申请人:Nisshin Flour Milling Co., Ltd.
公开号:EP0882716A1
公开(公告)日:1998-12-09
N-(12-Nitroxydodecyl)-6-(4-ethyl or isopropyl-1-piperazinyl)pyridine-3-carboxamide or physiologically acceptable salts thereof.
The said compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed neuronal death (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage cerebrovascular disorders and then the compounds are useful as an inhibiting agent for cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, because the compounds do hardly show a behavior suppressing action, which is considered to be side effect in treating cerebrovascular disorders at the acute stage, they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an activity of increasing cerebral blood flow, and an activity of inhibiting lipid peroxidation, and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
N-(12-硝基十二烷基)-6-(4-乙基或异丙基-1-哌嗪基)吡啶-3-甲酰胺或其生理上可接受的盐类。
上述化合物对脑水肿(尤其是缺血性脑水肿)有很好的抑制作用,对延迟神经元死亡(抑制神经元细胞中 Ca 的流入)也有很好的抑制作用。脑水肿是脑血管疾病,尤其是急性期脑血管疾病的一种病理状态,因此,这些化合物可作为脑水肿的抑制剂或脑血管疾病的治疗剂。此外,由于这些化合物在急性期治疗脑血管疾病时几乎不表现出被认为具有副作用的行为抑制作用,因此,它们尤其是急性期脑血管疾病的极佳治疗剂。此外,这些化合物还具有脑保护活性(抗缺氧活性)、增加脑血流量的活性和抑制脂质过氧化的活性,这些活性可能会增加其作为脑血管疾病治疗剂的效用。