发明申请
US20110105610A1 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
- 专利标题： Phospholipase A2 Inhibitors and their Use in Treating Neurological Injury and Disease
- 专利标题（中）： 磷脂酶A2抑制剂及其在治疗神经损伤和疾病中的应用
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申请号： US12666773申请日： 2008-07-03
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公开(公告)号： US20110105610A1公开(公告)日： 2011-05-05
- 发明人: Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
- 申请人： Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
- 国际申请： PCT/US2008/069257 WO 20080703
- 主分类号： A61K31/221
- IPC分类号： A61K31/221 ; C07C229/22 ; C12N5/071 ; A61K31/195 ; A61P25/00
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).
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