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1.发明授权公开(公告)号：US07935827B2
公开(公告)日：2011-05-03
申请号：US12338179
申请日：2008-12-18
申请人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
发明人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
IPC分类号： C07D215/14
CPC分类号： C12P17/14 , C07D215/12 , C07D217/02 , C07D235/06 , C07D263/56 , C07D277/62 , C07D277/64 , C12P17/10 , C12P17/12
摘要： The present invention relates to new optically active heteroaromatic β-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
摘要翻译： 本发明涉及可用于合成埃坡霉素衍生物的新的光学活性杂芳香族 - 羟基酯，用于生产这些中间体的某些化合物以及它们的生产方法。
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2.发明申请公开(公告)号：US20100248313A1
公开(公告)日：2010-09-30
申请号：US12338179
申请日：2008-12-18
申请人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
发明人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
IPC分类号： C12P17/14 , C12P17/00 , C12P17/12 , C07D217/02 , C07D215/48 , C07D277/64 , C07D263/56 , C07D235/06
CPC分类号： C12P17/14 , C07D215/12 , C07D217/02 , C07D235/06 , C07D263/56 , C07D277/62 , C07D277/64 , C12P17/10 , C12P17/12
摘要： The present invention relates to new optically active heteroaromatic β-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
摘要翻译： 本发明涉及可用于合成埃坡霉素衍生物的新的光学活性杂芳族和羟基酯，用于生产这些中间体的某些化合物，以及其制备方法。
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3.发明授权Optically active, heteroaromatic β-hydroxy esters and processes for their preparation from β-keto esters and processes for the preparation of these β-keto esters 失效光学活性的杂芳族β-羟基酯及其由β-酮酯制备的方法和制备这些β-酮酯的方法公开(公告)号：US07626035B2
公开(公告)日：2009-12-01
申请号：US11027671
申请日：2005-01-03
申请人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
发明人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa , Orlin Petrov
IPC分类号： C07D215/14 , C07D263/56 , C07D277/64
CPC分类号： C12P17/14 , C07D215/12 , C07D217/02 , C07D235/06 , C07D263/56 , C07D277/62 , C07D277/64 , C12P17/10 , C12P17/12
摘要： The present invention relates to new optically active heteroaromatic β-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
摘要翻译： 本发明涉及可用于合成埃坡霉素衍生物的新的光学活性杂芳族β-羟基酯，以及用于生产这些中间体的某些化合物，以及其生产方法。
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4.发明申请公开(公告)号：US20060148043A1
公开(公告)日：2006-07-06
申请号：US11027671
申请日：2005-01-03
申请人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa
发明人： Johannes Platzek , Ludwig Zorn , Bernd Buchmann , Werner Skuballa
IPC分类号： C12P17/00 , C07D277/62 , C07D215/12
CPC分类号： C12P17/14 , C07D215/12 , C07D217/02 , C07D235/06 , C07D263/56 , C07D277/62 , C07D277/64 , C12P17/10 , C12P17/12
摘要： The present invention relates to new optically active heteroaromatic β-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
摘要翻译： 本发明涉及可用于合成埃坡霉素衍生物的新的光学活性杂芳族β-羟基酯，用于生产这些中间体的某些化合物，以及它们的生产方法。
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5.发明授权Chiral heptyne derivatives for the preparation of epothilones and processes for their preparation 失效用于制备埃坡霉素的手性庚炔衍生物及其制备方法公开(公告)号：US07326798B2
公开(公告)日：2008-02-05
申请号：US11110959
申请日：2005-04-21
IPC分类号： C07D309/06 , C07C45/27
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.
摘要翻译： 本发明涉及用于生产可用于合成埃坡霉素或埃坡霉素衍生物的关键中间体，用于生产这些关键中间体的某些化合物和生产所述化合物的方法的新的合成方法。
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6.发明申请Novel chiral heptyne derivatives for the preparation of epothilones and processes for their preparation 失效用于制备埃坡霉素的新型手性庚炔衍生物及其制备方法公开(公告)号：US20060100442A1
公开(公告)日：2006-05-11
申请号：US11110959
申请日：2005-04-21
申请人： Johannes Platzek , Orlin Petrov , Marc Willuhn , Klaus Graske , Werner Skuballa
发明人： Johannes Platzek , Orlin Petrov , Marc Willuhn , Klaus Graske , Werner Skuballa
IPC分类号： A61K31/427 , C07D417/02 , C07D315/00
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.
摘要翻译： 本发明涉及用于生产可用于合成埃坡霉素或埃坡霉素衍生物的关键中间体，用于生产这些关键中间体的某些化合物和生产所述化合物的方法的新的合成方法。
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7.发明申请NOVEL CHIRAL HEPTYNE DERIVATIVES FOR THE PREPARATION OF EPOTHILONES AND PROCESSES FOR THEIR PREPARATION 审中-公开用于制备EPOTHILON的新型CHIRAL HEPTYNE衍生物及其制备方法公开(公告)号：US20080108838A1
公开(公告)日：2008-05-08
申请号：US11954348
申请日：2007-12-12
申请人： Johannes Platzek , Orlin Petrov , Marc Willuhn , Klaus Graske , Werner Skuballa
发明人： Johannes Platzek , Orlin Petrov , Marc Willuhn , Klaus Graske , Werner Skuballa
IPC分类号： C07D313/00
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.
摘要翻译： 本发明涉及用于生产可用于合成埃坡霉素或埃坡霉素衍生物的关键中间体，用于生产这些关键中间体的某些化合物和生产所述化合物的方法的新的合成方法。
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8.发明授权5-substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents 失效5-取代的喹啉和异喹啉衍生物，其制备方法及其作为抗炎剂的用途公开(公告)号：US07417056B2
公开(公告)日：2008-08-26
申请号：US11272009
申请日：2005-11-14
申请人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
发明人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
IPC分类号： C07D405/02 , A61K31/47
CPC分类号： C07D405/12
摘要： Compounds of general formula (IIa) or (IIb) and their use as pharmaceutical agents.
摘要翻译： 通式（IIa）或（IIb）的化合物及其作为药剂的用途。
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9.发明申请5-Substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents 失效5-取代的喹啉和异喹啉衍生物，其制备方法及其作为抗炎剂的用途公开(公告)号：US20060116396A1
公开(公告)日：2006-06-01
申请号：US11272009
申请日：2005-11-14
申请人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
发明人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
IPC分类号： A61K31/4709 , C07D405/02
CPC分类号： C07D405/12
摘要： Compounds of general formula (IIa) or (IIb) and their use as pharmaceutical agents.
摘要翻译： 通式（IIa）或（IIb）的化合物及其作为药剂的用途。
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公开(公告)号：US07700621B2
公开(公告)日：2010-04-20
申请号：US11214988
申请日：2005-08-31
申请人： Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
发明人： Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
IPC分类号： A01N43/42 , A01N43/78 , C07D417/00
CPC分类号： C07D493/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14
摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
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