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公开(公告)号：US20070197614A1
公开(公告)日：2007-08-23
申请号：US11676721
申请日：2007-02-20
申请人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jugen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
发明人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jugen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
IPC分类号： A61K31/421 , C12P7/02 , C07D263/30
CPC分类号： C07D413/12 , C07D263/62 , C07D309/12 , C12P17/14 , Y02P20/55
摘要： The invention relates generally to a process for preparing diarylcycloalkyl derivatives of the formula (I). wherein the respective R-group substituents are defined herein. These compounds of formula (I) are activators for peroxisome proliferator-activated receptors (PPAR activators) which are useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The present invention is a novel process for preparing PPAR activators of the formula (I) which do not have the disadvantages of the processes known in the prior art. In particular, a process is provided with which the PPAR activators of formula (I) can be prepared in a suitable enantiomeric excess, i.e. high enantioselectivity, without the need for subsequent chiral chromatography.
摘要翻译： 本发明一般涉及式（I）的二芳基环烷基衍生物的制备方法。 其中相应的R基取代基在本文中定义。 这些式（I）化合物是过氧化物酶体增殖物激活受体（PPAR活化剂）的活化剂，其可用于治疗多种中枢神经系统的疾病和病症如帕金森病，帕金森病，精神障碍和 喜欢。 本发明是制备式（I）的PPAR活化剂的新方法，其不具有现有技术中已知方法的缺点。 特别地，提供了一种方法，其中式（I）的PPAR活化剂可以以合适的对映异构体过量即高对映选择性制备，而不需要随后的手性色谱法。
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2.发明申请NOVEL INTERMEDIATE COMPOUNDS USEFUL IN THE PRODUCTION OF DIARYLCYCLOALKYL DERIVATIVES 审中-公开新的中间体化合物可用于生产二芳基胆碱衍生物公开(公告)号：US20080051583A1
公开(公告)日：2008-02-28
申请号：US11930244
申请日：2007-10-31
申请人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jugen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
发明人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jugen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
IPC分类号： C07D263/34 , C07D263/06
CPC分类号： C07D413/12 , C07D263/62 , C07D309/12 , C12P17/14 , Y02P20/55
摘要： The invention relates generally to intermediate compounds derived during the process for preparing diarylcycloalkyl derivatives which are activators for peroxisome proliferator-activated receptors (PPAR activators) and are therefore useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The intermediate compounds of the present invention are defined structurally by the formulae (Ia): and formula (II): wherein the respective substituent groups are defined herein.
摘要翻译： 本发明一般涉及在制备二芳基环烷基衍生物的方法中衍生的中间体化合物，二芳基环烷基衍生物是用于过氧化物酶体增殖物激活受体（PPAR活化剂）的活化剂，因此可用于治疗性治疗许多中枢神经系统的疾病和病症，例如 多发性硬化，帕金森病，精神障碍等。 本发明的中间体化合物在结构上由式（Ia）和式（II）定义：其中各取代基在本文中定义。
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公开(公告)号：US07803950B2
公开(公告)日：2010-09-28
申请号：US11676721
申请日：2007-02-20
申请人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jügen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
发明人： Christophe Salagnad , Frank Zocher , Andreas Burgard , Bernd Junker , Rolf Hoerlein , Thomas Stuedemann , Claus-Jügen Maier , Jochen Hachtel , Wolfgang Holla , Christoph Tappertzhofen , Berndt Kulitzscher , Stephane Mutti
IPC分类号： C07D263/32 , C12P7/62
CPC分类号： C07D413/12 , C07D263/62 , C07D309/12 , C12P17/14 , Y02P20/55
摘要： The invention relates generally to a process for preparing diarylcycloalkyl derivatives of the formula (I). wherein the respective R-group substituents are defined herein. These compounds of formula (I) are activators for peroxisome proliferator-activated receptors (PPAR activators) which are useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The present invention is a novel process for preparing PPAR activators of the formula (I) which do not have the disadvantages of the processes known in the prior art. In particular, a process is provided with which the PPAR activators of formula (I) can be prepared in a suitable enantiomeric excess, i.e. high enantioselectivity, without the need for subsequent chiral chromatography.
摘要翻译： 本发明一般涉及式（I）的二芳基环烷基衍生物的制备方法。 其中相应的R基取代基在本文中定义。 这些式（I）化合物是过氧化物酶体增殖物激活受体（PPAR活化剂）的活化剂，其可用于治疗多种中枢神经系统的疾病和病症如帕金森病，帕金森病，精神障碍和 喜欢。 本发明是制备式（I）的PPAR活化剂的新方法，其不具有现有技术中已知方法的缺点。 特别地，提供了一种方法，其中式（I）的PPAR活化剂可以以合适的对映异构体过量即高对映选择性制备，而不需要随后的手性色谱法。
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公开(公告)号：US07488818B2
公开(公告)日：2009-02-10
申请号：US11561626
申请日：2006-11-20
申请人： Andreas Lindenschmidt , David William Will , Gerhard Jaehne , Theodor Andreas Wollmann , Wendelin Frick , Bernd Junker , David Rigal , Guenter Billen , Heiner Jendralla
发明人： Andreas Lindenschmidt , David William Will , Gerhard Jaehne , Theodor Andreas Wollmann , Wendelin Frick , Bernd Junker , David Rigal , Guenter Billen , Heiner Jendralla
IPC分类号： C07D205/08 , C07F9/6503 , C07F9/6506 , C07F9/6541 , C07F9/653 , C07F9/572 , C07F9/54
CPC分类号： C07D205/08 , A61K31/33
摘要： The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from β-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.
摘要翻译： 本发明涉及可用于治疗高脂血症，动脉硬化，高胆固醇血症和其它相关代谢紊乱的新化合物的制备。 更具体地说，本发明是一种从β-取代氨基酰胺制备1,4-二苯基氮杂环丁酮衍生物的新方法，其在甲硅烷基化试剂和至少一种环化催化剂存在下被保护，其结构式由 通式：其中各种R基团在本文中定义。
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公开(公告)号：US4994311A
公开(公告)日：1991-02-19
申请号：US380869
申请日：1989-07-17
申请人： Bernd Junker
发明人： Bernd Junker
CPC分类号： E06B7/2314 , B60J10/17 , Y10T428/24198 , Y10T428/2902
摘要： A window channel receives a slidable pane of window glass within a gap. The glass slides in contact with areas which are coated with low friction material which is applied by sintering. For example, the sintered material may be powdery polyurethane, polypropylene or polyamide. The sintered powders may be transparent and may be applied after the areas have been coated with a solvent or primer. Using similar materials, but with colored powders, the exposed surfaces of door and other seals may be provided with a colored coating.
摘要翻译： 窗口通道在间隙内接收可滑动的窗玻璃。 玻璃与通过烧结施加的低摩擦材料的涂覆区域接触。 例如，烧结材料可以是粉末状聚氨酯，聚丙烯或聚酰胺。 烧结的粉末可以是透明的，并且可以在用溶剂或底漆涂覆区域之后施用。 使用类似的材料，但是使用有色粉末，门和其他密封件的暴露表面可以设置有彩色涂层。
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公开(公告)号：US20070149501A1
公开(公告)日：2007-06-28
申请号：US11557310
申请日：2006-11-07
IPC分类号： A61K31/397 , C07D205/02
CPC分类号： C07D205/08 , Y02P20/55
摘要： The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, R1 and/or R2 as defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain □-amino carboxamides or □-amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby.
摘要翻译： 本发明是制备式（I）的二苯并氮杂环丁酮衍生物或其形式的方法，其包含如本文所定义的取代基X，R 1和/或R 2 2 。 更具体地，本发明包括通过环化某些□ - 氨基甲酰胺或□ - 氨基羧酸酯来制备这些化合物的方法。 这些二苯基氮杂环丁酮化合物可用于治疗高血清胆固醇水平和维持由此实现的降低的胆固醇水平。
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公开(公告)号：US07563888B2
公开(公告)日：2009-07-21
申请号：US11557310
申请日：2006-11-07
申请人： Joachim-Heiner Jendralla , Guenter Billen , Wendelin Frick , Bernd Junker , Theodor Andreas Wollman
发明人： Joachim-Heiner Jendralla , Guenter Billen , Wendelin Frick , Bernd Junker , Theodor Andreas Wollman
IPC分类号： C07D205/08 , C07D307/20 , C07F7/18 , C07C237/20 , C07C235/38
CPC分类号： C07D205/08 , Y02P20/55
摘要： The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, R1 and/or R2 as defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain β-amino carboxamides or β-amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby.
摘要翻译： 本发明是制备式（I）的二苯并氮杂环丁酮衍生物或其形式的方法，其包含如本文所定义的取代基X，R 1和/或R 2。 更具体地，本发明包括通过环化某些β-氨基甲酰胺或β-氨基羧酸酯来制备这些化合物的方法。 这些二苯基氮杂环丁酮化合物可用于治疗高血清胆固醇水平和维持由此实现的降低的胆固醇水平。
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公开(公告)号：US20090082589A1
公开(公告)日：2009-03-26
申请号：US12271236
申请日：2008-11-14
申请人： Bernd Junker , Javier Manero
发明人： Bernd Junker , Javier Manero
IPC分类号： C07C229/34 , C07C69/612
CPC分类号： C07C233/18 , C07B2200/07
摘要： Provided are compounds of formula A and formula I:A compound of formula A: wherein n is an integer from 6 to 17 and a compound of formula I:
摘要翻译： 提供式A和式I的化合物：式A的化合物：其中n是6至17的整数，并且式I的化合物：
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9.发明申请Processes for Making and Using Benzyl Pentahydroxyhexylcarbamoylundecanoate 审中-公开苄基五羟基己基氨基甲酰十一酸酯的制备和使用方法公开(公告)号：US20080319218A1
公开(公告)日：2008-12-25
申请号：US11767284
申请日：2007-06-22
申请人： Andreas Haubrich , Bernd Junker , Javier Manero , Theo Wollmann
发明人： Andreas Haubrich , Bernd Junker , Javier Manero , Theo Wollmann
IPC分类号： C07C69/96 , C07C227/00 , C07C227/04 , C07C69/66
CPC分类号： C07C231/02 , C07C67/30 , C07C68/02 , C07C69/34 , C07C69/96 , C07C231/12 , C07C233/18
摘要： Provided are compounds and a process for preparing benzyl pentahydroxyhexylcarbamoylundecanoate (I) and uses thereof.
摘要翻译： 提供化合物和制备五羟基己基氨基甲酰基十一酸苄酯（I）的方法及其用途。
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公开(公告)号：US07678935B2
公开(公告)日：2010-03-16
申请号：US12271236
申请日：2008-11-14
申请人： Bernd Junker , Javier Manero
发明人： Bernd Junker , Javier Manero
CPC分类号： C07C233/18 , C07B2200/07
摘要： Provided are compounds of formula A and formula I:A compound of formula A: wherein n is an integer from 6 to 17 and a compound of formula I:
摘要翻译： 提供式A和式I的化合物：式A的化合物：其中n是6至17的整数，并且式I的化合物：
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