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1.发明申请METHODS FOR THE TREATMENT OF METABOLIC AND GLUCOSE UTILIZATION DISORDERS THROUGH THE ADMINISTRATION OF OXADIAZOLONES AND DERIVATIVES THEREOF AS PEROXISOME PROLIFERATOR - ACTIVATED RECEPTOR (PPAR) DELTA AGONISTS 审中-公开用于治疗代谢性和葡萄糖利用疾病的方法通过将过氧化物酶体增殖物 - 激活受体（PPAR）三角体激动剂作为过氧化物体和衍生物的施用公开(公告)号：US20080262052A1
公开(公告)日：2008-10-23
申请号：US12133408
申请日：2008-06-05
申请人： Stefanie KEIL , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Daniel G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
发明人： Stefanie KEIL , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Daniel G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
IPC分类号： A61K31/4245 , C07D271/06 , A61P3/10 , A61P25/28
CPC分类号： C07D417/12 , C07D413/12
摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta 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; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.
摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能衍生物，显示出PPARδ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涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。
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2.发明授权1, 3, 4-oxadiazol-2-ones as peroxisome-proliferator activated receptor delta modulators and their use in the treatment of neurological and metabolic disease 失效1,3,4-恶二唑-2-酮作为过氧化物酶体增殖物激活受体δ调节剂及其在治疗神经和代谢疾病中的应用公开(公告)号：US07638539B2
公开(公告)日：2009-12-29
申请号：US11535764
申请日：2006-09-27
申请人： Daniel G. McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandross , Jean Merrill , Wolfgang Wendler
发明人： Daniel G. McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandross , Jean Merrill , Wolfgang Wendler
IPC分类号： A61K31/4245 , A61K31/427 , C07D271/113 , C07D277/20
CPC分类号： C07D417/12 , C07D277/24 , C07D277/30
摘要： The present invention is directed to 1,3,4-oxadiazalones, i.e., the compounds of formula I and their pharmaceutically acceptable salts, stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization such as multiple scleroses.
摘要翻译： 本发明涉及1,3,4-恶二唑酮，即式I化合物及其药学上可接受的盐，立体异构体，互变异构体或溶剂合物。 新型化合物包括式I化合物，其中基团如本文所定义。 本发明的化合物是PPARdta的调节剂，因此可用作药剂，特别是用于治疗脱髓鞘疾病和脂肪酸代谢紊乱以及葡萄糖利用如多种硬化症。
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3.发明授权1, 3, 4-oxadiazol-2-ones as PPAR delta modulators and their use thereof 失效1,3,4-恶二唑-2-酮作为PPARδ调节剂及其用途公开(公告)号：US07872032B2
公开(公告)日：2011-01-18
申请号：US12505881
申请日：2009-07-20
申请人： Daniel G. McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandross , Jean Merrill , Wolfgang Wendler
发明人： Daniel G. McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandross , Jean Merrill , Wolfgang Wendler
IPC分类号： A61K31/427 , A61K31/426 , A61K31/422 , A61K31/443 , C07D277/30 , C07D413/12 , C07D271/113 , C07D419/02
CPC分类号： C07D417/12 , C07D277/24 , C07D277/30
摘要： The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.
摘要翻译： 本发明涉及1,3,4-恶二唑酮，式I化合物及其药学上可接受的盐立体异构体，互变异构体或溶剂化物。 新型化合物包括式I化合物，其中基团如本文所定义。 本发明的化合物是PPARdta的调节剂，因此可用作药剂，特别是用于治疗脱髓鞘疾病和脂肪酸代谢和葡萄糖利用的障碍。
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4.发明授权Oxadiazolones and derivatives thereof as peroxisome proliferator-activated receptor (PPAR) delta agonists 有权作为过氧化物酶体增殖物激活受体（PPAR）δ激动剂的恶二唑酮及其衍生物公开(公告)号：US07709509B2
公开(公告)日：2010-05-04
申请号：US12133405
申请日：2008-06-05
申请人： Stefanie Keil , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Daniel G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
发明人： Stefanie Keil , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Daniel G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
IPC分类号： A61K31/4245 , A61K31/422 , A61K31/427 , C07D277/20 , C07D271/07 , C07D263/30
CPC分类号： C07D417/12 , C07D413/12
摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. 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; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.
摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，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涉及胰岛素抵抗的疾病; 中枢和周围神经系统的神经变性疾病和/或脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。
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5.发明授权1,3,4-oxadiazol-2-ones as PPAR delta modulators and their use thereof 失效1,3,4-恶二唑-2-酮作为PPARδ调节剂及其用途公开(公告)号：US07576109B2
公开(公告)日：2009-08-18
申请号：US11535227
申请日：2006-09-26
申请人： Daniel G. McGarry , Karen Chandross , Jean Merrill , Jochen Goerlitzer , Stefanie Keil , Wolfgang Wendler , Patrick Bernardelli
发明人： Daniel G. McGarry , Karen Chandross , Jean Merrill , Jochen Goerlitzer , Stefanie Keil , Wolfgang Wendler , Patrick Bernardelli
IPC分类号： A61K31/4245 , C07D271/10 , C07D413/10
CPC分类号： C07D417/12
摘要： The present invention is directed to 1,3,4-oxadiazolones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.
摘要翻译： 本发明涉及1,3,4-恶二唑酮，式I化合物及其药学上可接受的盐立体异构体，互变异构体或溶剂合物。 新型化合物包括式I化合物，其中基团如本文所定义。 本发明的化合物是PPARdta的调节剂，因此可用作药剂，特别是用于治疗脱髓鞘疾病和脂肪酸代谢和葡萄糖利用的障碍。
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6.发明申请OXADIAZOLONES AND DERIVATIVES THEREOF AS PEROXISOME PROLIFERATOR - ACTIVATED RECEPTOR (PPAR) DELTA AGONISTS 有权氧化氮和衍生物作为过氧化物酶促活化剂 - 激活受体（PPAR）三角激素公开(公告)号：US20080255212A1
公开(公告)日：2008-10-16
申请号：US12133405
申请日：2008-06-05
申请人： Stefanie KEIL , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Danie G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
发明人： Stefanie KEIL , Wolfgang Wendler , Maike Glien , Jochen Goerlitzer , Karen Chandross , Danie G. McGarry , Jean Merrill , Patrick Bernardelli , Baptiste Ronan , Corinne Terrier
IPC分类号： A61K31/4245 , C07D271/07 , A61P3/00
CPC分类号： C07D417/12 , C07D413/12
摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. 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; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.
摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，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涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。
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7.发明申请1, 3, 4-OXADIAZOL-2-ONES AS PEROXISOME-PROLIFERATOR ACTIVATED RECEPTOR DELTA MODULATORS AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL AND METABOLIC DISEASE 失效1，3，4-OXADIAZOL-2-ONES作为过氧化物酶体增殖物激活受体调节剂及其在治疗神经病学和代谢疾病中的应用公开(公告)号：US20070099964A1
公开(公告)日：2007-05-03
申请号：US11535764
申请日：2006-09-27
申请人： Daniel McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandros , Jean Merrill , Wolfgang Wendler
发明人： Daniel McGarry , Jochen Goerlitzer , Stefanie Keil , Karen Chandros , Jean Merrill , Wolfgang Wendler
IPC分类号： A61K31/4439 , A61K31/4245 , A61K31/427 , C07D413/14 , C07D417/14
CPC分类号： C07D417/12 , C07D277/24 , C07D277/30
摘要： The present invention is directed to 1,3,4-oxadiazalones, i.e., the compounds of formula I and their pharmaceutically acceptable salts, stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization such as multiple scleroses.
摘要翻译： 本发明涉及1,3,4-恶二唑酮，即式I化合物及其药学上可接受的盐，立体异构体，互变异构体或溶剂合物。 新型化合物包括式I化合物，其中基团如本文所定义。 本发明的化合物是PPARdta的调节剂，因此可用作药剂，特别是用于治疗脱髓鞘疾病和脂肪酸代谢紊乱以及葡萄糖利用如多种硬化症。
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公开(公告)号：US20070280885A1
公开(公告)日：2007-12-06
申请号：US11568525
申请日：2005-05-04
申请人： Karen Chandross , Jean Merrill , Sridaran Natesan
发明人： Karen Chandross , Jean Merrill , Sridaran Natesan
CPC分类号： G01N33/6872 , C12Q1/485 , G01N33/6896 , G01N2333/71 , G01N2500/02
摘要： Methods of identifying and using compounds capable of treating demyelinating disorders such as multiple sclerosis by inhibiting EphB1-mediated cell repulsion of CNS and PNS glial cells (oligodendrocytes and Schwann cells and progenitor cells within these lineages).
摘要翻译： 鉴定和使用能够通过抑制CNS和PNS胶质细胞（这些谱系中的少突胶质细胞和雪旺氏细胞和祖细胞）的EphB1介导的细胞排斥来治疗脱髓鞘疾病如多发性硬化的化合物的方法。
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公开(公告)号：US20050054681A1
公开(公告)日：2005-03-10
申请号：US10925292
申请日：2004-08-24
申请人： Sharon Jackson , Thaddeus Nieduzak , Sam Rebello , Guyan Liang , Yulin Chiang , Jean Merrill
发明人： Sharon Jackson , Thaddeus Nieduzak , Sam Rebello , Guyan Liang , Yulin Chiang , Jean Merrill
IPC分类号： C07D311/46 , C07D405/12 , C07D407/12 , A61K31/443 , A61K31/366 , A61K31/4025 , A61K31/55 , A61K31/554 , C07D45/02
CPC分类号： C07D405/12 , C07D311/46 , C07D407/12
摘要： The present invention relates to coumarins of the formula (I): that are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions and methods of using these compounds as inhibitors of nitric oxide synthase are described herein.
摘要翻译： 本发明涉及式（I）的香豆素：其可用作一氧化氮合酶的抑制剂。 本文描述了使用这些化合物作为一氧化氮合酶抑制剂的药物组合物和方法。
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公开(公告)号：US07538233B2
公开(公告)日：2009-05-26
申请号：US10925292
申请日：2004-08-24
申请人： Sharon Jackson , Thaddeus Nieduzak , Sam Rebello , Guyan Liang , Yulin Chiang , Jean Merrill
发明人： Sharon Jackson , Thaddeus Nieduzak , Sam Rebello , Guyan Liang , Yulin Chiang , Jean Merrill
IPC分类号： C07D311/02 , A61K31/35
CPC分类号： C07D405/12 , C07D311/46 , C07D407/12
摘要： The present invention relates to coumarins of the formula (I): that are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions and methods of using these compounds as inhibitors of nitric oxide synthase are described herein.
摘要翻译： 本发明涉及式（I）的香豆素：其可用作一氧化氮合酶的抑制剂。 本文描述了使用这些化合物作为一氧化氮合酶抑制剂的药物组合物和方法。
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