公开(公告)号：EP0536399B1

公开(公告)日：1996-01-24

申请号：EP91910447.1

申请日：1991-06-07

申请人： ZERIA PHARMACEUTICAL CO., LTD.

发明人： OKUBO, Akihiro, Zeria Pharmac. Co., Ltd. ,  NISHIOKA, Hiroyasu, Zeria Pharmac. Co., Ltd. ,  ARAI, Heihachiro, Zeria Pharamc. Co., Ltd. ,  TANAKA, Yoshiaki, Zeria Pharmac. Co., Ltd. ,  KATO, Hisayoshi, Zeria Pharmac. Co., Ltd. ,  NAKATA, Naoki, Zeria Pharmac. Co., Ltd.

IPC分类号： C07D207/16 ,  A61K31/40 ,  A61K31/425 ,  C07D277/06 ,  C07D417/14 ,  C07D405/14 ,  C07D417/06

CPC分类号： C07D405/14 ,  C07D207/16 ,  C07D277/06 ,  C07D417/06 ,  C07D417/14

摘要： An arylalkanoylamine derivative represented by general formula (I), excellent in a prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia; and a drug for improving mneme, cerebral circulation and cerebral metabolism, containing the same as the active ingredient, wherein A represents indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl; m is an integer of 0 to 5; Z represents hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl and X and Y may be the same or different from each other and each represents methylene or sulfur, provided that the case where A represents indanyl, indenyl or 1,2,3,4-tetrahydronaphthalenyl, X and Y represent both methylene, and Z represents hydroxymethyl or formyl is excluded.

公开(公告)号：EP0536399A1

公开(公告)日：1993-04-14

申请号：EP91910447.1

申请日：1991-06-07

申请人： ZERIA PHARMACEUTICAL CO., LTD.

发明人： OKUBO, Akihiro, Zeria Pharmac. Co., Ltd. ,  NISHIOKA, Hiroyasu, Zeria Pharmac. Co., Ltd. ,  ARAI, Heihachiro, Zeria Pharamc. Co., Ltd. ,  TANAKA, Yoshiaki, Zeria Pharmac. Co., Ltd. ,  KATO, Hisayoshi, Zeria Pharmac. Co., Ltd. ,  NAKATA, Naoki, Zeria Pharmac. Co., Ltd.

IPC分类号： C07D207/16 ,  A61K31/40 ,  A61K31/425 ,  C07D277/06 ,  C07D417/14 ,  C07D405/14 ,  C07D417/06

CPC分类号： C07D405/14 ,  C07D207/16 ,  C07D277/06 ,  C07D417/06 ,  C07D417/14

摘要： An arylalkanoylamine derivative represented by general formula (I), excellent in a prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia; and a drug for improving mneme, cerebral circulation and cerebral metabolism, containing the same as the active ingredient, wherein A represents indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl; m is an integer of 0 to 5; Z represents hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl and X and Y may be the same or different from each other and each represents methylene or sulfur, provided that the case where A represents indanyl, indenyl or 1,2,3,4-tetrahydronaphthalenyl, X and Y represent both methylene, and Z represents hydroxymethyl or formyl is excluded.

摘要翻译： 通式（I）表示的芳基烷酰胺衍生物，脯氨酰内肽酶抑制作用优异，对缺氧和遗忘有抵抗性; 其中A代表茚满基，茚基，1,2,3,4-四氢萘基或苯并呋喃基;以及含有相同活性成分的用于改善病态，脑循环和脑代谢的药物。 m是0至5的整数; Z代表羟甲基，甲酰基，腈基，羟基亚氨基甲基，氨基羰基甲基或二烷氧基甲基，X和Y可以相同或不同，各自代表亚甲基或硫，条件是A代表茚满基，茚基或1,2,3， 4-四氢萘基，X和Y代表两个亚甲基，Z代表羟甲基或甲酰基。