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1.发明授权Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament 有权螺环取代的1,3-丙二醇衍生物，其制备方法及其作为药物的用途公开(公告)号：US08859494B2
公开(公告)日：2014-10-14
申请号：US13176333
申请日：2011-07-05
申请人： Stefanie Keil , Elisabeth Defossa , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
发明人： Stefanie Keil , Elisabeth Defossa , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
IPC分类号： A61K38/28 , A61P5/50 , C07C59/72 , C07D213/64 , C07D305/06 , C07D213/65
CPC分类号： C07C59/72 , C07D213/64 , C07D213/65 , C07D305/06
摘要： The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives, and to the physiologically compatible salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, A and X are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
摘要翻译： 本发明涉及螺环取代的1,3-丙二醇衍生物及其与生理相容的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，A和X各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。
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2.发明授权(2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments 有权（2-芳氧基乙酰氨基）苯基丙酸衍生物，其制备方法及其作为药物的用途公开(公告)号：US08648038B2
公开(公告)日：2014-02-11
申请号：US13176503
申请日：2011-07-05
申请人： Elisabeth Defossa , Stefanie Keil , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
发明人： Elisabeth Defossa , Stefanie Keil , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
CPC分类号： C07C235/24 , C07C255/44
摘要： The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
摘要翻译： 本发明涉及取代的（2-芳氧基乙酰基氨基）苯基丙酸衍生物及其生理上可接受的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和A各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。
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3.发明授权Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments 有权具有氧代基的杂环取代的甲氧基苯基衍生物，其制备方法及其作为药物的用途公开(公告)号：US08530413B2
公开(公告)日：2013-09-10
申请号：US13154946
申请日：2011-06-07
申请人： Stefanie Keil , Elisabeth Defossa , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
发明人： Stefanie Keil , Elisabeth Defossa , Viktoria Dietrich , Siegfried Stengelin , Andreas Herling , Guido Haschke , Thomas Klabunde
CPC分类号： C07D209/34 , C07D215/227 , C07D265/36 , C07D277/68 , C07D498/04
摘要： Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicamentsThe invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
摘要翻译： 具有氧代基的杂环取代的甲氧基苯基衍生物，其制备方法及其作为药物的用途本发明涉及具有氧代基的杂环取代的甲氧基苯基衍生物及其生理上相容的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 10，X，n，B 1，B 2，B 3和B 4各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。
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4.发明授权Phenothiazin derivatives, method for the production thereof and use thereof as pharmaceuticals 有权吩噻嗪衍生物，其制备方法和作为药物的用途公开(公告)号：US07732440B2
公开(公告)日：2010-06-08
申请号：US12507202
申请日：2009-07-22
申请人： Stefanie Keil , Elisabeth Defossa , Karl Schoenafinger , Dieter Schmoll , Axel Deitrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
发明人： Stefanie Keil , Elisabeth Defossa , Karl Schoenafinger , Dieter Schmoll , Axel Deitrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
IPC分类号： C07D417/14 , A61K31/5415
CPC分类号： C07D417/12 , C07D417/14 , C07D513/04
摘要： The invention relates to compounds of the formula I, wherein R1, R2, R3, R4, R5, R6, R7, A and B are as defined herein, the pharmaceutical compositions and the uses as pharmaceuticals.
摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，A和B如本文所定义，药物组合物和用作药物。
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5.发明授权Phenothiazine derivative having a double bond, method for the production thereof, and use thereof as a pharmaceutical 有权具有双键的吩噻嗪衍生物，其制备方法及其作为药物的用途公开(公告)号：US08207146B2
公开(公告)日：2012-06-26
申请号：US12724520
申请日：2010-03-16
申请人： Stefanie Keil , Elisabeth Defossa , Dieter Schmoll , Axel Dietrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
发明人： Stefanie Keil , Elisabeth Defossa , Dieter Schmoll , Axel Dietrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
IPC分类号： A61K31/675 , C07D279/00
CPC分类号： C07D417/12 , C07D513/04
摘要： The present invention relates to substituted phenothiazines with a double bond and physiologically acceptable salts thereof, and their use as a medicament.
摘要翻译： 本发明涉及具有双键的取代吩噻嗪及其生理上可接受的盐，以及它们作为药物的用途。
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![2-heteroaryl-pyrrolo[3,4-c]pyrrole derivatives and their use as SCD inhibitors](/abs-image/US/2011/08/23/US08003677B2/abs.jpg.150x150.jpg)
6.发明授权2-heteroaryl-pyrrolo[3,4-c]pyrrole derivatives and their use as SCD inhibitors 有权2-杂芳基 - 吡咯并[3,4-c]吡咯衍生物及其作为SCD抑制剂的用途公开(公告)号：US08003677B2
公开(公告)日：2011-08-23
申请号：US12605631
申请日：2009-10-26
IPC分类号： A61K31/426
CPC分类号： C07D487/04
摘要： The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.
摘要翻译： 本发明涉及式I的杂环衍生物，其中R，R 1，A，B，D，M，L和n如本文所定义，或其生理上相容的盐，其药物组合物及其作为SCD1抑制剂的用途。
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![2-HETEROARYL-PYRROLO[3,4-C]PYRROLE DERIVATIVES AND THEIR USE AS SCD](/abs-image/US/2011/10/06/US20110245263A1/abs.jpg.150x150.jpg)
7.发明申请2-HETEROARYL-PYRROLO[3,4-C]PYRROLE DERIVATIVES AND THEIR USE AS SCD 审中-公开2-异丙基吡咯并[3,4-C]吡咯并吡喃衍生物及其作为SCD公开(公告)号：US20110245263A1
公开(公告)日：2011-10-06
申请号：US13160705
申请日：2011-06-15
IPC分类号： A61K31/501 , C07D487/04 , A61K31/506 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P3/10 , A61P3/04 , A61K31/427 , A61K31/517 , A61P3/00 , A61P25/28 , A61P25/18
CPC分类号： C07D487/04
摘要： The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.
摘要翻译： 本发明涉及式I的杂环衍生物，其中R，R 1，A，B，D，M，L和n如本文所定义，或其生理上相容的盐，其药物组合物及其作为SCD1抑制剂的用途。
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8.发明授权Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals 有权带有恶二唑酮头孢烯的吡咯烷磺酰胺，其制备方法及其作为药物的用途公开(公告)号：US08329725B2
公开(公告)日：2012-12-11
申请号：US12996784
申请日：2009-05-22
申请人： Stefanie Keil , Matthias Urmann , Wolfgang Wendler , Ulrike Wendler , Maike Glien , Hans Matter , Eugen Falk
发明人： Stefanie Keil , Matthias Urmann , Wolfgang Wendler , Ulrike Wendler , Maike Glien , Hans Matter , Eugen Falk
CPC分类号： C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/04
摘要： The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译： 本发明涉及具有恶二唑酮头基的环状吡咯烷磺酰胺及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARδ和PPARα激动剂活性。 所描述的是式（I）的化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。
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9.发明申请ANNELATED N-HETEROCYCLIC SULFONAMIDES WITH OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 有权与OXADIAZOLONE HEADGROUP联合的N-杂环磺酰胺，其制备方法及其作为药物的用途公开(公告)号：US20120122853A1
公开(公告)日：2012-05-17
申请号：US12996692
申请日：2009-05-22
申请人： Stefanie Keil , Matthias Urmann , Wolfgang Wendler , Maike Glien , Hans Matter , Eugen Falk , Ulrike Wendler
发明人： Stefanie Keil , Matthias Urmann , Wolfgang Wendler , Maike Glien , Hans Matter , Eugen Falk , Ulrike Wendler
IPC分类号： A61K31/55 , C07D471/04 , C07D413/14 , C07D498/04 , A61K31/4375 , A61P3/00 , A61K31/4709 , A61K31/5383 , A61P3/10 , A61P3/06 , A61P25/00 , C07D413/12 , A61K31/538
CPC分类号： C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/04
摘要： Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译： 具有恶二唑酮头基的神经化N-杂环磺酰胺，其制备方法及其作为药物的用途本发明涉及具有恶二唑酮头基的环状N-杂环磺酰胺及其生理学上可接受的盐和生理功能衍生物，其显示PPARδ或PPARα和PPARα激动剂活性。 所描述的是式I化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。
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10.发明授权2-{-3,′2-(phenyl)-oxazol-4-ylmethoxyl-cyclohexyl methoxy}-propionic acid derivatives used as peroxisome proliferator-activated receptor (PPAR) ligands for the treatment of hyperlipidemia and diabetes 有权用作治疗高脂血症和糖尿病的过氧化物酶体增殖物激活受体（PPAR）配体的2 - { - 3，“2-（苯基） - 恶唑-4-基甲氧基] - 环己基甲氧基} - 丙酸衍生物公开(公告)号：US07956077B2
公开(公告)日：2011-06-07
申请号：US11671673
申请日：2007-02-06
申请人： Heiner Glombik , Christian Stapper , Eugen Falk , Stefanie Keil , Hans-Ludwig Schaefer , Wolfgang Wendler , Stephanie Knieps
发明人： Heiner Glombik , Christian Stapper , Eugen Falk , Stefanie Keil , Hans-Ludwig Schaefer , Wolfgang Wendler , Stephanie Knieps
IPC分类号： A01N43/76 , C07D263/34
CPC分类号： C07D263/32
摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein the various substituent R-groups are more specifically defined herein.
摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及包含具有环己基甲氧基取代基的乙酸衍生物及其盐的血液的那些胰岛素相关代谢紊乱，例如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中各种取代基R基团在本文中更具体地定义。
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