公开(公告)号：EP0308515A1

公开(公告)日：1989-03-29

申请号：EP88902569.8

申请日：1988-03-17

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： NAKAO, Toru ,  MORITA, Kenji ,  HISADOME, Masao ,  TAKEHARA, Shuzo

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： Thienocinnoline compounds represented by general for-
(wherein R represents hydrogen, halogen or lower alkyl, Ar represents aryl, heteroaryl, or aryl or heteroaryl having at least one substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and lower alkanoylamino, and between 5a-position and 6-position represents either a single or a double bond) useful as anti-anxious agents, amnesia treating agents, brain function activating agents, anti-dement agents or bioprotection accelerating agents.

摘要翻译： （其中R代表氢，卤素或低级烷基，Ar代表具有至少一个选自卤素，低级烷基，低级烷氧基，硝基，氨基的取代基的芳基，杂芳基或芳基或杂芳基的噻吩并喹啉化合物 ，羟基，三氟甲基和低级烷酰基氨基，以及5a-位和6-位之间代表单键或双键），用作抗焦虑剂，遗忘症治疗剂，脑功能活化剂，抗痴呆剂或生物保护促进剂 。

公开(公告)号：EP0308515B1

公开(公告)日：1994-01-26

申请号：EP88902569.8

申请日：1988-03-17

申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

发明人： NAKAO, Toru ,  MORITA, Kenji ,  HISADOME, Masao ,  TAKEHARA, Shuzo

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： Thienocinnoline compounds represented by general formula (I) (wherein R represents hydrogen, halogen or lower alkyl, Ar represents aryl, heteroaryl, or aryl or heteroaryl having at least one substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and lower alkanoylamino, and ----- between 5a-position and 6-position represents either a single or a double bond) useful as anti-anxious agents, amnesia treating agents, brain function activating agents, anti-dement agents or bioprotection accelerating agents.

摘要翻译： 由通式（I）表示的噻吩并喹啉化合物（其中R代表氢，卤素或低级烷基，Ar代表具有至少一个选自卤素，低级烷基，低级烷氧基，硝基的取代基的芳基，杂芳基或芳基或杂芳基 ，氨基，羟基，三氟甲基和低级烷酰基氨基，以及在5a-位和6-位之间代表单键或双键），用作抗焦虑剂，遗忘症治疗剂，脑功能活化剂，抗 代谢剂或生物保护促进剂。

公开(公告)号：EP0252990A1

公开(公告)日：1988-01-20

申请号：EP87900297.0

申请日：1986-12-27

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： NAKAO, Toru ,  KAWAKAMI, Minoru ,  MORIMOTO, Yasuto ,  TAKEHARA, Shuzo ,  TAHARA, Tetsuya

IPC分类号： C07D495/04 ,  A61K31/50 ,  C07D237/00 ,  C07D335/00

CPC分类号： C07D495/04

摘要： Benzothiopyrano(4,3-C)pyridazine compounds represented by general formula (I), wherein R 1 and R 2 , which may be the same or different, each represents hydrogen, halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, Ci- 4 alkyl, C 1-4 alkoxy or C 2-5 alkanoylamido, R 3 represents hydrogen, C 1-8 alkyl, hydroxy-C 1-4 alkyl, C 2-5 alkanoyloxy-C 1-4 alkyl, pyridyi, aryl, aryl-C 1 - 4 alkyl, or aryl or aryl-C 1-4 alkyl having on the aromatic ring at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, C 1-4 alkyl, C 1-4 alkoxy and C 2-5 alkanoylamido, n represents 0,1 or 2, and a bond - between the 4-position and 4a-position represents a single bond or a double bond. A process for their preparation, and the use thereof are disclosed. These compounds have an anti-anxiety effect, and are useful as drugs.

摘要翻译： 式（I）的苯并噻喃（4,3-c）哒嗪是新的：其中R1和R2是H，卤素，三氟戊基，OH，氨基，硝基，氰基，1-4C烷基，1-4C烷氧基或2-5C烷酰基酰氨基 ; R3是H，1-8C烷基，羟基 - （1-4C）烷基，（2-5C烯氧基） - （1-4C）烷基，吡啶基或芳基或芳基 - （1-4C）烷基，其中芳环带 硝基，氰基，1-4C烷基，1-4C烷氧基或2-5C烷酰基酰胺基gp;至少一个卤素，三氟甲基，OH，氨基，硝基，氰基， n为0,1或2; 虚线表示4-4a连接可以是单键或双键。 优选R 1和R 2 = H，卤素或1-4C烷基; R3 =具有至少一个卤原子的芳环的芳基; n = 0,1或2; 4-4a连接是单键。 2-（4-氯苯基）-2,3,4,4a-四氢-5H-1-苯并噻喃（4,3-c）哒嗪-3-酮6-氧化物及其（4aR，6R）和（4aR，S ）异构体 2-（4-氯苯基）-9-氟-2,3,4a-四氢-5H-1-苯并噻喃（4,3-c）哒嗪-3-酮6-氧化物和其它四种化合物。 cpds的反应。 （II）和（III）：和所得腙环化。 产品 （I）可以被修饰以给出其它（I），例如 通过氧化。 （I，n = 0）给出（I，n = 1）或（I，n = 2）; 或（I，R3 = H）与R4X（其中R4为1-4C烷基，羟基 - （1-4C）烷基，（2-5C烷酰氧基） - （1-4C）烷基或芳基 - （1-4C） ）烷基; X是反应性gp。）; 或通过溴化和消除（I，4-4a链接是单带），得到（I，4-4a链接是双键）。

公开(公告)号：EP0190367B1

公开(公告)日：1990-01-17

申请号：EP85904155.0

申请日：1985-08-26

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： TAHARA, Tetsuya ,  KAWAKAMI, Minoru ,  TAKEHARA, Shuzo ,  SAKAMORI, Masamitsu

IPC分类号： C07D237/36 ,  A61K31/50

CPC分类号： C07D401/04 ,  C07D237/36

摘要： Benzo ADh BDcinnoline compounds represented by general formula (I) wherein X and Y each represents hydrogen, halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, amino, C2-4 alkanoylamido, nitro, cyano, or C2-4 alkanoyl, Ar represents phenyl or pyridyl optionally having at least one of halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, amino, C2-4 alkanoylamido, nitro, and cyano, and dotted line represents a single or double bond), a process for their preparation, and a medicinal composition containing them. These compounds possess a strong affinity for benzodiazepine receptor and an anti-anxiety effect and are therefore useful for neutralizing excess administration anti-anxiety agents or as an anti-anxiety agent itself.

公开(公告)号：EP0190367A1

公开(公告)日：1986-08-13

申请号：EP85904155.0

申请日：1985-08-26

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： TAHARA, Tetsuya ,  KAWAKAMI, Minoru ,  TAKEHARA, Shuzo ,  SAKAMORI, Masamitsu

IPC分类号： C07D237/36 ,  A61K31/50

CPC分类号： C07D401/04 ,  C07D237/36

摘要： Benzo[h]cinnoline compounds represented by general formula (I) wherein X and Y each represents hydrogen, halogen, trifluoromethyl, hydroxy, C 1-4 alkyl, C 1-4 alkoxy, amino, C 2-4 alkanoylamido, nitro, cyano, or C 2-4 alkanoyl, Ar represents phenyl or pyridyl optionally having at least one of halogen, trifluoromethyl, hydroxy, C 1-4 alkyl, C 1-4 alkoxy, amino, C 2-4 alkanoylamido, nitro, and cyano, and dotted line represents a single or double bond), a process for their preparation, and a medicinal composition containing them. These compounds possess a strong affinity for benzodiazepine receptor and an anti-anxiety effect and are therefore useful for neutralizing excess administration anti-anxiety agents or as an anti-anxiety agent itself.