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1. 发明申请

WO1998000400A1 TETRAHYDROBENZINDOLE COMPOUNDS 审中-公开
标题翻译：四氢化萘化合物
公开(公告)号：WO1998000400A1
公开(公告)日：1998-01-08
申请号：PCT/JP1997002226
申请日：1997-06-27
申请人： MEIJI SEIKA KAISHA, LTD. , KOYAMA, Masao , KIKUCHI, Chika , USHIRODA, Osamu , ANDO, Takashi , NAGASO, Hiroshi , FUJI, Kazuyuki , OKUNO, Masayo , HIRANUMA, Toyokazu
发明人： MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D209/92
CPC分类号： C07D401/06 , C07D209/92 , C07D401/12 , C07D403/12
摘要： Compounds represented by general formula (I) and pharmaceutically acceptable salts thereof which strongly inhibit [ H]-serotonin and [ H]-5-CT binding to the human serotonin 5-HT7 receptor subtype expressed in a cultured cell line and can provide medicinal compositions for treating or preventing mental diseases. In said formula (I) A represents N, CH, C having a double bond or CR ; B and Z independently represent each N, CH or CR , provided that A is N when B and/or Z is N; R represents hydrogen, halogeno, lower alkyl, cyano, trihalomethyl, hydroxy, alkoxy, alkylthio, alkylsulfenyl, alkylsulfonyl, alkoxycarbonyl, sulfamoyl, optionally substituted amino, optionally alkylated carbamoyl, acyl or carboxy; R represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl or aralkyl; R represents hydrogen, halogeno, lower alkyl, hydroxyl, alkoxy, acyl, alkoxycarbonyl, nitro, optionally substituted amino, optionally alkylated carbamoyl or acyloxy; R represents lower alkyl, cyano, carbamoyl, carboxy, acyl, acyloxy, alkoxy, alkoxycarbonyl, trihalomethyl or hydroxy; and n is an integer of from 2 to 6.
摘要翻译：由通式（I）表示的化合物及其药学上可接受的盐，其强力抑制在培养细胞中表达的人5-羟色胺5-HT7受体亚型的[3 H] - 血清素和[3 H] -5-CT结合可以提供用于治疗或预防精神疾病的药物组合物。在所述式（I）中，A表示具有双键或CR 5的N，CH，C; B和Z独立地表示每个N，CH或CR 1，条件是当B和/或Z为N时A为N; R 1表示氢，卤代，低级烷基，氰基，三卤代甲基，羟基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷氧基羰基，氨磺酰基，任选取代的氨基，任选烷基化的氨基甲酰基，酰基或羧基; R 2表示氢或低级烷基; R 3表示氢，低级烷基或芳烷基; R 4表示氢，卤代，低级烷基，羟基，烷氧基，酰基，烷氧基羰基，硝基，任选取代的氨基，任选烷基化的氨基甲酰基或酰氧基; R 5代表低级烷基，氰基，氨基甲酰基，羧基，酰基，酰氧基，烷氧基，烷氧基羰基，三卤代甲基或羟基; n为2〜6的整数。

2. 发明申请

WO1996033194A1 BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS MODULATORS OF THE GABA A RECEPTOR COMPLEX 审中-公开
标题翻译：苯并咪唑化合物及其作为GABA受体复合物的调节剂
公开(公告)号：WO1996033194A1
公开(公告)日：1996-10-24
申请号：PCT/EP1996001606
申请日：1996-04-17
申请人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, LTD. , TEUBER, Lene , WÄTJEN, Frank , FUKUDA, Yoshimasa , USHIRODA, Osamu , SASAKI, Toshiro
发明人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D405/14
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof or an oxide thereof, wherein R is (II), wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH; R is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, alkoxy, phenyl, halogen, CF3, amino, nitro, cyano, acyl, acylamino, phenyl and monocyclic heteroaryl; and one of R and R is hydrogen and the other is furanyl or isoxazolyl each of which may be substituted one or more times with substituents selected from halogen, alkyl, alkoxy and phenyl. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐或其氧化物，其中R 3为（II），其中A，B和D各自为CH，或A，B中的一种或两种 D为N，其余为CH; R 11是苯基，苯并咪唑基或单环杂芳基，其全部可以被选自烷基，烷氧基，苯基，卤素，CF 3，氨基，硝基，氰基，酰基，酰氨基，苯基和单环杂芳基的取代基取代一次或多次 ; R 6和R 7中的一个是氢，另一个是可以被选自卤素，烷基，烷氧基和苯基的取代基取代一次或多次的呋喃基或异恶唑基。该化合物可用于治疗各种中枢神经系统疾病如癫痫和其他惊厥性疾病，焦虑症，睡眠障碍和记忆障碍。

3. 发明申请

WO1996033191A1 BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS MODULATORS OF THE GABAA RECEPTOR COMPLEX 审中-公开
标题翻译：苯并咪唑化合物及其作为GABA A受体复合物的调节剂
公开(公告)号：WO1996033191A1
公开(公告)日：1996-10-24
申请号：PCT/EP1996001649
申请日：1996-04-19
申请人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, LTD. , TEUBER, Lene , WÄTJEN, Frank , FUKUDA, Yoshimasa , USHIRODA, Osamu , SASAKI, Toshiro
发明人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D401/10
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R is (II) wherein A, B, and D each is CH, or one or two of A, B and D is N and the others are CH; R is phenyl, benzimidazolyl, or monocyclic heteroaryl, all of which may be substituted one or more times with substituents selected from alkyl, alkoxy, halogen, CF3, amino, nitro, cyano, acylamino, acyl, phenyl and monocyclic heteroaryl; one of R and R is hydrogen and the other is -CR'=NOR'', wherein R' and R'' each independently are hydrogen, alkyl, alkenyl, alkynyl or phenyl. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
摘要翻译：本专利申请公开了具有式（I）化合物或其药学上可接受的盐或其氧化物，其中R 3为（II）其中A，B和D各自为CH，或A，B和 D为N，其余为CH; R 11是苯基，苯并咪唑基或单环杂芳基，它们都可以被选自烷基，烷氧基，卤素，CF 3，氨基，硝基，氰基，酰氨基，酰基，苯基和单环杂芳基的取代基取代一次或多次。 R 6和R 7中的一个是氢，另一个是-CR'= NOR“，其中R'和R”各自独立地是氢，烷基，烯基，炔基或苯基。该化合物可用于治疗各种中枢神经系统疾病如癫痫和其他惊厥性疾病，焦虑症，睡眠障碍和记忆障碍。

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