申请人:KOWA COMPANY LTD.
公开号:EP0541798A1
公开(公告)日:1993-05-19
The present invention provides a diamine compound of formula (I) or an acid addition salt thereof:
wherein R1, R2, R3, R4, R5 and R6 are the same or different from each other and represent individually a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, lower acyloxy group, lower alkoxycarbonyloxy group, lower alkylsulfonyloxy group or am amino group, among which the lower alkyl group and lower alkoxy group may be substituted by a halogen atom or a phenyl group; R7 and R8 are the same or different from each other and represent individually a lower alkyl group or the two bind to each other to represent an alkylene group having 1 to 4 carbon atoms; A and A' are the same or different from each other and represent individually a single bond, -O-, -NH-, -NHCO→, -CONH→, -NHCOO→, NHCONH-, -SO₂NH→ or -COS→ (here, the symbol '→' denotes a bond to Y or Y'), Y and Y' are the same or different from each other and represent a lower alkylene group or lower alkenylene group; and cerebral protective drugs containing such compound.
The diamine compounds (I) or its acid addition salts have an excellent cerebral protective action, are very safe, and exhibit a strong action when even orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.
本发明提供了一种式 (I) 的二胺化合物或其酸加成盐:
其中 R1、R2、R3、R4、R5 和 R6 彼此相同或不同,分别代表氢原子、卤素原子、羟基、低级烷基、低级烷氧基、低级酰氧基、低级烷氧基羰氧基、低级烷基磺酰氧基或氨基,其中低级烷基和低级烷氧基可被卤素原子或苯基取代;R7 和 R8 彼此相同或不同,单独代表一个低级烷基,或两者相互结合代表一个具有 1 至 4 个碳原子的亚烷基;A和A'相同或不同,分别代表单键、-O-、-NH-、-NHCO→、-CONH→、-NHCOO→、NHCONH-、-SO₂NH→或-COS→(此处符号'→'表示与Y或Y'的键),Y和Y'相同或不同,分别代表低级亚烷基或低级亚烯基;以及含有此类化合物的脑保护药物。
二胺化合物(I)或其酸加成盐具有很好的脑保护作用,非常安全,即使口服也能表现出很强的作用,因此,含有此类化合物的药物可有效治疗由脑出血、脑梗塞、蛛网膜下腔出血、短暂性脑缺血发作、脑血管疾病等引起的疾病,或预防此类疾病的进展。