申请人:TORAY INDUSTRIES, INC.
公开号:EP0894799A1
公开(公告)日:1999-02-03
The present invention provides an indolomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing and preventing cerebral disorders composed of the derivative and salt thereof, which is represented by the following formula (I):
[wherein R1 represents cyclopropylmethyl or the like; R2 and R3 each represent hydroxy, methoxy, or the like; R4 represents hydrogen, methyl, benzyl, 3-isothiocyanatopropyl, or the like; and (R5)m represents hydrogen, substituted benzo, or the like].
It was apparent that the compounds of the present invention have the excellent effect of preventing damages of the cerebral nerve cells. Therefore, the compounds of the present invention are useful as medicines used for curing and preventing various cerebral diseases such as cerebral stroke, traumatic cerebral diseases, cerebral edema, and cerebral neurodegenerative diseases, ameliorating aftereffects thereof, and preventing the recurrence thereof by inhibiting various ischemic, hemorrhagic or traumatic cerebral disorders, and damages of the cerebral nerve cells caused by various nerve degenerations.
本发明提供了一种吲哚吗啡南衍生物或其药理上可接受的酸加成盐,以及由该衍生物及其盐组成的治疗和预防脑部疾病的制剂,该衍生物和盐由下式(I)表示:
[其中 R1 代表环丙基甲基或类似物;R2 和 R3 各自代表羟基、甲氧基或类似物;R4 代表氢、甲基、苄基、3-异硫氰酸丙基或类似物;(R5)m 代表氢、取代的苯或类似物]。
显然,本发明的化合物具有防止脑神经细胞受损的卓越功效。因此,本发明化合物通过抑制各种缺血性、出血性或外伤性脑疾病以及各种神经变性引起的脑神经细胞损伤,可作为治疗和预防各种脑疾病(如脑中风、脑外伤疾病、脑水肿和脑神经变性疾病)、改善其后遗症和防止其复发的药物。