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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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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：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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4.发明授权Method for the production of oxazoles by condensing aromatic aldehydes with α-ketoximes to N-oxides and then reacting the same with activated acid derivatives 有权通过将芳香族醛与α-酮肟缩合成N-氧化物然后使其与活性酸衍生物反应生产恶唑的方法公开(公告)号：US07825144B2
公开(公告)日：2010-11-02
申请号：US12509853
申请日：2009-07-27
申请人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
发明人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
IPC分类号： A61K31/421 , C07D263/30
CPC分类号： C07D263/32
摘要： The invention is related to a process for preparing compounds of the formula IV by means of conversion of aromatic aldehydes of the formula I using α-ketoximes of the formula II via N-oxides of the formula III to halomethyloxazoles of the formula IV, wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, o, n1 and n2 are as defined herein.
摘要翻译： 本发明涉及一种制备式Ⅳ化合物的方法，该方法是通过使式Ⅶ的α-酮肟通过式III的N-氧化物转化为式Ⅳ的卤代甲氧基，将式Ⅰ的芳族醛转化成式Ⅳ的卤代甲氧基唑，其中R 1 ，R2，R3，R4，R5，R6，R7，R8，X1，X2，X3，o，n1和n2如本文所定义。
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5.发明授权Method for the preparation of oxazoles by condensing aromatic aldehydes with α-ketoximes to form n-oxides and reacting same with activated acid derivatives 有权通过将芳族醛与α-酮肟缩合形成N-氧化物并与活化的酸衍生物反应制备恶唑的方法公开(公告)号：US07544809B2
公开(公告)日：2009-06-09
申请号：US11754477
申请日：2007-05-29
申请人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
发明人： Wolfgang Holla , Rolf-Ludwig Hoerlein , Berndt Kulitzscher , Wolfgang Laux , Thomas Stuedemann , Christoph Tappertzhofen , Robert J. H. Scheffer
IPC分类号： C07D263/32
CPC分类号： C07D263/32
摘要： The present invention is comprised of improved methods in the preparation of oxazoles which results in higher yields with less impurities and contaminants. Oxazoles constitute valuable intermediates in the synthesis of pharmaceutically active substances such as, for example peroxisome proliferator activated receptor (PPAR) agonists which are pharmaceutical actives which can have a positive influence on both lipid and glucose metabolism.
摘要翻译： 本发明包括改进的制备恶唑的方法，其导致较高的产率，较少的杂质和污染物。 恶唑在合成药物活性物质（例如过氧化物酶体增殖物激活受体（PPAR）激动剂）中是组成有价值的中间体，其是可以对脂质和葡萄糖代谢具有积极影响的药物活性物质。
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6.发明申请METHOD FOR THE PREPARATION OF ENANTIOMER FORMS OF CIS-CONFIGURED 3-HYDROXYCYCLOHEXANE CARBOXYLIC ACID DERIVATIVES USING HYDROLASES 审中-公开使用水解制备CIS配置的3-羟基环己烷羧酸衍生物的成膜剂形式的方法公开(公告)号：US20070197788A1
公开(公告)日：2007-08-23
申请号：US11669545
申请日：2007-01-31
IPC分类号： C07F7/02 , C07D413/02 , C07D263/02
CPC分类号： C12P41/004 , C12P7/00 , C12P17/00
摘要： The present invention relates to a process for preparing chiral non-racemic cis-configured cyclohexanols or cyclohexanol derivatives of the formula (I) Cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds which allow a therapeutic modulation of the lipid and/or carbohydrate metabolism and are thus suitable for preventing and/or treating type II diabetes, hyperglycemia and artherosclerosis. The cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds described in the prior art.
摘要翻译： 本发明涉及制备式（I）的手性非外消旋顺式配位的环己醇或环己醇衍生物的方法。式（I）的顺式构型的羟基 - 环己烷羧酸衍生物是用于药物的中心结构单元或直接前体 允许治疗性调节脂质和/或碳水化合物代谢并因此适合于预防和/或治疗II型糖尿病，高血糖症和动脉粥样硬化的活性化合物。 式（I）的顺式构型的羟基 - 环己烷羧酸衍生物是现有技术中描述的药物活性化合物的中心构建块或立即前体。
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公开(公告)号：US20110015400A1
公开(公告)日：2011-01-20
申请号：US12895068
申请日：2010-09-30
IPC分类号： C07D405/06
CPC分类号： C07F7/10 , C07D211/26 , C07D211/52 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/53 , C07D405/06
摘要： This invention is directed to processes for the preparation of a compound of the formula I or salt thereof, that is useful as a tryptase inhibitor, to intermediates useful in the preparation of such a compound, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such a compound.
摘要翻译： 本发明涉及制备式I化合物或其盐的方法，其可用作类胰蛋白酶抑制剂，可用于制备这种化合物的中间体，制备这种中间体的方法，以及 使用这样的中间体制备这种化合物。
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公开(公告)号：US20070197597A1
公开(公告)日：2007-08-23
申请号：US11469599
申请日：2006-09-01
IPC分类号： A61K31/452 , C07D405/02
CPC分类号： C07F7/10 , C07D211/26 , C07D211/52 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/53 , C07D405/06
摘要： This invention is directed to processes for the preparation of a compound of the formula I or salt thereof, that is useful as a tryptase inhibitor, to intermediates useful in the preparation of such a compound, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such a compound.
摘要翻译： 本发明涉及制备式I化合物或其盐的方法，其可用作类胰蛋白酶抑制剂，可用于制备这种化合物的中间体，制备这种中间体的方法，以及 使用这样的中间体制备这种化合物。
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