申请人:Zeria Pharmaceutical Co., Ltd.
公开号:US05407950A1
公开(公告)日:1995-04-18
Arylalkanoylamine derivatives having excellent prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia which are represented by the following general formula (I): ##STR1## wherein A represents an indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl group; m represents an integer of 0 to 5; Z represents a hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl group; X and Y may be the same or different, and individually represent a methylene group or sulfur atom, wherein compounds defined by the following substituents are excluded: A represents an indanyl, indenyl, or 1,2,3,4-tetrahydronaphthalenyl group; X and Y each represent a methylene group; and Z represents a hydroxymethyl or formyl group. Also disclosed is a pharmaceutical composition and method for improving mneme, cerebral circulation and cerebral metabolism comprising the arylalkanoylamine derivatives as the effective ingredient.
具有出色的蛋白内切酶抑制作用以及对缺氧和记忆障碍具有抗性的芳基酰胺衍生物,其表示为以下通用式(I):##STR1## 其中A代表吲哚基、茚基、1,2,3,4-四氢萘基或苯并呋喃基;m代表0到5的整数;Z代表羟甲基、甲酰基、腈基、羟肼基甲基、半胱氨酰甲基或二烷氧基甲基;X和Y可以相同也可以不同,分别代表亚甲基基或硫原子,其中被以下取代基定义的化合物被排除:A代表吲哚基、茚基或1,2,3,4-四氢萘基;X和Y各自代表亚甲基基;Z代表羟甲基或甲酰基。还公开了一种包含芳基酰胺衍生物作为有效成分的药物组合物和用于改善记忆、脑循环和脑代谢的方法。