Edward A. Dennis,Daren Stephens,Samuel David,Ruben Lopez-Vales,Athena Kalyvas,George Kokotos,Violetta Constantinou-Kokotou,Efrosini Barbayianni,Victoria Magrioti
申请号：
US12666773
公开号：
US08420852B2
申请日:
2008.07.03
申请国别(地区):
US
年份:
2013
代理人:
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).
