申请人:Nisshin Flour Milling Co., Ltd.
公开号:EP0885886A1
公开(公告)日:1998-12-23
Pyridinecarboxamide derivatives of the formula
(wherein n represents an integer of 14 - 18, and R represents a hydrogen atom or a straight or branched C1-C4 alkyl group) or physiologically acceptable salts thereof.
The compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed death of neuronal cells (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage of cerebrovascular disorders and then the compounds are useful as an agent for inhibiting cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, the compounds have no hypotensive action which is considered to be side-effect in treating the acute stage cerebrovascular disorders and hardly show a behavior suppressing action so that 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 increasing activity of cerebral blood flow, and an inhibiting activity of lipid peroxidation and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
式中的吡啶甲酰胺衍生物
(其中 n 代表 14 - 18 的整数,R 代表氢原子或直链或支链 C1-C4 烷基)或其生理上可接受的盐。
这些化合物对脑水肿,尤其是缺血性脑水肿有很好的抑制作用,对神经元细胞的延迟死亡也有很好的抑制作用(抑制神经元细胞中 Ca 的内流)。脑水肿是脑血管疾病,尤其是脑血管疾病急性期的一种病理状态,因此,这些化合物可作为抑制脑水肿的药物或脑血管疾病的治疗药物。此外,这些化合物在治疗急性期脑血管疾病时没有被认为是副作用的降压作用,也几乎没有行为抑制作用,因此是一种特别适用于急性期脑血管疾病的优良治疗剂。此外,这些化合物还显示出脑保护活性(抗缺氧活性)、增加脑血流量活性和抑制脂质过氧化活性,这些活性可能会增加其作为脑血管疾病治疗剂的效用。