公开(公告)号：EP0551527A1

公开(公告)日：1993-07-21

申请号：EP92916818.5

申请日：1992-08-06

申请人： SUNTORY LIMITED

发明人： MIZUNO, Akira ,  CHO, Hidetsura ,  MIYA, Mikiko ,  TATSUOKA, Toshio ,  ISHIHARA, Takafumi

IPC分类号： C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04

摘要： A pyrroloazepine derivative represented by general formula (I), a salt thereof, a process for the production thereof, and a remedy for the diseases of circulatory organs containing the same as the active ingredient. In formula (I) Z₁ represents H when there is a bond represented by the broken line, whereas when there is no such a bond, Z₁ represents H and Z₂ represents OH, or alternatively Z₁ and Z₂ are combined together to represent O or NOR₁ (wherein R₁ represents H, alkyl, etc.); R represents H, alkyl, etc.; A represents alkylene, alkenylene or alkynylene each of which may be substituted with one OH group ; and Y represents (α) or (β) wherein R₂ and R₃ represent each H, alkyl, etc.; R₄ and R₅ represent each H or alkyl; B represents carbonyl, sulfonyl, etc.; m represents 1 or 2; n represents 0 or 1; and D represents alkoxy, aromatic heterocyle, etc.

摘要翻译： 由通式（I）表示的吡咯并氮杂衍生物，其盐，其制备方法以及含有该化合物作为有效成分的循环器官疾病的治疗剂。 在式（Ⅰ）中，Z 1代表H，当用虚线表示键时，而当没有这种键时，Z 1代表H，Z 2代表OH，或者Z 1和Z 2结合在一起代表O或NOR 1 其中R 1代表H，烷基等）; R代表H，烷基等; A代表各自可以被一个OH基团取代的亚烷基，亚烯基或亚炔基; Y代表（α）或（β），其中R 2和R 3各代表H，烷基等; R 4和R 5分别代表H或烷基; B代表羰基，磺酰基等; m代表1或2; n代表0或1; D代表烷氧基，芳香族杂环等

公开(公告)号：EP0557526B1

公开(公告)日：2003-04-02

申请号：EP92916814.4

申请日：1992-08-06

申请人： SUNTORY LIMITED

发明人： MIZUNO, Akira ,  MIYA, Mikiko ,  INOMATA, Norio ,  TATSUOKA, Toshio ,  ISHIHARA, Takafumi

IPC分类号： C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04

公开(公告)号：EP0551527B1

公开(公告)日：2003-04-02

申请号：EP92916818.5

申请日：1992-08-06

申请人： SUNTORY LIMITED

发明人： MIZUNO, Akira ,  CHO, Hidetsura ,  MIYA, Mikiko ,  TATSUOKA, Toshio ,  ISHIHARA, Takafumi

IPC分类号： C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04

公开(公告)号：EP0557526A1

公开(公告)日：1993-09-01

申请号：EP92916814.4

申请日：1992-08-06

申请人： SUNTORY LIMITED

发明人： MIZUNO, Akira ,  MIYA, Mikiko ,  INOMATA, Norio ,  TATSUOKA, Toshio ,  ISHIHARA, Takafumi

IPC分类号： C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04

摘要： A pyrroloazepine compound represented by general formula (I) or (II), a salt thereof, a process for the production thereof, and a remedy for the diseases of circulatory organs containing the same as the active ingredient. In general formula (I) or (II) Z₁ represents H when there is a bond represented by the broken line, whereas when there is no such a bond, Z₁ represents H and Z₂ represents OH, or alternatively Z₁ and Z₂ are combined together to represent O or NOR₁ (wherein R₁ represents H, alkyl, aryl or aralkyl); R represents alkyl, cycloalkyl, cyclalkyl-alkyl, aryl or aralkyl; A represents alkylene, alkenylene or alkynylene; and Y represents optionally substituted heterocycle or (α) wherein R₂ and R₃ represent each H, alkyl, lower alkoxy, aryloxy-substituted alkyl, aryl or aralkyl.

摘要翻译： 由通式（I）或（II）表示的吡咯并氮杂化合物，其盐，其制备方法和含有该化合物作为活性成分的循环器官疾病的治疗剂。 在通式（Ⅰ）或（Ⅱ）中，当存在由虚线表示的键时，Z 1代表H，而当没有这种键时，Z 1代表H，Z 2代表OH，或者Z 1和Z 2一起结合到 代表O或NOR 1（其中R 1代表H，烷基，芳基或芳烷基）; R代表烷基，环烷基，环烷基 - 烷基，芳基或芳烷基; A代表亚烷基，亚烯基或亚炔基; Y代表任选取代的杂环或（α），其中R 2和R 3分别代表H，烷基，低级烷氧基，芳氧基取代的烷基，芳基或芳烷基。

公开(公告)号：EP0908182A1

公开(公告)日：1999-04-14

申请号：EP97937845.2

申请日：1997-08-29

申请人： SUNTORY LIMITED

发明人： ISHIHARA, Takafumi ,  KANAYAMA, Yoshiharu ,  OKAMURA, Mikio ,  YOSHIKAWA, Junichi ,  SHINTAKU, Haruo

IPC分类号： A61K31/505

CPC分类号： A61K31/525 ,  A61K31/519 ,  C07D475/04

摘要： It is an object of the present invention to provide a therapeutic agent for effectively preventing or ameliorating diseases caused by dysfunction of NOS.
The present invention provides a pharmaceutical composition for preventing and/or treating diseases associated with dysfunction of NOS, comprising as an effective ingredient, a compound of the formula (I):
wherein R 1 and R 2 each represents a hydrogen atom or, taken together with each other, represent a single bond, while R 3 represents -CH(OH)CH(OH)CH 3 , -CH(OCOCH 3 )CH(OCOCH 3 )CH 3 , -CH 3 , - CH 2 OH, or a phenyl group when R 1 and R 2 each represents a hydrogen atom, or -COCH(OH)CH 3 when R 1 and R 2 together represent a single bond, or a pharmaceutically acceptable salt thereof.