公开(公告)号：EP0424528A1

公开(公告)日：1991-05-02

申请号：EP89905187.4

申请日：1989-05-01

申请人： ZERIA PHARMACEUTICAL CO., LTD.

发明人： OGURA, Kuniyoshi, Zeria Pharmaceutical Co., Ltd. ,  AOTSUKA, Tomoji, Zeria Pharmaceutical Co., Ltd. ,  TORIZUKA, Motoki, Zeria Pharmaceutical Co., Ltd. ,  SOEDA, Mitsuo, Zeria Pharmaceutical Co., Ltd. ,  TANAKA, Yoshiaki, Zeria Pharmaceutical Co., Ltd. ,  KATO, Hisayoshi, Zeria Pharmaceutical Co., Ltd. ,  MIURA, Naoyoshi, Zeria Pharmaceutical Co., Ltd. ,  NAKATA, Naoki, Zeria Pharmaceutical Co., Ltd. ,  MORITA, Hikaru, Zeria Pharmaceutical Co., Ltd. ,  OKUBO, Akihiro, Zeria Pharmaceutical Co., Ltd.

IPC分类号： C07D277/04 ,  C07D211/70 ,  C07D295/18 ,  A61K31/40 ,  A61K31/425 ,  A61K31/435 ,  A61K31/54 ,  C07D207/20

CPC分类号： C07D295/185 ,  C07D207/20 ,  C07D211/70 ,  C07D277/04

摘要： Drugs for improving cerebral circulation, cerebral metabolism and memory containing as the active ingredient a phenylalkanoylamine derivative or its salt represented by general formula (I) (wherein A represents a 1,3-thiazolin-3-yl group, a 1,2,3,6-tetrahydropyridin-1-yl group, a morpholino group, a thiomorpholin-4-yl group or a 3-pyrrolin-1-yl group, R¹ and R² may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group or (α) (wherein R³ and R⁴ each represents a lower alkyl group or, when taken together, they represent a 5- or 6-membered heterocyclic group together with the nitrogen atom), and n represents an integer of 2 to 6) and novel phenylalkanoylamine derivatives among the compounds represented by (I), and a process for their preparation are disclosed. The above drugs are useful for treating sequelae of cerebral hemorrhage, sequelae of cerebral infarction, arterial aclerosis of brain, sequelae of subarachnoidal hemorrhage, sequelae of head trauma, sequelae of cerebral operation, dementia of cerebral vessel origin, Parkinson's disease, Alzheimer's disease, Pick's disease, sequelae of hypoxia, alcoholic cerebral diseases, etc.

摘要翻译： 用于改善脑循环，大脑代谢和记忆的药物，其含有通式（I）表示的苯基烷酰基胺衍生物或其盐作为活性成分（其中A表示1,3-噻唑啉-3-基，1,2,3 ，6-四氢吡啶-1-基，吗啉代基，硫代吗啉-4-基或3-吡咯啉-1-基，R 1和R 2可以相同或不同，各代表氢原子，卤素 低级烷基，低级烷氧基，硝基，氨基或（α）（其中R 3和R 4各自代表低级烷基，或者当合在一起时，它们代表5或6元杂环 与氮原子一起形成的基团），n表示2至6的整数）和由（I）表示的化合物中的新型苯基烷酰基胺衍生物及其制备方法。 上述药物可用于治疗脑出血后遗症，脑梗塞后遗症，脑动脉硬化症，蛛网膜下腔出血后遗症，头部创伤后遗症，脑手术后遗症，脑血管源性痴呆，帕金森病，阿尔茨海默氏病，Pick's 疾病，缺氧后遗症，酒精性脑病等。