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1.发明申请METHOD FOR THE PREPARATION OF OXAZOLES BY CONDENSING AROMATIC ALDEHYDES WITH ALPHA-KETOXIMES TO FORM N-OXIDES AND REACTING SAME WITH ACTIVATIVED ACID DERIVATIVES 有权通过将具有阿尔卡胶的芳族醛缩合形成N-氧化物并用活性酸衍生物反应的方法制备氧化剂的方法公开(公告)号：US20080058529A1
公开(公告)日：2008-03-06
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 SCHEFFER
发明人： Wolfgang HOLLA , Rolf-Ludwig HOERLEIN , Berndt KULITZSCHER , Wolfgang LAUX , Thomas STUEDEMANN , Christoph TAPPERTZHOFEN , Robert SCHEFFER
IPC分类号： C07D263/30
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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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：US5018554A
公开(公告)日：1991-05-28
申请号：US394533
申请日：1989-08-16
申请人： Berndt Kulitzscher
发明人： Berndt Kulitzscher
CPC分类号： F04B11/0091
摘要： In the device for the damping of pumps with intermittent delivery, a feed line (2) and a discharge line (3) for the medium to be delivered protrude into a slender tube (1), closed on both sides. The lines (2, 3) are led into the tube through one of the closed ends of the tube (1). In this arrangement, at least the outflow opening (8) for the discharge line (3) is arranged in the vicinity of the other closed end (9) of the tube.
摘要翻译： 在用于间歇输送的泵的阻尼装置中，用于要输送的介质的进料管线（2）和排出管线（3）突出到细长管（1）中，两侧封闭。 线（2,3）通过管（1）的一个封闭端引入管中。 在这种布置中，至少用于排出管线（3）的流出口（8）布置在管的另一封闭端（9）附近。
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4.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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5.发明授权Process for the preparation of chiral, nonracemic (4-aryl-2,5-dioxoimidazolidin-1-yl) acetic acids 失效手性，非糖化（4-芳基-2,5-二氧代咪唑烷-1-基）乙酸的制备方法
公开(公告)号：US6018053A
公开(公告)日：2000-01-25
申请号：US879289
申请日：1997-06-19
IPC分类号： A61K31/415 , A61K31/4166 , A61P7/02 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/80
CPC分类号： C07D233/76
摘要： The present invention relates to a process for the preparation of chiral, nonracemic compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings indicated in claim 1 and which are useful intermediates for the preparation of pharmaceutical active compounds in which, for resolution, a salt is formed from the racemic compound of the formula I and a chiral, nonracemic amino compound. It furthermore relates to compounds of the formula I and esters thereof.
摘要翻译： 本发明涉及制备式I的手性，非微量化合物的方法，其中R 1和R 2具有权利要求1所示的含义，并且它们是制备药物活性化合物的有用的中间体，其中为了拆分， 盐由式I的外消旋化合物和手性，非糖化的氨基化合物形成。 此外，它还涉及式I的化合物及其酯。
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6.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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7.发明申请METHOD FOR THE PRODUCTION OF OXAZOLES BY CONDENSING AROMATIC ALDEHYDES WITH a-KETOXIMES TO N-OXIDES AND THEN REACTING THE SAME WITH ACTIVATED ACID DERIVATIVES 有权通过将具有α-酮氧化物的芳族醛缩合到N-氧化物上并随后与活化酸衍生物反应来生产氧化剂的方法公开(公告)号：US20090286988A1
公开(公告)日：2009-11-19
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： 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-氧化物转化成式Ⅳ的卤代甲基唑将式Ⅰ的芳族醛转化成式Ⅳ的卤代甲基恶唑，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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8.发明申请NOVEL INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF OXAZOLES AND PHARMACEUTICAL ACTIVES FOR THE REGULATION OF LIPID AND GLUCOSE METABOLISM 审中-公开用于制备用于调节脂质和葡萄糖代谢的氧化剂和药物活性的新型中间体化合物公开(公告)号：US20080114035A1
公开(公告)日：2008-05-15
申请号：US11928117
申请日：2007-10-30
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： A61K31/4439 , A61K31/421 , C07D413/04
CPC分类号： C07D263/32
摘要： The present invention is directed to compounds of Formula III wherein the R1-R7 groups or substituents are defined herein. The present invention also comprises improved methods in the preparation of oxazoles in which the compounds of Formula III are intermediates and 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： 本发明涉及式III化合物，其中R 1 -R 7基团或取代基在本文中定义。 本发明还包括制备恶唑的改进方法，其中式III的化合物是中间体，并且其产生更高的产率，更少的杂质和污染物。 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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公开(公告)号：US20120264925A1
公开(公告)日：2012-10-18
申请号：US13391759
申请日：2010-08-26
申请人： Michael Podeschwa , David Rigal , Kai Rossen , Bernhard Otto , Hermut Wehlan , Theodor Andreas Wollmann , Bernd Becker , Berndt Kulitzscher , Alexander Schaefer
发明人： Michael Podeschwa , David Rigal , Kai Rossen , Bernhard Otto , Hermut Wehlan , Theodor Andreas Wollmann , Bernd Becker , Berndt Kulitzscher , Alexander Schaefer
IPC分类号： C07H17/02 , C07D231/20 , C07C69/716
摘要： A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C1-C3)-alkylene, (C2-C3)-alkenylene.
摘要翻译： 制备通式（I）的吡唑 - 糖苷衍生物的方法，其中R 1 H和R 2 F的含义; 或R1F和R2H; 或R1F和R2F; R3（C1-C8） - 烷基，其中一个，多于一个或全部氢可以被氟代替; X（C 1 -C 3） - 亚烷基，（C 2 -C 3） - 亚烯基。
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10.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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