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1.发明申请公开(公告)号：US20070179191A1
公开(公告)日：2007-08-02
申请号：US11535266
申请日：2006-09-26
申请人： Stefanie KEIL , Wolfgang WENDLER , Maike GLIEN , Jochen GOERLITZER , Karen CHANDROSS , Daniel McGARRY , Jean MERRILL , Patrick BERNARDELLI , Baptiste RONAN , Corinne TERRIER
发明人： Stefanie KEIL , Wolfgang WENDLER , Maike GLIEN , Jochen GOERLITZER , Karen CHANDROSS , Daniel McGARRY , Jean MERRILL , Patrick BERNARDELLI , Baptiste RONAN , Corinne TERRIER
IPC分类号： A61K31/4245 , C07D413/02
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 demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuroinflammatory 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; 涉及神经炎症过程和/或其他周围神经病变的中枢和周围神经系统的神经变性疾病和/或脱髓鞘疾病和/或神经疾病。
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2.发明申请1,3,4-OXADIAZOL-2-ONES AS PPAR DELTA MODULATORS AND THEIR USE THEREOF 失效1,3,4-OXADIAZOL-2-ONES作为PPAR DELTA调制器及其使用公开(公告)号：US20070060626A1
公开(公告)日：2007-03-15
申请号：US11535227
申请日：2006-09-26
申请人： Daniel MCGARRY , Karen CHANDROSS , Jean MERRILL , Jochen GOERLITZER , Stefanie KEIL , Wolfgang WENDLER , Patrick BERNARDELLI
发明人： Daniel MCGARRY , Karen CHANDROSS , Jean MERRILL , Jochen GOERLITZER , Stefanie KEIL , Wolfgang WENDLER , Patrick BERNARDELLI
IPC分类号： A61K31/427 , A61K31/4245 , C07D413/02 , C07D417/02
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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3.发明申请1, 3, 4-OXADIAZOL-2-ONES AS PPAR DELTA MODULATORS AND THEIR USE THEREOF 失效1，3，4-OXADIAZOL-2-ONES作为PPAR DELTA调制器及其使用公开(公告)号：US20090275621A1
公开(公告)日：2009-11-05
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 , C07D277/30 , A61K31/426 , C07D413/12
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.发明申请USE OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA AGONISTS FOR THE TREATMENT OF MS AND OTHER DEMYELINATING DISEASES 审中-公开使用过氧化物酶促活化激活受体三角体激动剂治疗MS和其他脱髓鞘疾病公开(公告)号：US20070149580A1
公开(公告)日：2007-06-28
申请号：US11535240
申请日：2006-09-26
申请人： Karen CHANDROSS , Jean MERRILL , Anne MINNICH , Lan LEE , Olga KHORKOVA , Yun LIU
发明人： Karen CHANDROSS , Jean MERRILL , Anne MINNICH , Lan LEE , Olga KHORKOVA , Yun LIU
IPC分类号： A61K31/426 , A61K31/192
CPC分类号： A61K31/426 , A61K31/192 , A61K2300/00
摘要： A method for treating demyelinating diseases in a patient in need thereof by treatment with an effective amount of a PPAR delta agonist is disclosed. Demyelinating diseases that may be effectively treated by this method include but are not limited to multiple sclerosis, Charcot-Marie-Tooth disease, Pelizaeus-Merzbacher disease, encephalomyelitis, neuromyelitis optica, adrenoleukodystrophy, Guillian-Barre syndrome and disorders in which myelin forming glial cells are damaged including spinal cord injuries, neuropathies and nerve injury.
摘要翻译： 公开了通过用有效量的PPARδ激动剂治疗来治疗有需要的患者脱髓鞘疾病的方法。 可以通过该方法有效治疗的脱髓鞘疾病包括但不限于多发性硬化症，Charcot-Marie-Tooth病，Pelizaeus-Merzbacher病，脑脊髓炎，视神经脊髓炎，肾上腺脑白质营养不良，Guillian-Barre综合征和髓鞘形成胶质细胞的疾病 损伤包括脊髓损伤，神经病变和神经损伤。
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5.发明申请USE OF CERTAIN BIPHENYL COMPOUNDS FOR PROTECTION OF NEURONS AND OLIGODENDROCYTES IN THE TREATMENT OF MULTIPLE SCLEROSIS (MS) 审中-公开使用某些联苯化合物保护神经元和寡糖在治疗多发性硬化（MS）公开(公告)号：US20070249706A1
公开(公告)日：2007-10-25
申请号：US11757607
申请日：2007-06-04
IPC分类号： A61K31/047 , A61K31/135 , A61K31/341 , A61K31/40
CPC分类号： A61K31/136 , A61K31/047 , A61K31/05 , A61K31/135 , A61K31/341 , A61K31/40 , A61K31/402
摘要： A method for the treatment of multiple sclerosis through the protection on the central nervous system neurons or oligodendrocytes which comprises administering to a patient having multiple sclerosis a therapeutically effective amount of a biphenyl compound as defined by formula I as follows: Wherein R1, R2, R3 and R4 are as defined herein
摘要翻译： 一种通过对中枢神经系统神经元或少突胶质细胞的保护来治疗多发性硬化的方法，其包括向具有多发性硬化症的患者施用治疗有效量的式I定义的联苯化合物如下：其中R 1 R 2，R 3和R 4如本文所定义
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公开(公告)号：US20080033005A1
公开(公告)日：2008-02-07
申请号：US11764259
申请日：2007-06-18
IPC分类号： A61K31/4375
CPC分类号： A61K31/381 , A61K31/445 , A61K31/47
摘要： Certain compounds, including 5,6-dihydro-3,9-dihydroxyindolo[2,1-a-isoquinolin12yl)[4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone and arzoxifen, are useful for providing protection to oligodendrocytes and neurons of multiple sclerosis patients.
摘要翻译： 某些化合物，包括5,6-二氢-3,9-二羟基吲哚并[2,1-a-异喹啉基] [4- [2-（1-哌啶基）乙氧基]苯基] - 甲酮和阿佐昔芬，可用于提供保护 多发性硬化症患者的少突胶质细胞和神经元。
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7.发明申请USE OF CERTAIN PHENYL NAPTHYL COMPOUNDS FOR PROTECTION OF NEURONS AND OLIGODENDROCYTES IN THE TREATMENT OF MULTIPLE SCLEROSIS (MS) 审中-公开在治疗多发性硬化症（MS）中使用某些苯甲酸钠化合物治疗神经元和寡糖化合物公开(公告)号：US20070249732A1
公开(公告)日：2007-10-25
申请号：US11757604
申请日：2007-06-04
CPC分类号： A61K31/05 , A61K31/055
摘要： Certain biphenyl compounds, including 5-chloro-6-(4-hydroxyphenyl)-2-naphthalenol and 6-(4-hydroxy-phenyl)-2-naphthalene methanol are useful in the treatment of multiple sclerosis on the cellular level of the central nervous system through the protection of the patients' oligodendrocytes and neurons.
摘要翻译： 某些联苯化合物，包括5-氯-6-（4-羟基苯基）-2-萘酚和6-（4-羟基 - 苯基）-2-萘甲醇可用于治疗中枢细胞水平的多发性硬化 神经系统通过保护患者的少突胶质细胞和神经元。
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8.发明申请USE OF CERTAIN PHENYL-NAPHTHYL COMPOUNDS THAT DO NOT HAVE SIGNIFICANT AFFINITY TO ER ALPHA OR ER BETA FOR PROTECTION OF NEURONS AND OLIGODENDROCYTES IN THE TREATMENT OF MULTIPLE SCLEROSIS 审中-公开使用某些苯甲酸化合物，对于治疗多发性SCLEROSIS而言，不会对神经元和寡糖在保护神经元和寡核苷酸中具有重要的亲和力公开(公告)号：US20070225330A1
公开(公告)日：2007-09-27
申请号：US11758884
申请日：2007-06-06
IPC分类号： A61K31/445 , A61K31/138 , A61K31/075 , A61K31/05
CPC分类号： A61K31/05 , A61K31/055 , A61K31/075 , A61K31/138 , A61K31/445
摘要： The invention provides a new use for certain SERM-like phenylnaphthyl compounds that do not exhibit affinity for alpha or beta type estrogen receptors (ER) in the treatment of multiple sclerosis.
摘要翻译： 本发明提供了在治疗多发性硬化中不表现出对α或β型雌激素受体（ER）的亲和力的某些SERM样苯基萘基化合物的新用途。
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