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公开(公告)号：US20100331417A1
公开(公告)日：2010-12-30
申请号：US12918787
申请日：2009-02-20
IPC分类号： A61K31/164 , A61P25/00
CPC分类号： A61K31/167 , A61K45/06 , A61K49/0008
摘要： Compounds, methods, uses, compositions, kits and packages for the prevention and/or treatment of neural injury or a neurodegenerative disease, based on the use of a retinoic acid derivative, such as fenretinide, and/or analogs, derivatives, pro-drugs, precursors thereof, and/or salts thereof, are described.
摘要翻译： 基于视黄酸衍生物如芬维A胺和/或类似物衍生物，前药的用途，用于预防和/或治疗神经损伤或神经变性疾病的化合物，用途，组合物，试剂盒和包装 ，其前体和/或其盐。
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公开(公告)号：US08642658B2
公开(公告)日：2014-02-04
申请号：US12918787
申请日：2009-02-20
IPC分类号： A61K31/16 , C07C233/00
CPC分类号： A61K31/167 , A61K45/06 , A61K49/0008
摘要： Compounds, methods, uses, compositions, kits and packages for the prevention and/or treatment of neural injury or a neurodegenerative disease, based on the use of a retinoic acid derivative, such as fenretinide, and/or analogs, derivatives, pro-drugs, precursors thereof, and/or salts thereof, are described.
摘要翻译： 基于视黄酸衍生物如芬维A胺和/或类似物衍生物，前药的用途，用于预防和/或治疗神经损伤或神经变性疾病的化合物，用途，组合物，试剂盒和包装 ，其前体和/或其盐。
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3.发明授权Phospholipase A2 inhibitors and their use in treating neurological injury and disease 失效磷脂酶A2抑制剂及其在治疗神经损伤和疾病中的应用公开(公告)号：US08420852B2
公开(公告)日：2013-04-16
申请号：US12666773
申请日：2008-07-03
申请人： Edward A. Dennis , Daren Stephens , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokotou , Efrosini Barbayianni , Victoria Magrioti
发明人： Edward A. Dennis , Daren Stephens , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokotou , Efrosini Barbayianni , Victoria Magrioti
IPC分类号： C07C229/00 , A01N37/12 , A01N37/44
CPC分类号： C07C235/80
摘要： Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).
摘要翻译： 磷脂酶A2（PLA2）形式在脊髓中表达，其抑制诱导有效的抗痛觉过敏。 提供PLA2抑制剂化合物，其包括由具有烃尾部的2-氧代酰胺和四碳系链组成的共同基序。 化合物阻断IVA类钙依赖性PLA2（cPLA2）和/或VIA钙独立PLA2（iPLA2）和/或V组分泌的PLA2（sPLA2）。 具有cPLA2抑制活性（但不是iPLA2或sPLA2抑制活性）的化合物的药物组合物可用于治疗多发性硬化，而具有sPLA2抑制活性的化合物（以及iPLA2和CPLA2活性）可用于治疗脊髓损伤（具有 相关的功能恢复）。
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4.发明申请Phospholipase A2 Inhibitors and their Use in Treating Neurological Injury and Disease 失效磷脂酶A2抑制剂及其在治疗神经损伤和疾病中的应用公开(公告)号：US20110105610A1
公开(公告)日：2011-05-05
申请号：US12666773
申请日：2008-07-03
申请人： Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
发明人： Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
IPC分类号： A61K31/221 , C07C229/22 , C12N5/071 , A61K31/195 , A61P25/00
CPC分类号： C07C235/80
摘要： Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).
摘要翻译： 磷脂酶A2（PLA2）形式在脊髓中表达，其抑制诱导有效的抗痛觉过敏。 提供PLA2抑制剂化合物，其包括由具有烃尾部的2-氧代酰胺和四碳系链组成的共同基序。 化合物阻断IVA类钙依赖性PLA2（cPLA2）和/或VIA钙独立PLA2（iPLA2）和/或V组分泌的PLA2（sPLA2）。 具有cPLA2抑制活性（但不是iPLA2或sPLA2抑制活性）的化合物的药物组合物可用于治疗多发性硬化，而具有sPLA2抑制活性的化合物（以及iPLA2和CPLA2活性）可用于治疗脊髓损伤（具有 相关的功能恢复）。
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公开(公告)号：US20100048727A1
公开(公告)日：2010-02-25
申请号：US12594579
申请日：2008-04-04
申请人： Samuel David , Athena Kalyvas , Ruben Lopez-Vales , George Kokotos , Violetta Constantinou-Kokotou , Constantinos Baskakis , Christoforos G. Kokotos , Edward A. Dennis , Daren Stephens
发明人： Samuel David , Athena Kalyvas , Ruben Lopez-Vales , George Kokotos , Violetta Constantinou-Kokotou , Constantinos Baskakis , Christoforos G. Kokotos , Edward A. Dennis , Daren Stephens
IPC分类号： A61K31/121 , C12N5/00 , A61K31/12 , C07C49/11 , C07C45/54 , C07C49/105 , C07C49/115 , C07C49/04 , A61P25/00 , A61P29/00
CPC分类号： C07C49/233 , C07C49/167 , C07C49/245 , C07C49/255
摘要： Novel perfluoroketone compounds of formula [I] and [Ia] are described. Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and/or inflammatory conditions, such as demyelinating (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).
摘要翻译： 描述了式[I]和[Ia]的新型全氟酮化合物。 还描述了其用途，例如用于抑制磷脂酶A2活性。 还描述了其治疗用途，例如用于治疗神经病症和/或炎性病症，例如脱髓鞘（例如多发性硬化症）和神经损伤（例如脊髓损伤）。
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