PROPHYLACTIC OR THERAPEUTIC AGENT FOR OPTIC NERVE DISORDERS COMPRISING 4,6-DICHLORO-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVE OR SALT THEREOF AS ACTIVE INGREDIENT
申请人:Santen Pharmaceutical Co., Ltd
公开号:EP2407454A1
公开(公告)日:2012-01-18
Disclosed is a compound useful as a preventive or therapeutic agent for optic nerve disorders, an inhibitor of retinal ganglion cell death or an agent for restoring the expression level of a neurofilament light chain, particularly a compound capable of exhibiting the abovementioned pharmacological activities when administered orally. A 4,6-dichloro-1H-indole-2-carboxylic acid derivative or a salt thereof can significantly inhibit the decrease in the number of cells in a retinal ganglion cell layer of an NMDA-induced rat retinal disorder model when administered to the model orally, and can also restore the decrease in the expression level of a neurofilament light chain in a retina of the model when administered to the model intravitreally (intraocular local administration). Therefore, the compound or a salt thereof is useful as a preventive or therapeutic agent for optic nerve disorders, an inhibitor of retinal ganglion cell death or an agent for restoring the expression level of a neurofilament light chain.
本发明公开了一种可作为视神经疾病的预防或治疗剂、视网膜神经节细胞死亡抑制剂或恢复神经丝蛋白轻链表达水平的药物的化合物,特别是一种在口服给药时能够表现出上述药理活性的化合物。一种 4,6-二氯-1H-吲哚-2-羧酸衍生物或其盐在口服给药 NMDA 诱导的大鼠视网膜紊乱模型时,能显著抑制该模型视网膜神经节细胞层细胞数量的减少;在玻璃体内给药(眼内局部给药)时,还能恢复该模型视网膜中神经丝轻链表达水平的减少。因此,该化合物或其盐类可用作视神经疾病的预防或治疗药物、视网膜神经节细胞死亡抑制剂或恢复神经丝轻链表达水平的药物。