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：EP0288575A1

公开(公告)日：1988-11-02

申请号：EP87906939.1

申请日：1987-10-22

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： NAKAO, Toru ,  MORITA, KENJI ,  OBATA, Minoru ,  MORIMOTO, Yasuto

IPC分类号： C07D207/26 ,  C07D239/26 ,  C07D295/14 ,  C07D307/32 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/495 ,  A61K31/505

CPC分类号： C07D207/26 ,  C07D295/112 ,  C07D307/33 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

摘要： Piperazine compounds represented by general formula (1), wherein Ar represents aryl or heteroaryl, A represents lower alkylene, and C = W represents C = 0 or C = NOH) and piperazine compounds represented by general formula (II),


[wherein Ar represents aryl or heteroaryl, A represents alkylene, and Z represents -0- or -NR- (wherein R represents hydrogen, lower alkyl, aryl, aralkyl, acyl, a group represented by formula (III), (wherein R 1 and R 2 , which may be the same or different, each represents hydrogen, lower alkyl, aralkyl or, when taken together, a group forming a 5- to 7- membered heterocyclic ring together with the adjacent nitrogen atom, and B represents lower alkylene) or a group represented by- CONHR 3 (wherein R 3 represents hydrogen, lower alkyl, lower alkenyl or aryl))] or medicinally acceptable acid addition salts thereof. These piperazine compounds have a psychotropic action accompanied with less side effects on a pyramidal outer tract, thus being useful as drugs.

摘要翻译： 式（I）和（II）的哌嗪和（I）的药学上可接受的盐是新的，其中Ar是（杂）芳基（优选苯基选择性地被一个或两个卤素，低级烷基，低级烷氧基或三氟甲基 ）; A是低级亚烷基; Z是O或NR; R为H，低级烷基，芳基，芳烷基，酰基，-B-NR1R2或-CONHR3; R1和R2是H，低级烷基或芳烷基或一起完成5-7元环; B是低级亚烷基; R3是H，低级烷基，低级烯基或芳基; W为0或NOH。 具体要求的是例如 5-（4-（4-（4-（3-三氟甲基苯基）-1-哌嗪基）丁基）苯基）-2-吡咯烷酮。

公开(公告)号：EP0394471A1

公开(公告)日：1990-10-31

申请号：EP89910671.0

申请日：1989-09-20

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： NAKAO, Tohru ,  TANAKA, Hiroshi 345, Oaza-Naoe ,  MORIMOTO, Yasuto ,  TAKEHARA, Shuzo 684-1, Shimomiyanaga 3-chome

IPC分类号： C07D495/04 ,  A61K31/50

CPC分类号： C07D495/04

摘要： Thienocycloheptapyridazine compounds represented by general formula (I), wherein R represents hydrogen, halogen or C 1·4 alkyl, Ar represents aryl or heteroaryl which may have at least one substituent selected from among halogen, C 1·4 alkyl, C 1·4 alkoxy, nitro, amino. hydroxy, trifluoromethyl and C 2·5 alkanoyl, and a bond ---- between the 6a-position and the 7-position represents a single or double bond are disclosed. The compounds are useful as an anti-anxiety agent, amnesia treating agent, brain function activating agent or dementia treating agent.

摘要翻译： 式（I）的噻吩并（2'，3'：6,7）环庚（1,2-c）哒嗪酮是新的：其中R是H，卤素或1-4C烷基; Ar是芳基或杂芳基， substd。 1-4C烷基，1-4C烷氧基，硝基，氨基，羟基，三氟甲基或2-5C烷酰基氨基; 虚线是可选的双键。 具体（I）是例如 9-（4-氯苯基）-2-甲基-5,6,6a，7-四氢-4H-噻吩并（2'，3'：6,7） - 环庚基（1,2-c）哒嗪-8（9H ）-一; 2-溴-9-（4-氯苯基）-5,6-二氢-4H-噻吩并（2'，3'：6,7）环庚（1,2-c）哒嗪-8（9H） - 酮; 和其他十个。