martin , ZORN, Ludwig , INCE, Stuart , BOHLMANN, Rolf , THIERAUCH, Karl-Heinz , MENRAD, Andreas , HABEREY, Martin , HESS-STUMPP, Holger
IPC分类号： C07D213/64 , A61K31/4412 , A61P17/06 , A61P19/02 , A61P35/00
CPC分类号： C07D213/64
摘要： The invention relates to selected anthranylamide pyridones that inhibit VEGFR-2 and VEGFR-3 and to their use as medicaments for treating diseases that are triggered by persistent angiogenesis.
摘要翻译： 本发明涉及选择性抑制VEGFR-2和VEGFR-3的蒽基酰胺吡啶酮及其作为治疗由持续性血管生成引发的疾病的药物的用途。
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7.发明公开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：EP1448591A1
公开(公告)日：2004-08-25
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 17α-alkyl-17β-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 17β-hydroxy-estra-1,3,5(10)-trienes as intermediates for producing the inventive estratrienes. The invention further relates to the use of 17α-alkyl-17β-oxy-estratrienes for the production of medicaments and pharmaceutical preparations containing at least one 17α-alkyl-17β-oxy-estratriene and at least one pharmaceutically acceptable carrier.
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8.发明授权11BETA-HALOGEN-7ALPHA-SUBSTITUIERTE-ESTRATRIENE, VERFAHREN ZUR HERSTELLUNG PHARMAZEUTISCHER PRÄPARATE, DIE DIESE 11BETA-HALOGEN-7ALPHA-SUBSTITUIERTE-ESTRATRIENE ENTHALTEN, SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 有权11β-卤素取代7alpha-雌三烯，PROCESS FOR PRODUCING药物制剂THAT THIS11β-卤素取代7alpha-雌三烯容纳和它们在药物的生产
公开(公告)号：EP1042355B1
公开(公告)日：2003-02-12
申请号：EP98966410.7
申请日：1998-12-23
发明人： BOHLMANN, Rolf , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KROLL, Jorg , KÜNZER, Hermann , SAUER, Gerhard , ZORN, Ludwig , FRITZEMEIER, Karl-Heinrich , LESSL, Monika , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
IPC分类号： C07J41/00 , A61K31/565 , C07J43/00 , C07J31/00 , A61K31/58
CPC分类号： C07J41/0094 , C07J31/006 , C07J41/0072 , C07J43/003
摘要： The invention relates to novel 11 beta -halogen-7 alpha -substituted estratrienes of formula (I), wherein R is a fluorine or chlorine atom and the other substituents have the meanings given in the description. The inventive compounds have anti-estrogen or tissue selective estrogenic characteristics and are suitable for producing medicaments.
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9.发明公开11$g(b)-ARYLSUBSTITUIERTE 14,17-ETHANO ESTRATRIENE, VERFAHREN ZUR HERSTELLUNG DIESER VERBINDUNGEN, SOWIE IHRE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效11 $克（b）中的芳基取代的14,17-乙醇雌三烯，PROCESS用于生产这些化合物，以及它们在药物的生产
公开(公告)号：EP0986574A1
公开(公告)日：2000-03-22
申请号：EP98937433.5
申请日：1998-06-02
发明人： BOHLMANN, Rolf , FRITZEMEIER, Karl-Heinrich , HEGELE-HARTUNG, Christa , KNAUTHE, Rudolf , PARZCYK, Karsten
IPC分类号： C07J41/00 , A61K31/565 , C07J53/00
CPC分类号： C07J41/0083 , C07J53/002
摘要： The invention relates to 11β-aryl-substituted 14,17-ethano-oestratriens of general formula (I), in which R1 is a hydrogen atom, a C¿1?-C12-alkanoyl-, a benzoyl-, a straight-chain or branched C1-C12-alkyl-, a C3-C7-cycloalkyl- or a C4-C8-alkyl cycloalkyl group, which can all optionally be substituted; R?2¿ is a hydrogen atom or an optionally substituted C¿1?-C12-alkanoyl group; R?3¿ stands for a group in which n = 4, 5, 6, or 7; m = 0, 1 or 2; R4 or R5 are, independently of each other, a hydrogen atom or a straight-chain or branched, optionally substituted C¿1?-C8-alkyl group, which can also be partially or completely fluorinated, or R?4 and R5¿ together mean a methylene to pentamethylene group -(CH¿2?)p-(p=1-5); and R?6¿ is the same as R4 or R5, or is an optionally substituted aryl or aryl alkyl radical, whereby said alkyl radical can have up to 6 carbon atoms, and the aryl radical, on its own or in the aryl alkyl radical, is a 5 or 6-link monocyclic ring or a condensed 8-10-link ring system, and the aryl radical can have one or more heteroatoms selected from oxygen, nitrogen, and sulphur. The new compounds are selective oestrogens whose effect is tissue-selective. In particular, the oestrogenic effect occurs on bone, in the cardiovascular system and in the central nervous system. However, it has little or no oestrogenic effect on the uterus and the liver. The compounds are suitable for producing medicaments which are used in many indications (for example, for hormone replacement therapy, prevention and treatment of osteoporosis).
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10.发明授权N-FLUORSULFONIMIDE, VERFAHREN ZU IHRER HERSTELLUNG SOWIE DEREN VERWENDUNG ALS FLUORIERUNGSMITTEL 失效N-二fluorosulfonimides，生产方式及其作为氟化
公开(公告)号：EP0695290B1
公开(公告)日：1997-11-05
申请号：EP94915088.2
申请日：1994-04-20
发明人： BOHLMANN, Rolf
IPC分类号： C07C311/48 , C07D285/00 , C07B39/00
CPC分类号： C07D285/15 , C07B39/00 , C07C17/202 , C07C17/206 , C07C45/63 , C07C67/307 , C07C311/48 , C07C25/18 , C07C25/22 , C07C49/80 , C07C69/65
摘要： Described are Ξ-fluorosulphonimides of the general formula (I) (R1-SO2)2NF in which each R1 is a methyl group or the R1 groups together form a -(CH¿2?)n- group in which n=1, 2 or 3, in particular N-fluoromethansulphonimide, (CH3SO2)2NF, their preparation and their use in the electrophilic fluorination of activated C-H bonds in organic molecules.
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